Pharmaceutical composition, treatment method for a patient suffering from allergic rhinitis

Description

1 / 54 “NASAL SPRAY COMPOSITION” RELATED REQUEST

[0001] This application claims the benefit of Indian provisional patent application No. 202321078834, filed on November 21, 2023, the full disclosure of which is incorporated by reference herein. FIELD OF THE INVENTION

[0002] The present invention relates to a pharmaceutical composition in the form of an aqueous suspension suitable for nasal administration. The composition comprises mometasone furoate or a hydrate thereof, olopatadine or a pharmaceutically acceptable salt thereof (e.g., olopatadine hydrochloride), and a means for controlling obstruction of an actuator and / or immersion tube in a spray device from which the composition is administered. The composition is suitable for providing consistent delivery, for example, for at least 30 days without obstruction in the actuator or immersion tube of a nasal spray device. The present invention also relates to a process for preparing the composition in the form of an aqueous suspension. BACKGROUND OF THE INVENTION

[0003] Nasal spray devices for delivering an active ingredient to the nasal cavity, primarily the nasal mucosa, can be useful for the prophylaxis and / or treatment of certain diseases and disorders of the nasal cavity. Such devices are also capable of delivering a drug to the systemic circulation via the turbinates and lymphoid tissues located in the posterior part of the nasal cavity and to the central nervous system via the olfactory region at the top of the nasal cavity.

[0004] Nasal spray pharmaceutical products contain therapeutically active ingredients dissolved or suspended in solutions or mixtures of excipients, such as preservatives, viscosity modifiers, emulsifiers, buffering agents in dispensers. Petition 870260061385, dated 06 / 23 / 2026, page 9 / 67 2 / 54 non-pressurized devices that deliver a spray containing a measured dose of the active ingredient. The dose may be measured by the spray pump or may be pre-measured during manufacturing. A nasal spray unit may be designed for unit dosing or may discharge up to several hundred measured sprays of formulation containing the pharmacological substance.

[0005] The dose can be delivered by the integral pump components of the canister closure system to the intranasal cavity by nasal spray for local and / or systemic effects.

[0006] The container closure system for these pharmaceutical products comprises a container, a closure, an actuator, and a pump. It may also include protective packaging comprising a dust cap. Regardless of the design, the most crucial attributes of such nasal sprays are dose reproducibility, spray plume, spray content uniformity, and droplet size distribution. These parameters are significant and can affect drug delivery to the intended administration site and biological target.

[0007] A metered nasal spray composition comprising mometasone furoate and olopatadine hydrochloride is disclosed in international publication no. WO 2015 / 036902. Although such compositions are stable, they may result in obstruction of the actuator and / or immersion tube, which may impact the consistent delivery of the metered nasal spray suspension.

[0008] To control such obstruction problems associated with metered-dose nasal spray devices, a patient information leaflet typically instructs the patient to clean the spray pump tip with a clean, dry tissue or cloth and to hold the spray pump unit and push the dust cap back onto the spray pump tip of the bottle after use. However, if the patient does not follow the instructions properly, the patient may Petition 870260061385, dated 06 / 23 / 2026, page 10 / 67 3 / 54 find inconsistent delivery due to obstruction of the actuator and / or immersion tube. Consequently, such patient instruction is typically not an efficient solution to control obstruction problems associated with metered-dose nasal spray devices.

[0009] There is a need for new methods to control obstruction problems associated with compositions comprising mometasone furoate or a hydrate thereof and olopatadine hydrochloride delivered by metered-dose nasal spray devices. The present invention addresses such needs. SUMMARY OF THE INVENTION

[0010] In one aspect, the present invention is directed to a pharmaceutical composition comprising mometasone, an ester thereof (e.g., mometasone furoate) or a salt thereof and olopatadine or a salt thereof (e.g., olopatadine hydrochloride) and a means for controlling obstruction associated with a nasal spray device (e.g., a metered-dose nasal spray device). The means for controlling obstruction may be a decongestant. The pharmaceutical composition is suitable for a nasal spray device comprising an actuator and a dip tube through which the composition is to be delivered. The means for controlling obstruction (such as by including a decongestant) prevents or minimizes obstruction in the actuator and / or dip tube of the nasal spray device.

[0011] In one embodiment, the pharmaceutical composition can be used for the treatment of allergic rhinitis in a human individual.

[0012] The addition of a means to control obstruction (e.g., a decongestant) to the pharmaceutical composition achieves consistent dosing of the mometasone and olopatadine components and prevents obstruction of an actuator and / or nasal spray immersion tube.

[0013] In one embodiment, the composition comprises mometasone furoate, olopatadine hydrochloride and a decongestant. Petition 870260061385, dated 06 / 23 / 2026, page 11 / 67 4 / 54

[0014] In one embodiment, the pharmaceutical composition is an aqueous suspension comprising a hydrocolloid, wherein mometasone (or an ester thereof, for example, mometasone furoate, or a salt thereof) is present in particulate form, and olopatadine or a salt thereof (for example, olopatadine hydrochloride) is present in dissolved form. In one embodiment, the pharmaceutical composition comprises an amount of a hydrocolloid such that the pharmaceutical composition has a viscosity of about 10 cps to about 200 cps, as of about 20 cps to about 150 cps or of about 20 cps to about 120 cps. The pharmaceutical composition may comprise approximately 0.001% w / w to approximately 0.075% w / w of mometasone, an ester thereof (e.g., mometasone furoate) or a salt thereof in particulate form, and approximately 0.5% w / w to approximately 0.8% w / w of olopatadine or a salt thereof (e.g., olopatadine hydrochloride) in dissolved form.

[0015] In one embodiment, the pharmaceutical composition comprises about 0.001% w / w about 0.075% w / w of mometasone, an ester thereof (e.g., mometasone furoate), or a salt thereof in particulate form and about 0.5% w / w about 0.8% w / w of olopatadine or its salt (e.g., olopatadine hydrochloride) in dissolved form, and a means for controlling the obstruction of a nasal spray actuator and / or immersion tube, as a decongestant.

[0016] In another embodiment, the pharmaceutical composition comprises about 0.025% w / w about 0.05% w / w of mometasone, an ester thereof (for example, mometasone furoate), or a salt thereof in particulate form, about 0.5% w / w about 0.8% w / w of olopatadine or its salt (for example, olopatadine hydrochloride), and about 0.05% w / w about 5% w / w of a decongestant.

[0017] In yet another embodiment, the pharmaceutical composition comprises about 0.025% w / w or about 0.05% w / w of mometasone, an ester thereof (for example, mometasone furoate), or a salt of mometasone. Petition 870260061385, dated 06 / 23 / 2026, p. 12 / 67 5 / 54 same in particulate form, approximately 0.6% w / w approximately 0.7% w / w of olopatadine or its salt (e.g., olopatadine hydrochloride), and approximately 0.05% w / w approximately 5% w / w of a decongestant.

[0018] In yet another embodiment, the pharmaceutical composition comprises about 0.025% w / w about 0.05% w / w of mometasone, an ester thereof (for example, mometasone furoate) or a salt thereof in particulate form, about 0.6% w / w about 0.7% w / w of olopatadine or its salt (for example, olopatadine hydrochloride), and about 0.1% w / w about 5% w / w of a decongestant.

[0019] In yet another embodiment, the pharmaceutical composition comprises about 0.025% w / w about 0.05% w / w of mometasone furoate in particulate form, about 0.6% w / w about 0.7% w / w of olopatadine hydrochloride, and about 0.1% w / w about 3% w / w of a decongestant.

[0020] In another embodiment, the pharmaceutical composition comprises mometasone furoate in an amount of about 0.025% w / w in particulate form, olopatadine hydrochloride in an amount of about 0.665% w / w in dissolved form, and a means for controlling obstruction in an actuator from which the composition is delivered to facilitate consistent delivery of the composition.

[0021] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human comprising about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrochloride and about 0.05% w / w about 5% w / w of glycerol.

[0022] In yet another embodiment, the pharmaceutical composition described herein comprises glycerol in an amount of about 0.05% w / w about 3% w / w, about 0.05% w / w about 2% w / w, or about 0.05% w / w about 1% w / w. Petition 870260061385, dated 06 / 23 / 2026, p. 13 / 67 6 / 54

[0023] In yet another embodiment, the pharmaceutical composition described herein comprises glycerol in an amount of about 0.075% w / w about 3% w / w, about 0.075% w / w about 2% w / w, or about 0.075% w / w about 1% w / w.

[0024] In yet another embodiment, the pharmaceutical composition described herein comprises glycerol in an amount of about 0.05% w / w, about 0.06% w / w, about 0.07% w / w, about 0.075% w / w, about 0.08% w / w, about 0.085% w / w, about 0.09% w / w, about 0.25% w / w, about 0.27% w / w, about 0.28% w / w, about 0.3% w / w, about 0.4% w / w, about 0.5% w / w, about 1% w / w, about 2% w / w or about 3% w / w.

[0025] In another embodiment, the dispensing device (such as a nasal spray actuator and a pump) dispenses approximately 100 µl of the pharmaceutical composition per actuation, wherein a single actuation dispenses 665 μg of olopatadine hydrochloride and approximately 25 μg or approximately 50 μg of mometasone furoate (preferably 25 μg of mometasone furoate).

[0026] In additional embodiments, the dispensing device may include a container, a lid, and a dispenser head which may include a pump, a dip tube, an actuator, a dispensing channel, and a dispensing orifice. The pump is designed to dispense the pharmaceutical composition through the dip tube to the pump via the actuator fitted with the dispensing orifice. The pharmaceutical composition is released in the form of a uniform spray. The pump may operate in tandem with the actuator, which allows for easy opening and closing of the pump and provides a desired spray characteristic. Actuators include, but are not limited to, spray actuators, foam actuators, solid current actuators, and special actuators. The Petition 870260061385, dated 06 / 23 / 2026, page 14 / 67 The 7 / 54 dispensing device delivers a nasal spray in a uniform dose of, for example, mometasone (e.g., as mometasone furoate) and olopatadine (e.g., as olopatadine hydrochloride), wherein the dose is dispensed each time the dispensing device is actuated by a user.

[0027] The dispensing device may require preparation, for example, by about 2-6 actuations, to consistently dispense the composition. The device can be prepared by releasing 6 sprays or until a fine mist appears. The droplet size of the nasal spray can be controlled by the size of the dispensing orifice of the container. The size of the dispensing orifice can also influence characteristics of the spray pattern. BRIEF DESCRIPTION OF THE DRAWING

[0028] The present invention is best understood with reference to the following description taken in combination with the drawing. For illustrative purposes, certain embodiments of the present invention are shown in the drawing. It should be understood, however, that the invention is not limited to the precise arrangements, dimensions and instruments shown:

[0029] Figure 1 illustrates a nasal spray device comprising a container, immersion tube, nasal spray pump, actuator, actuator tip and dust cap and pharmaceutical composition of the present invention. DETAILED DESCRIPTION OF THE INVENTION

[0030] In a nasal spray product comprising a suspension formulation, a patient information leaflet typically instructs the patient to clean the spray pump tip with a clean, dry tissue or cloth and to hold the spray pump unit and push the dust cap back onto the spray pump tip of the bottle after use. However, typically, patients themselves Petition 870260061385, dated 06 / 23 / 2026, page 15 / 67 8 / 54 forget to clean the tip actuator, or improperly fit the dust cap, which can result in obstruction of the actuator and / or immersion tube. Such obstruction further leads to a lack of reproducibility of dose uniformity, spray plume, spray content uniformity, and droplet size distribution. These problems, then, cause inappropriate drug delivery to the nasal cavity.

[0031] The present inventors have surprisingly and unexpectedly found that the addition of a deblocking agent can substantially control blockage in the actuator and / or immersion tube.

[0032] In one aspect, the present invention is directed to a pharmaceutical composition for nasal administration to a human individual for the treatment of rhinitis, wherein the composition comprises mometasone, an ester thereof (for example, mometasone furoate), or a salt thereof and olopatadine or its salt (for example, olopatadine hydrochloride) and a means for controlling obstruction associated with a nasal spray device (for example, a metered-dose nasal spray device).

[0033] In another aspect, the present invention is directed to a dispensing device containing a pharmaceutical composition comprising mometasone, an ester thereof (for example, mometasone furoate) or a salt thereof and olopatadine or its salt (for example, olopatadine hydrochloride) and a means for controlling obstruction problems associated with a metered-dose nasal spray device.

[0034] In one embodiment, the means of controlling the obstruction is a deblocking agent. Suitable deblocking agents include, but are not limited to, sugar alcohols (polyols), polyethers, or any combination thereof.

[0035] In one embodiment, the unblocking agent is glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol, or any combination of any of the foregoing.

[0036] In one embodiment, the unblocking agent is Petition 870260061385, dated 06 / 23 / 2026, page 16 / 67 9 / 54 present in the pharmaceutical composition in a quantity sufficient to control actuator clogging, for example, during storage at 25 °C and 60% relative humidity (RH), or 30 °C and 65% RH, or 30 °C and 75% RH, or 40 °C and 75% RH for 1, 2, 3, 4, 5 or 6 months. In another embodiment, the unclogging agent is present in the pharmaceutical composition in an amount of about 0.01% w / w to about 5% w / w, based on the total weight of the pharmaceutical composition. In yet another embodiment, the unclogging agent is present in the pharmaceutical composition in an amount of about 0.05% w / w to about 5% w / w (as from about 0.05% to about 2% w / w), based on the total weight of the pharmaceutical composition.

[0037] Such nasal spray compositions offer the advantage that patients do not need to clean the actuator tip after each use and no obstruction is observed, even if the cap is not properly fitted to the dispensing device, for example, for up to 30 days.

[0038] Another embodiment is a pharmaceutical composition comprising mometasone furoate in an amount of about 0.025% w / w in particulate form, olopatadine hydrochloride in an amount of about 0.665% w / w in dissolved form, and a means for controlling obstruction in an actuator from which the composition is delivered to facilitate consistent delivery of the composition.

[0039] In another embodiment, the addition of a decongestant to a pharmaceutical composition (e.g., an aqueous suspension composition) comprising mometasone furoate and olopatadine hydrochloride controls (or prevents, reduces or suppresses) the obstruction of a nasal spray actuator and / or immersion tube (through which the pharmaceutical composition is delivered) for at least 5 days (e.g., when stored at 25 ± 2 °C and 60 % ± 5 % relative humidity), when the dispensing device remains open without a cap. Petition 870260061385, dated 06 / 23 / 2026, page 17 / 67 10 / 54 dust on the same.

[0040] In any embodiment of any of the pharmaceutical compositions described herein, the pharmaceutical composition is stored under standard conditions (at 25 ± 2 °C and 60 % ± 5 % relative humidity).

[0041] In another embodiment, the addition of a decongestant to a pharmaceutical composition (e.g., an aqueous suspension composition) comprising mometasone furoate and olopatadine hydrochloride controls (or prevents, reduces or suppresses) the obstruction of a nasal spray actuator and / or immersion tube for at least about 10 days, when the dispensing device remains open without a dust cap placed on it.

[0042] In one embodiment, the addition of a decongestant to a pharmaceutical composition (e.g., an aqueous suspension composition) comprising mometasone furoate and olopatadine hydrochloride controls (or prevents, reduces or suppresses) the obstruction of a nasal spray actuator and / or immersion tube for at least about 15 days, when the dispensing device remains open without placing a dust cap on it.

[0043] An embodiment is a pharmaceutical composition (for example, an aqueous suspension composition) comprising mometasone furoate, olopatadine hydrochloride and a sufficient amount of a decongestant to control (or reduce or suppress) the obstruction of a nasal spray actuator and / or immersion tube (for example, for at least about 30 days), when the dispensing device remains open without placing a dust cap on it.

[0044] In another aspect, the addition of a decongestant to a pharmaceutical composition (for example, an aqueous suspension composition) comprising mometasone furoate and olopatadine hydrochloride controls (or prevents, reduces or suppresses) obstruction Petition 870260061385, dated 06 / 23 / 2026, page 18 / 67 11 / 54 of a nasal spray actuator and / or immersion tube for at least about 5 days, such as for about 10 days, for about 15 days, or for about 30 days, when the dispensing device remains open without placing a dust cap on it.

[0045] In one embodiment, the addition of a decongestant to an aqueous suspension composition controls (or prevents, reduces or suppresses) the obstruction of the nasal spray actuator and / or immersion tube for approximately 15 days, approximately 20 days, approximately 25 days, approximately 30 days when the dispensing device remains open without placing a dust cap on it.

[0046] In another embodiment, the addition of a decongestant to an aqueous suspension composition controls the obstruction of a nasal spray actuator and / or immersion tube for about 5 days to about 30 days, for about 5 days to about 25 days, for about 5 days to about 20 days, for about 5 days to about 15 days, for about 5 days to about 10 days when the dispensing device remains open without placing a dust cap on it.

[0047] In another embodiment, the addition of a decongestant to an aqueous suspension composition controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 8 days, approximately 12 days, approximately 16 days, approximately 22 days, approximately 28 days when the dispensing device remains open without placing a dust cap on it.

[0048] In another embodiment, the addition of a decongestant to an aqueous suspension composition controls the obstruction of a nasal spray actuator and / or immersion tube for about 7 days to about 17 days, for about 10 days to about 20 days, for about 15 days to about 20 days, for about 15 days to about 25 days, for about 15 days to about 30 days, when the dispensing device remains open without placing a dust cap on it. Petition 870260061385, dated 06 / 23 / 2026, p. 19 / 67 12 / 54

[0049] In another embodiment, the addition of a decongestant to an aqueous suspension composition controls the obstruction of a nasal spray actuator and / or immersion tube for about 10 days to about 30 days, or for about 10 days to about 25 days when the dispensing device remains open without placing a dust cap on it.

[0050] In one embodiment of any of the pharmaceutical compositions described herein, the composition is an aqueous suspension comprising a hydrocolloid, mometasone, an ester thereof (for example, mometasone furoate), or a salt thereof in particulate form and olopatadine or a salt thereof (for example, olopatadine hydrochloride) in dissolved form, and a decongestant.

[0051] In one embodiment of any of the pharmaceutical compositions described herein, the composition comprises about 0.001% w / w about 0.075% w / w of mometasone, an ester thereof (for example, mometasone furoate) or a salt thereof in particulate form, about 0.5% w / w about 0.8% w / w of olopatadine or its salt (for example, olopatadine hydrochloride) in dissolved form, and about 0.05% w / w about 5% w / w of a decongestant.

[0052] In one embodiment of any of the pharmaceutical compositions described herein, the composition comprises about 0.025% w / w about 0.05% w / w of mometasone, an ester thereof (for example, mometasone furoate) or a salt thereof in particulate form; and about 0.5% w / w about 0.8% w / w of olopatadine or its salt (for example, olopatadine hydrochloride). In this embodiment, the pharmaceutical composition may further comprise a hydrocolloid and about 0.05% w / w about 5% w / w of a decongestant.

[0053] In any of the compositions' modes Petition 870260061385, dated 06 / 23 / 2026, p. 20 / 67 13 / 54 pharmaceutical compositions described in this document comprise approximately 0.025% w / w approximately 0.05% w / w of mometasone, an ester thereof (e.g., mometasone furoate) or a salt thereof in particulate form; and approximately 0.5% w / w approximately 0.8% w / w of olopatadine or its salt (e.g., olopatadine hydrochloride). In this embodiment, the pharmaceutical composition may further comprise a hydrocolloid and approximately 0.1% w / w approximately 5% w / w of a decongestant.

[0054] In one embodiment of any of the pharmaceutical compositions described herein, the composition comprises (a) about 0.025% w / w about 0.05% w / w of mometasone furoate in particulate form, (b) about 0.5% w / w about 0.8% w / w of olopatadine hydrochloride, and (c) about 0.1% w / w about 5% w / w of a decongestant. The pharmaceutical composition may further comprise a hydrocolloid.

[0055] Another embodiment is a pharmaceutical composition suitable for a nasal spray device comprising an actuator and a dip tube through which the composition is delivered, wherein (a) the composition is in the form of an aqueous suspension suitable for nasal administration, and (b) the composition comprises mometasone furoate (for example, in an amount of about 0.025% w / w in particulate form), olopatadine or a pharmaceutically acceptable salt thereof (for example, olopatadine hydrochloride in an amount of about 0.665% w / w in dissolved form), and an amount of a clearing agent sufficient to control obstruction in the actuator and dip tube from which the composition is delivered to facilitate consistent delivery of the composition. The clearing agent may be any of such agents described herein.In one embodiment, the unclogging agent is selected from glycerol, sorbitol, mannitol, propylene glycol, polyethylene glycol, and any combination of any of the foregoing. Petition 870260061385, dated 06 / 23 / 2026, page 21 / 67 14 / 54 In a preferred embodiment, the unblocking agent is glycerol. In one embodiment, the glycerol is present in an amount of about 0.05% w / w to about 5% w / w. In another embodiment, the glycerol is present in an amount of about 0.05% w / w to about 1% w / w.

[0056] Yet another embodiment is a method of delivering a pharmaceutical composition comprising mometasone furoate and olopatadine hydrochloride to a patient in need thereof via an actuator and immersion tube of a nasal spray device while reducing obstruction of the actuator or immersion tube, wherein the method comprises internally administering the pharmaceutical composition via the actuator and immersion tube of the nasal spray device to the patient, wherein the pharmaceutical composition is in the form of an aqueous suspension suitable for nasal administration, and (b) the composition comprises mometasone furoate (for example, in an amount of about 0.025% w / w in particulate form), olopatadine or a pharmaceutically acceptable salt thereof (for example, olopatadine hydrochloride in an amount of about 0.665% w / w in dissolved form),and a means to control obstruction in the actuator and immersion tube from which the composition is delivered to facilitate consistent delivery of the composition. In one embodiment, the patient suffers from allergic rhinitis, such as seasonal allergic rhinitis or perennial allergic rhinitis. In one embodiment, the unblocking agent is selected from glycerol, sorbitol, mannitol, propylene glycol, polyethylene glycol, and any combination of any of the aforementioned. In a preferred embodiment, the unblocking agent is glycerol. In one embodiment, the glycerol is present in an amount of about 0.05% w / w to about 5% w / w. In another embodiment, the glycerol is present in an amount of about 0.05% w / w to about 1% w / w.

[0057] In yet another embodiment, the nasal spray device or dispensing device may include a container, a cap, and a dispenser head which may include a pump, a tube, Petition 870260061385, dated 06 / 23 / 2026, page 22 / 6715 / 54 immersion, an actuator, a dispensing channel, and a dispensing orifice as shown in Figure 1. The pump is designed to dispense the pharmaceutical composition through the immersion tube into the pump via the actuator fitted with the dispensing orifice. The pharmaceutical composition is released in the form of a uniform spray. The pump can operate in tandem with the actuator, which allows for easy opening and closing of the pump and provides a desired spray characteristic. Actuators include, but are not limited to, spray actuators, foam actuators, solid current actuators, and special actuators. The container of the nasal spray device can be rounded or oval; preferably, the container is rounded. The container may have a conical or flat inner bottom. A cap may or may not be included.The dispensing device delivers a nasal spray in a uniform dose of, for example, mometasone (e.g., as mometasone furoate) and olopatadine (e.g., as olopatadine hydrochloride), wherein the dose is dispensed each time the dispensing device is activated by a user.

[0058] As further detailed below, in certain embodiments, the dispensing device is suitable for dispensing about 100 pl of a pharmaceutical composition per actuation, wherein a single actuation dispenses about 665 μg of olopatadine hydrochloride and about 25 μg or about 50 μg of mometasone furoate, preferably 25 μg of mometasone furoate. Definitions

[0059] The singular forms “a”, “an”, “the” and “the” encompass plural references, unless the context clearly dictates otherwise. Therefore, for example, reference to a compound refers to one or more compounds or at least one compound. In this way, the terms “a”, “one or more”, and “at least one” can be used interchangeably in this document. Petition 870260061385, dated 06 / 23 / 2026, p. 23 / 67 16 / 54

[0060] As used in this document, the term “about”, when referring to a number or a numerical range, means that the number or numerical range mentioned is an approximation within the experimental variability (or within the statistical experimental error), and the number or numerical range may vary from, for example, between 1% and 15% of the number or numerical range mentioned.

[0061] The term “effective amount” when used in connection with an active ingredient denotes an amount of the active ingredient that, when administered to an individual to treat rhinitis, produces an intended therapeutic benefit in that individual.

[0062] The term “active ingredient” (used interchangeably with “active” or “active substance” or “drug”) as used herein includes mometasone (or its ester, such as mometasone furoate) or its salt and olopatadine or its salt (such as olopatadine hydrochloride). The effective amount of mometasone (or its ester, such as mometasone furoate) or its salt may range from about 0.01 mg to about 10 mg, preferably from about 0.02 mg to about 5 mg, or more preferably from about 0.02 mg to about 3 mg. The effective amount of olopatadine or its salt (as olopatadine hydrochloride) may vary from about 0.05 mg to about 20 mg, preferably from about 0.1 mg to about 15 mg, or more preferably from about 0.1 mg to about 10 mg.

[0063] As used in this document, the term “αhydroxy olopatadine” of olopatadine refers to “(Z)-2-{11-[3(Dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-yl}-2-hydroxyacetic acid”.

[0064] As used in this document, the term “EIsomer of Olopatadine” refers to “11-[(E)-3(Dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid”.

[0065] As used in this document, the term Petition 870260061385, dated 06 / 23 / 2026, page 24 / 67 17 / 54 “Isomer of (z) carbaldehyde of olopatadine” refers to “(Z)-11-(3(dimethylamino)propylidene)-6,11-dihydrodibenzo[b,e]oxepine-2-carbaldehyde, hydrochloride”.

[0066] As used in this document, the term “Olopatadine-related Compound B” refers to “(Z)-3-{2(carboxymethyl)dibenzo[b,e]oxepin-11(6H)-ylidene}-N,N-dimethylpropan-1amine oxide”.

[0067] As used in this document, the term “8-DM” of mometasone refers to “(9β, 11 β-epoxy-17α, 21-dihydroxy-16α-methyl pregna-1,4-dience-3,20-dione)”.

[0068] As used in this document, the term “DMC” for mometasone refers to “(21-chloro-9β, 11β-epoxy, 17α,-hydroxyl-16α-methyl pregna-1,4-diene-3,20-dione)”.

[0069] As used herein, the term “DMCF” of mometasone refers to “(21-chloro-9β,11β-epoxy-16α-methyl-3,20-dioxo pregna-1,4-dien-17ylfuran-2-carboxylate)”.

[0070] In one aspect of this invention, for daily administration via the nasal route, the effective amount of mometasone (or its ester, such as mometasone furoate) or its salt may vary from about 10 μg to about 500 μg, preferably from about 20 μg to about 400 μg, and the effective amount of olopatadine or its salt (such as olopatadine hydrochloride) may vary from about 50 μg to about 7,000 μg, preferably from about 100 μg to about 5,400 μg.

[0071] By “salt” or “pharmaceutically acceptable salt” are meant those salts which are, within the scope of reasonable medical judgment, suitable for use in contact with the tissues of humans and lower animals without undue toxicity, irritation and allergic response, proportionate to a reasonable benefit-to-risk ratio, and effective for their intended use. Representative acid addition salts include, for example, hydrochloride, hydrobromide, sulfate, bisulfate, acetate, oxalate salts, Petition 870260061385, dated 06 / 23 / 2026, page 25 / 67 18 / 54 valerate, oleate, palmitate, stearate, laurate, borate, benzoate, lactate, phosphate, tosylate, mesylate, citrate, maleate, fumarate, succinate, tartrate, ascorbate, glucoheptonate, lactobionate, and lauryl sulfate. Representative alkaline or alkaline earth metal salts include, for example, sodium, calcium, potassium, and magnesium salts.

[0072] As used in this document, the terms “treatment” and “treat” refer to an approach to obtain beneficial or desired results including, but not limited to, therapeutic benefit and / or a prophylactic benefit. By therapeutic benefit is meant eradication or improvement of the underlying disorder being treated. Furthermore, a therapeutic benefit is achieved by eradicating or improving one or more of the physiological symptoms associated with the underlying disorder, such that an improvement is observed in the patient, notwithstanding that the patient may still be afflicted by the underlying disorder. For prophylactic benefit, the compositions may be administered to a patient at risk of developing a particular disease, or to a patient who reports one or more of the physiological symptoms of a disease, although a diagnosis of that disease may not have been made.

[0073] By “pharmaceutically acceptable excipient” is meant any component of a pharmaceutical composition other than the active ingredients that is approved by regulatory authorities or is generally considered safe for human or animal use.

[0074] As used in this document, the term “average particle size” (or synonymously, “average particle size”) refers to the particle distribution in which approximately 50 percent by volume of all measured particles are smaller than the defined average particle size value and approximately 50 percent by volume of all measured particles are larger than the defined average particle size value. This can be identified by the term “D50” or “d(0.5)”. The average particle size can Petition 870260061385, dated 06 / 23 / 2026, page 26 / 67 19 / 54 can be measured using various techniques such as microscopy, laser diffraction, photon correlation spectroscopy (PCS) and Coulter's principle.

[0075] As used in this document, the term “D10” refers to the particle distribution in which approximately 10 percent by volume of all measured particles have a size smaller than the defined particle size value. This can also be identified by the term “d(0,1)”. Similarly, as used in this document, the term “D80” refers to the particle distribution in which approximately 80 percent by volume of all measured particles have a size smaller than the defined particle size value. This can also be identified by the term “d(0,8)”. Along similar lines, as used in this document, the term “D90” refers to the particle distribution in which approximately 90 percent by volume of all measured particles have a size smaller than the defined particle size value. This can also be identified by the term “d(0,9)”.

[0076] As used in this document, the term “hydrocolloid” refers to a colloid system in which hydrophilic colloidal particles (e.g., hydrophilic polymers) are dispersed in water. The hydrocolloid system may exist in a gel state or a soluble (liquid) state. In suspension compositions, the hydrocolloid functions as a thickening, stabilizing, and suspending agent. Non-limiting examples of hydrocolloids include cellulose derivatives (such as sodium carboxymethylcellulose), xanthan gum, gum arabic, guar gum, locust bean gum, alginate, starch, agar-agar, carrageenan, gelatin, a mixture of microcrystalline cellulose and sodium carboxymethylcellulose, or any combination of any of the foregoing. Preferably, the hydrocolloid includes xanthan gum or sodium carboxymethylcellulose.

[0077] Hydrocolloids comprising a mixture of microcrystalline cellulose and sodium carboxymethylcellulose may be a water-dispersible, spray-dried colloidal blend of cellulose. Petition 870260061385, dated 06 / 23 / 2026, page 27 / 67 20 / 54 microcrystalline cellulose and sodium carboxymethylcellulose or coprocessed microcrystalline cellulose and sodium carboxymethylcellulose or simple physical mixture of microcrystalline cellulose and sodium carboxymethylcellulose. A mixture of microcrystalline cellulose and sodium carboxymethylcellulose may be Avicel RC591® (available from FMC Biopolymer, Philadelphia, PA) which contains 8.3% w / w and 13.8% w / w of sodium carboxymethylcellulose.

[0078] Some embodiments of the present invention provide compositions comprising sodium carboxymethylcellulose. In some embodiments, the compositions comprise at least about 0.1% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise about 0.1% w / w to about 3% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise about 0.6% w / w to about 2% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise about 0.5% w / w to about 1.5% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise about 0.5% w / w to about 1% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise approximately 0.5% w / w or approximately 0.75% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise approximately 0.67% w / w of sodium carboxymethylcellulose.In some embodiments, the compositions comprise approximately 0.68% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise approximately 0.9% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise 1% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise approximately 0.7% w / w of sodium carboxymethylcellulose. In some embodiments, the compositions comprise 0.6656% w / w of sodium carboxymethylcellulose.

[0079] The term “clearing agent” refers to an agent that controls or prevents or reduces or minimizes obstruction of the actuator and / or Petition 870260061385, dated 06 / 23 / 2026, page 28 / 67 21 / 54 nasal spray immersion tube. Non-limiting examples of decongestant include glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol, and mixtures thereof.

[0080] The term “control obstruction” means to prevent or avoid or reduce or minimize obstruction of the nasal spray actuator and / or immersion tube.

[0081] The term “consistent delivery” refers to a spray in which each spray comprises, for example, about 25 μg of mometasone furoate and about 665 μg of olopatadine hydrochloride with the desired in-vitro parameters, such as spray pattern, spray content uniformity and droplet size distribution.

[0082] The terms “formulation” and “composition” are used interchangeably and refer to a mixture of at least one compound, element or molecule. In some respects, the terms “formulation” and “composition” may be used to refer to a mixture of one or more active agents with one or more pharmaceutically acceptable excipients.

[0083] The pharmaceutical compositions for nasal administration to a human being described in this document may comprise about 0.001% w / w about 0.075% w / w of mometasone, an ester thereof (for example, mometasone furoate), or a salt thereof, about 0.5% w / w about 0.8% w / w of olopatadine or its salt (for example, olopatadine hydrochloride) and a decongestant.

[0084] The pharmaceutical compositions described in this document may be in the form of a solution or a suspension. In a preferred embodiment, the composition is in the form of a suspension (such as a single-phase suspension), wherein mometasone, an ester thereof (e.g., mometasone furoate), or a salt thereof is present in particulate form and olopatadine or its salt (e.g., olopatadine hydrochloride) is present in dissolved form. Petition 870260061385, dated 06 / 23 / 2026, p. 29 / 67 22 / 54

[0085] The compositions described in this document preferably also include a hydrocolloid. In one embodiment, the composition is a suspension and includes a hydrocolloid in an amount of about 0.3% w / w to about 5% w / w to prevent phase separation (i.e., separation of particles and solution) after 3 or 6 months of storage at 25 ± 2 °C and 60% ± 5% relative humidity (RH) or at 40 ± 2 °C and 75% ± 5% RH. In another embodiment, the aqueous pharmaceutical composition is a single-phase suspension that remains a single-phase suspension after 3 or 6 months of storage at 25 ± 2 °C and 60% ± 5% RH or at 40 ± 2 °C and 75% ± 5% RH.

[0086] In another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, wherein the composition comprises about 0.025% w / w about 0.05% w / w of mometasone, an ester thereof (for example, mometasone furoate), or a salt thereof, about 0.6% w / w about 0.7% w / w of olopatadine or its salt (for example, olopatadine hydrochloride), about 0.3% w / w about 3% w / w of hydrocolloid and about 0.05% w / w about 5% w / w of a decongestant.

[0087] In another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, wherein the composition comprises about 0.025% w / w about 0.05% w / w of mometasone, an ester thereof (for example, mometasone furoate), or a salt thereof, about 0.6% w / w about 0.7% w / w of olopatadine or its salt (for example, olopatadine hydrochloride), about 0.3% w / w about 3% w / w of hydrocolloid and about 0.1% w / w about 5% w / w of a decongestant.

[0088] In yet another embodiment, any of the pharmaceutical compositions described in this document is a Petition 870260061385, dated 06 / 23 / 2026, p. 30 / 67 23 / 54 aqueous suspension for nasal administration to a human being, the composition comprising approximately 0.025% w / w approximately 0.05% w / w of mometasone furoate, approximately 0.6% w / w approximately 0.7% w / w of olopatadine hydrochloride, approximately 0.3% w / w approximately 2% w / w of hydrocolloid selected from sodium carboxymethylcellulose and xanthan gum, and approximately 0.05% w / w approximately 5% w / w of a decongestant, such as, for example, glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol and any combination thereof.

[0089] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, wherein the composition comprises about 0.025% w / w about 0.05% w / w of mometasone furoate, about 0.6% w / w about 0.7% w / w of olopatadine hydrochloride, about 0.3% w / w about 2% w / w of hydrocolloid selected from sodium carboxymethylcellulose and xanthan gum, and about 0.1% w / w about 5% w / w of a decongestant, such as, for example, glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol and any combination thereof.

[0090] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, wherein the composition comprises about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrocolloid, at least about 0.3% w / w of hydrochloride selected from sodium carboxymethylcellulose and xanthan gum and about 0.1% w / w to about 3% w / w of a decongestant, such as, for example, glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol and any combination thereof.

[0091] In yet another embodiment, any of the pharmaceutical compositions described in this document is an aqueous suspension for nasal administration to a human being, which Petition 870260061385, dated 06 / 23 / 2026, p. 31 / 67 24 / 54 comprises approximately 0.025% w / w and approximately 0.05% w / w of mometasone furoate, approximately 0.6% w / w and approximately 0.7% w / w of olopatadine hydrochloride, and a decongestant such as, for example, glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol, and any combination thereof. The decongestant may be present at a concentration of at least approximately 0.05% w / w, as well as between approximately 0.1% w / w and approximately 3% w / w of the composition.

[0092] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w about 0.05% w / w of mometasone furoate, about 0.6% w / w about 0.7% w / w of olopatadine hydrochloride and a decongestant such as, for example, glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol and any combination thereof. The decongestant may be present at a concentration of at least about 0.05% w / w or at least about 0.1% w / w of the composition.

[0093] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w about 0.05% w / w of mometasone furoate, about 0.6% w / w about 0.7% w / w of olopatadine hydrochloride and a decongestant such as, for example, glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol and any combination thereof. The unclogging agent may be present at a concentration of approximately 0.05% w / w, approximately 0.1% w / w, approximately 0.2% w / w, approximately 0.3% w / w, approximately 0.4% w / w, approximately 0.5% w / w, approximately 0.6% w / w, approximately 0.8% w / w, approximately 1% w / w, approximately 1.2% w / w, approximately 1.3% w / w, approximately 1.5% w / w, approximately 2% w / w, approximately 2.5% w / w, approximately 3% w / w, approximately 3.5% w / w, approximately 4% w / w, approximately 4.5% w / w, or approximately Petition 870260061385, dated 06 / 23 / 2026, p. 32 / 67 25 / 54 of 5% w / w of the composition.

[0094] In another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w about 0.05% w / w of mometasone furoate, about 0.6% w / w about 0.7% w / w of olopatadine hydrochloride and a decongestant such as, for example, glycerol (or glycerin), sorbitol, mannitol, propylene glycol, polyethylene glycol and any combination thereof. The unclogging agent may be present at a concentration of approximately 0.05% w / w, approximately 1% w / w, approximately 0.1% w / w, approximately 1% w / w, approximately 1% w / w, approximately 1.5% w / w, approximately 1.5% w / w, approximately 2.5% w / w, approximately 2.5% w / w, approximately 3% w / w, approximately 3.5% w / w, approximately 3.5% w / w, approximately 4% w / w, or approximately 4% w / w, approximately 5% w / w of the composition.

[0095] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrochloride and about 0.05% w / w about 5% w / w of a decongestant.

[0096] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrochloride and about 0.1% w / w about 5% w / w of a decongestant.

[0097] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately Petition 870260061385, dated 06 / 23 / 2026, p. 33 / 67 26 / 54 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w of approximately 3% w / w of a decongestant.

[0098] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrochloride and about 0.1% w / w about 1% w / w of a decongestant.

[0099] In yet another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and a decongestant in an amount at a concentration of approximately 0.05% w / w or approximately 0.1% w / w, approximately 0.2% w / w, approximately 0.3% w / w, approximately 0.4% w / w, approximately 0.5% w / w, approximately 0.6% w / w, approximately 0.8% w / w, approximately 1% w / w, approximately 1.2% w / w, approximately 1.3% w / w, approximately 1.5% w / w, approximately 2% w / w, approximately 2.5% w / w, approximately 3% w / w, approximately 3.5% w / w, approximately 4% w / w, approximately 4.5% w / w, or approximately 5% w / w of the composition.

[00100] In another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and a decongestant in an amount at a concentration of approximately 0.05% w / w approximately 1% w / w, approximately 0.1% w / w approximately 1% w / w, approximately 1% w / w, approximately 1.5% w / w, approximately 1.5% w / w, approximately 2.5% w / w, approximately 2.5% w / w, approximately 3% w / w, approximately 3% w / w, approximately 3.5% w / w, approximately 3.5% w / w, approximately 4% w / w or approximately 4% w / w, approximately 5% w / w of the composition.

[00101] In yet another modality, any of Petition 870260061385, dated 06 / 23 / 2026, p. 34 / 67 27 / 54 pharmaceutical compositions described in this document is an aqueous suspension for nasal administration to a human being comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.05% w / w of glycerol.

[00102] In yet another embodiment, any of the pharmaceutical compositions described in this document is an aqueous suspension for nasal administration to a human comprising about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrochloride and about 0.1% w / w about 5% w / w of glycerol.

[00103] In yet another embodiment, any of the pharmaceutical compositions described in this document is an aqueous suspension for nasal administration to a human comprising about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrochloride and about 0.1% w / w about 3% w / w of glycerol.

[00104] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w and approximately 2% w / w of glycerol.

[00105] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.01% to approximately 1% w / w (as approximately 0.1% w / w to approximately 1% w / w) of glycerol.

[00106] In yet another embodiment, the pharmaceutical composition described in this document is an aqueous suspension for Petition 870260061385, dated 06 / 23 / 2026, p. 35 / 67 28 / 54 nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w of glycerol.

[00107] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.05% w / w and approximately 5% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube (for example, for at least about 5 days) through which the pharmaceutical composition is delivered.

[00108] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w of mometasone furoate, about 0.665% w / w of olopatadine hydrochloride and about 0.05% w / w about 5% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube (through which the pharmaceutical composition is delivered) for at least about 10 days, for at least about 15 days, for at least about 20 days, for at least about 25 days, for at least about 30 days.

[00109] In one embodiment, control of nasal spray actuator and / or immersion tube obstruction for up to 30 days is observed even when the dispensing device remains open without a dust cap fitted thereto, or the dust cap is improperly fitted to the dispensing device.

[00110] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of hydrochloride of Petition 870260061385, dated 06 / 23 / 2026, p. 36 / 67 29 / 54 olopatadine and approximately 0.05% w / w approximately 5% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 to 30 days, approximately 5 to 25 days, approximately 5 to 20 days, approximately 5 to 15 days, approximately 5 to 10 days.

[00111] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 5% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately 10 days, for at least approximately 15 days, for at least approximately 20 days, for at least approximately 25 days, for at least approximately 30 days.

[00112] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 5% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 days to approximately 30 days, approximately 5 days to approximately 25 days, approximately 5 days to approximately 20 days, approximately 5 days to approximately 15 days, approximately 5 days to approximately 10 days.

[00113] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w and approximately 3% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately Petition 870260061385, dated 06 / 23 / 2026, p. 37 / 67 30 / 54 days, for at least about 15 days, for at least about 20 days, for at least about 25 days, for at least about 30 days.

[00114] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 3% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 days to approximately 30 days, approximately 5 days to approximately 25 days, approximately 5 days to approximately 20 days, approximately 5 days to approximately 15 days, approximately 5 days to approximately 10 days.

[00115] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 1% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately 10 days, for at least approximately 15 days, for at least approximately 20 days, for at least approximately 25 days, for at least approximately 30 days.

[00116] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 1% w / w of a decongestant that controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 days to approximately 30 days, approximately 5 days to approximately 25 days, approximately 5 days to approximately 20 days, approximately 5 days to approximately 15 days, approximately 5 days to approximately 10 days.

[00117] In another modality, the pharmaceutical composition Petition 870260061385, dated 06 / 23 / 2026, pp. 38 / 67 31 / 54 described in this document is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.05% w / w and approximately 5% w / w of glycerol, which controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately 10 days, for at least approximately 15 days, for at least approximately 20 days, for at least approximately 25 days, for at least approximately 30 days.

[00118] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.05% w / w and approximately 5% w / w of glycerol which controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 days to approximately 30 days, approximately 5 days to approximately 25 days, approximately 5 days to approximately 20 days, approximately 5 days to approximately 15 days, approximately 5 days to approximately 10 days.

[00119] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 5% w / w of glycerol that controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately 10 days, for at least approximately 15 days, for at least approximately 20 days, for at least approximately 25 days, for at least approximately 30 days.

[00120] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of hydrochloride of Petition 870260061385, dated 06 / 23 / 2026, pp. 39 / 67 32 / 54 olopatadine and approximately 0.1% w / w approximately 5% w / w of glycerol that controls the obstruction of an actuator and / or nasal spray immersion tube for approximately 5 days to approximately 30 days, for approximately 5 days to approximately 25 days, for approximately 5 days to approximately 20 days, for approximately 5 days to approximately 15 days, for approximately 5 days to approximately 10 days.

[00121] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 3% w / w of glycerol that controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately 10 days, for at least approximately 15 days, for at least approximately 20 days, for at least approximately 25 days, for at least approximately 30 days.

[00122] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 3% w / w of glycerol which controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 days to approximately 30 days, approximately 5 days to approximately 25 days, approximately 5 days to approximately 20 days, approximately 5 days to approximately 15 days, approximately 5 days to approximately 10 days.

[00123] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w and approximately 1% w / w of glycerol that controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately 10 days, for at least Petition 870260061385, dated 06 / 23 / 2026, p. 40 / 67 33 / 54 approximately 15 days, for at least approximately 20 days, for at least approximately 25 days, for at least approximately 30 days.

[00124] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w approximately 1% w / w of glycerol which controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 days to approximately 30 days, approximately 5 days to approximately 25 days, approximately 5 days to approximately 20 days, approximately 5 days to approximately 15 days, approximately 5 days to approximately 10 days.

[00125] In another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w of glycerol that controls the obstruction of a nasal spray actuator and / or immersion tube for at least approximately 5 days, for at least approximately 10 days, for at least approximately 15 days, for at least approximately 20 days, for at least approximately 25 days, for at least approximately 30 days.

[00126] In yet another embodiment, the pharmaceutical composition described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride and approximately 0.1% w / w of glycerol that controls the obstruction of a nasal spray actuator and / or immersion tube for approximately 5 days to approximately 30 days, approximately 5 days to approximately 25 days, approximately 5 days to approximately 20 days, approximately 5 days to approximately 15 days, approximately 5 days to approximately 10 days.

[00127] In another modality, the unblocking agent can Petition 870260061385, dated 06 / 23 / 2026, p. 41 / 67 34 / 54 to be present at a concentration of approximately 0.05% w / w approximately 1% w / w, approximately 0.1% w / w approximately 2% w / w, approximately 1% w / w approximately 3% w / w, approximately 1.5% w / w approximately 4% w / w, approximately 2.5% w / w approximately 4% w / w, approximately 3% w / w approximately 3.5% w / w, approximately 3.5% w / w approximately 4% w / w or approximately 4% w / w approximately 5% w / w of the composition.

[00128] In another embodiment, the unblocking agent is glycerol (or glycerin) present at a concentration of about 0.05% w / w about 1% w / w, about 0.1% w / w about 2% w / w, about 0.1% w / w about 3% w / w, about 1% w / w about 3% w / w, about 1.5% w / w about 4% w / w, about 2.5% w / w about 4% w / w, about 3% w / w about 3.5% w / w, about 3.5% w / w about 4% w / w, or about 4% w / w about 5% w / w of the composition.

[00129] In another embodiment, the unblocking agent is glycerol (or glycerin) present at a concentration of between about 0.1% w / w and about 5% w / w.

[00130] In another embodiment, the unblocking agent is glycerol (or glycerin) present at a concentration of approximately 0.05% w / w, approximately 0.06% w / w, approximately 0.07% w / w, approximately 0.08% w / w, approximately 0.09% w / w, approximately 0.1% w / w, approximately 0.125% w / w, approximately 0.15% w / w, approximately 0.17% w / w, approximately 0.18% w / w, approximately 0.19% w / w, approximately 0.2% w / w, 0.3% w / w, 0.4% w / w, 0.5% w / w, 0.6% w / w, 0.7% w / w, 0.8% w / w, 0.9% w / w, 1% w / w, 1.2% w / w, 1.3% w / w, 1.4% w / w, 1.5% w / w, 1.6% w / w, 1.8% w / w, 2% w / w, 2.5% w / w or 3% w / w of the composition.

[00131] In another embodiment, the unblocking agent is sorbitol present at a concentration of approximately 0.05% w / w, approximately 0.1% w / w, 0.2% w / w, 0.3% w / w, 0.4% w / w, 0.5% w / w, 0.6% w / w, 0.7% w / w, 0.8% w / w, 0.9% w / w, 1% w / w, 1.2% w / w, 1.3% w / w, 1.4% w / w, 1.5% w / w, 1.6% w / w, 1.8% w / w, 2% w / w, 2.5% w / w or 3% w / w of the composition.

[00132] In another embodiment, the unblocking agent is sorbitol present at a concentration of approximately 0.05% w / w or approximately 1% w / w, Petition 870260061385, dated 06 / 23 / 2026, p. 42 / 67 35 / 54 approximately 0.1% w / w approximately 2% w / w, approximately 0.1% w / w approximately 3% w / w, approximately 1% w / w approximately 3% w / w, approximately 1.5% w / w approximately 4% w / w, approximately 2.5% w / w approximately 4% w / w, approximately 3% w / w approximately 3.5% w / w, approximately 3.5% w / w approximately 4% w / w, or approximately 4% w / w approximately 5% w / w of the composition.

[00133] In another embodiment, the unblocking agent is mannitol present at a concentration of about 0.05% w / w about 1% w / w, about 0.1% w / w about 2% w / w, about 1% w / w about 3% w / w, about 1.5% w / w about 4% w / w, about 2.5% w / w about 4% w / w, about 3% w / w about 3.5% w / w, about 3.5% w / w about 4% w / w or about 4% w / w about 5% w / w of the composition.

[00134] In another embodiment, the unclogging agent is mannitol present at a concentration of approximately 0.05% w / w, approximately 0.1% w / w, 0.2% w / w, 0.3% w / w, 0.4% w / w, 0.5% w / w, 0.6% w / w, 0.7% w / w, 0.8% w / w, 0.9% w / w, 1% w / w, 1.2% w / w, 1.3% w / w, 1.4% w / w, 1.5% w / w, 1.6% w / w, 1.8% w / w, 2% w / w, 2.5% w / w or 3% w / w of the composition.

[00135] In another embodiment, the unblocking agent is propylene glycol present at a concentration of about 0.05% w / w about 1% w / w, about 0.1% w / w about 2% w / w, about 1% w / w about 3% w / w, about 1.5% w / w about 4% w / w, about 2.5% w / w about 4% w / w, about 3% w / w about 3.5% w / w, about 3.5% w / w about 4% w / w or about 4% w / w about 5% w / w of the composition.

[00136] In another embodiment, the unblocking agent is propylene glycol present at a concentration of approximately 0.05% w / w, approximately 0.1% w / w, 0.2% w / w, 0.3% w / w, 0.4% w / w, 0.5% w / w, 0.6% w / w, 0.7% w / w, 0.8% w / w, 0.9% w / w, 1% w / w, 1.2% w / w, 1.3% w / w, 1.4% w / w, 1.5% w / w, 1.6% w / w, 1.8% w / w, 2% w / w, 2.5% w / w or 3% w / w of the composition.

[00137] In another embodiment, the unblocking agent is polyethylene glycol present at a concentration of approximately 0.05% w / w, approximately 1% w / w, approximately 0.1% w / w, approximately 2% w / w, approximately 1% w / w, approximately Petition 870260061385, dated 06 / 23 / 2026, p. 43 / 67 36 / 54 of 3% w / w, approximately 1.5% w / w approximately 4% w / w, approximately 2.5% w / w approximately 4% w / w, approximately 3% w / w approximately 3.5% w / w, approximately 3.5% w / w approximately 4% w / w or approximately 4% w / w approximately 5% w / w of the composition.

[00138] In another embodiment, the unblocking agent is polyethylene glycol present at a concentration of approximately 0.05% w / w, approximately 0.1% w / w, 0.2% w / w, 0.3% w / w, 0.4% w / w, 0.5% w / w, 0.6% w / w, 0.7% w / w, 0.8% w / w, 0.9% w / w, 1% w / w, 1.2% w / w, 1.3% w / w, 1.4% w / w, 1.5% w / w, 1.6% w / w, 1.8% w / w, 2% w / w, 2.5% w / w or 3% w / w of the composition.

[00139] In another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising about 0.025% w / w about 0.05% w / w of mometasone furoate, about 0.6% w / w about 0.7% w / w of olopatadine hydrochloride, about 0.5% w / w about 0.7% w / w of sodium carboxymethylcellulose and about 0.1% w / w of glycerol.

[00140] In another embodiment, any of the pharmaceutical compositions described herein is an aqueous suspension for nasal administration to a human being, comprising approximately 0.025% w / w of mometasone furoate, approximately 0.665% w / w of olopatadine hydrochloride, approximately 0.67% w / w of sodium carboxymethylcellulose and approximately 0.1% w / w of glycerol.

[00141] It will also be observed by those skilled in the art that, in order to enhance the physical properties, appearance and / or smell of the compositions of the present invention, one or more additional pharmaceutically acceptable excipients may be added as desired. Suitable pharmaceutically acceptable excipients include, but are not limited to, chelating agents, preservatives, buffers, surfactants, isotonicity agents, flavor masking agents, antioxidants, humectants, pH adjusting agents and any combination of any of the foregoing.

[00142] Suitable surfactants that can be used for Petition 870260061385, dated 06 / 23 / 2026, pp. 44 / 67 37 / 54 Prepare aqueous nasal spray compositions may include, for example, one or more anionic, cationic, nonionic or zwitterionic surfactants. Examples of suitable surfactants that can be used in aqueous nasal spray suspensions may be selected from, but not limited to, polyethoxylated sorbitan derivatives such as polysorbates, their ethoxylates, produced by reaction of sorbitan esters with ethylene oxide, polyoxyethylene alkyl phenol, polyoxyethylene cetyl ether, polyoxyethylene alkyl-aryl ether, polyoxyethylene monolaurate, polyoxyethylene vegetable oil, polyoxyethylene sorbitan monolaurate, polyoxyethylene esters of mixed fatty acids and resins, polyoxyethylene sorbitol lanolin derivative, polyoxyethylene tridecyl ether, polyoxyethylene sorbitan esters of mixed fatty acids and resins, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan monooleate,Polyoxyethylene sorbitan monostearate, polyoxyethylene stearyl ether, polyoxyethylene oleyl ether, polyoxyethylene tridecyl ether, polyoxyethylene fatty alcohol, polyoxyethylene alkylamine, polyoxyethylene glycol monopalmitate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene cetyl ether, polyoxyethylene oxypropylene stearate, polyoxyethylene lauryl ether, polyoxyethylene lanolin derivative, sodium oleate, quaternary ammonium derivative, potassium oleate, N-cetyl N-ethyl morpholino ethosulfate, sodium lauryl sulfate, or mixtures thereof. Preferred surfactants are polyethoxylated sorbitan derivatives (such as polysorbate 80). The amount of surfactant may vary from about 0.001% to about 1% w / w relative to the total weight of the composition.

[00143] In order to improve the tolerability of aqueous nasal spray suspension when administered to the nasal mucous membrane, it is advantageous to formulate it as isotonic. Osmolarity can be defined by varying the amounts of substances present in the aqueous nasal spray suspension in addition to the active agents, and / or by adding an isotonic agent, preferably a salt. Petition 870260061385, dated 06 / 23 / 2026, pp. 45 / 67 38 / 54 physiologically tolerated, such as sodium chloride or potassium chloride. The amount of isotonic agent may vary from about 0.001% to about 1% w / w relative to the total weight of the composition.

[00144] Examples of suitable preservatives that may be employed in the aqueous nasal spray suspensions described in this document include, but are not limited to, benzyl alcohol, quaternary ammonium halides, phenylcarbinol, thimerosal, and disodium edadate. Quaternary ammonium halide preservatives are preferred. Suitable quaternary ammonium halide preservatives include, for example, polyquaternium-1 halides and benzalkonium halides. Preferred benzalkonium halides include benzalkonium chloride and benzalkonium bromide. The amount of preservative may vary from about 0.005 to about 0.2% w / w relative to the total weight of the composition. Preferably, the preservative is present at a concentration of about 0.02% w / w relative to the total weight of the composition.

[00145] Examples of suitable chelating agents that may be employed in the aqueous nasal spray suspensions described in this document include, but are not limited to, disodium edetate (EDTA), trisodium edetate, tetrasodium edetate, and diethyleneamine pentaacetate, preferably EDTA. The amount of chelating agent present in the aqueous nasal spray suspensions described in this document may vary from about 0.0002% w / w to about 0.5% w / w relative to the total weight of the composition.

[00146] Examples of suitable buffers that may be used in the aqueous nasal spray suspensions described herein include, but are not limited to, citric acid, acetic acid, fumaric acid, hydrochloric acid, malic acid, nitric acid, phosphoric acid, propionic acid, sulfuric acid, tartaric acid, phosphate salts (e.g., dibasic sodium phosphate, such as dibasic sodium phosphate heptahydrate), or combinations thereof. The suspensions of the present Petition 870260061385, dated 06 / 23 / 2026, pp. 46 / 67 39 / 54 The invention may comprise an amount of buffer sufficient to maintain the pH of the composition from about 3 to about 6. Preferably, the amount of buffer ranges from about 0.005% to about 2% w / w relative to the total weight of the composition.

[00147] Examples of suitable sweetening / flavor-masking agents that may be employed in the aqueous nasal spray suspensions described herein include, but are not limited to, sucralose, thaumatin, sucrose, saccharin (including salt forms such as sodium and calcium salts), fructose, glucose, dextrose, corn syrup, aspartame, acesulfame-K, xylitol, sorbitol, erythritol, ammonium glycyrrhizinate, neotamo, mannitol, eucalyptus oil, camphor, and natural or artificial flavoring agents (e.g., menthol, mints, vanilla, orange, etc.), or combinations of two or more such agents. A preferred flavor-masking agent is sucralose. The amount of sweetener / flavor-masking agent present in the aqueous nasal spray suspension may vary from about 0.01% to about 1% w / w relative to the total weight of the composition.

[00148] Examples of suitable antioxidants that may be employed in the aqueous nasal spray suspensions described in this document include, but are not limited to, ascorbic acid, alpha-tocopherol (vitamin E), butylated hydroxyanisole, butylated hydroxytoluene, glutathione, and any combination thereof. The amount of antioxidants present in the aqueous nasal spray composition may vary from about 0.0002% w / w to about 0.5% w / w relative to the total weight of the composition.

[00149] Suitable pH adjusting agents include, but are not limited to, sodium hydroxide and hydrochloric acid.

[00150] An aqueous suspension for nasal administration as described in this document may have a pH between about 3.3 and about 4.1, or between about 3.5 and about 3.9. Petition 870260061385, dated 06 / 23 / 2026, pp. 47 / 67 40 / 54

[00151] The osmolarity of any of the compositions described in this document may vary from about 200 mOsm / kg to about 400 mOsm / kg, or from about 250 mOsm / kg to about 350 mOsm / kg. The viscosity of any of the compositions described in this document may be from about 10 cps to about 200 cps, as from about 20 cps to about 150 cps, or from about 20 cps to about 120 cps. Viscosity may be determined by various known instruments, such as a dynamic stress rheometer or Brookfield viscometer. In a preferred embodiment, viscosity is determined by a Brookfield viscometer measuring torque transmission through a sample using a rotating spindle.

[00152] In yet another aspect, any of the compositions described herein may be in the form of a suspension comprising particles of mometasone, an ester thereof (such as mometasone furoate) or a salt thereof, wherein the particles have an average particle size in the range of about 1 µm to about 20 µm, as well as from about 1 µm to about 15 µm. In one embodiment, the particles of the suspension have an average particle size of less than 15 µm when determined by a microscopy technique.

[00153] In yet another aspect, any of the compositions described in this document, when delivered in a dispensing device, exhibits a spray pattern having a longer geometric axis of about 15-75 mm, a shorter geometric axis of about 10-65 mm, and an ellipticity of about 1-2.

[00154] In yet another embodiment, any of the compositions described in this document is an aqueous suspension for nasal administration to a human being, comprising mometasone furoate monohydrate, olopatadine hydrochloride and a decongestant comprising glycerol (or glycerin) at a concentration of at least about 0.1% w / w of the composition, wherein the composition has Petition 870260061385, dated 06 / 23 / 2026, pp. 48 / 67 41 / 54 a pH between about 3.5 and about 4.1.

[00155] In yet another embodiment, any of the compositions described in this document is an aqueous suspension for nasal administration to a human being, comprising mometasone furoate monohydrate, olopatadine hydrochloride and a decongestant comprising glycerol (or glycerin) at a concentration of at least about 0.1% w / w of the composition.

[00156] In yet another embodiment, any of the compositions described herein is an aqueous suspension for nasal administration to a human being, comprising mometasone furoate monohydrate, olopatadine hydrochloride and a decongestant comprising glycerol (or glycerin) at a concentration between about 0.1% w / w and about 5% w / w of the composition.

[00157] In yet another embodiment, any of the compositions described in this document is an aqueous suspension for nasal administration to a human being, comprising mometasone furoate monohydrate, olopatadine hydrochloride and a decongestant comprising sorbitol at a concentration of at least about 0.1% w / w of the composition.

[00158] In yet another embodiment, any of the compositions described in this document is an aqueous suspension for nasal administration to a human being, comprising mometasone furoate monohydrate, olopatadine hydrochloride and a decongestant comprising polyethylene glycol at a concentration of at least about 0.1% w / w of the composition.

[00159] In yet another embodiment, any of the compositions described in this document additionally comprises: - a chelating agent in an amount of about 0.0002 to about 0.5% w / w; - an isotonic agent of about 0.001% to about 1% w / w; Petition 870260061385, dated 06 / 23 / 2026, pp. 49 / 67 42 / 54 - a surfactant in an amount of about 0.001% to about 1% w / w; - preservative in an amount of approximately 0.005 to approximately 0.2% w / w; and - a buffer in an amount of about 0.005% to about 1% w / w.

[00160] In yet another embodiment, any of the compositions described herein comprises, in addition to olopatadine (e.g., olopatadine hydrochloride) and mometasone furoate, (i) about 0.1% glycerol, (ii) 0.5% w / w sodium carboxymethylcellulose, (iii) about 1.2% w / w of a mixture of microcrystalline cellulose and sodium carboxymethylcellulose, (iv) about 0.02% w / w benzalkonium chloride, (v) about 0.41% w / w sodium chloride, (vi) about 0.01% w / w disodium edetate, (vii) about 0.94% w / w dibasic sodium phosphate, and (viii) about 0.01% polysorbate 80.

[00161] In yet another embodiment, any of the compositions described in this document is an aqueous suspension composition for nasal administration to a human being, wherein the composition comprises (1) about 0.025% w / w mometasone furoate monohydrate, (2) about 0.665% w / w olopatadine hydrochloride, (3) a decongestant selected from about 0.1% w / w glycerol (or glycerin), about 0.1% w / w sorbitol, about 0.1% w / w polyethylene glycol and about 0.1% w / w mannitol, (4) a hydrocolloid selected from about 0.3% w / w xanthan gum and about 0.67% w / w sodium carboxymethylcellulose, (5) about 0.02% w / w of benzalkonium chloride, (6) about 0.4% w / w sodium chloride, (7) about 0.01% w / w disodium edetate, (8) about 0.94% w / w sodium phosphate heptahydrate and (9) about 0.01% w / w polysorbate 80.

[00162] In yet another modality, any of the compositions described in this document is a composition of Petition 870260061385, dated 06 / 23 / 2026, pp. 50 / 67 43 / 54 aqueous suspension for nasal administration to a human being, the composition comprising (1) about 0.025% w / w mometasone furoate monohydrate, (2) about 0.665% w / w olopatadine hydrochloride, (3) a decongestant selected from about 0.1% w / w glycerol (or glycerin), about 0.1% w / w sorbitol, about 0.1% w / w polyethylene glycol and about 0.1% w / w mannitol, (4) a hydrocolloid selected from about 0.3% w / w xanthan gum and about 0.5% w / w sodium carboxymethylcellulose, (5) about 1% w / w about 1.2% w / w of a mixture of microcrystalline cellulose and sodium carboxymethylcellulose, (6) about 0.02% w / w benzalkonium chloride, (7) about 0.41% w / w sodium chloride, (8) about 0.01% w / w disodium edetate, (9) about 0.94% w / w sodium phosphate heptahydrate and (10) about 0.01% polysorbate 80.

[00163] In a further embodiment, the dispensing devices described herein contain any of the pharmaceutical compositions described herein in the form of a kit with a packaging insert containing instructions on the use of the pharmaceutical composition.

[00164] In one embodiment, the composition, when stored for up to 12 months at 25 ± 2 °C and 60 % ± 5 % relative humidity in the dispensing device, has one or more of the following properties: (i) the composition contains no more than 1% of total impurities (after storage); (ii) the composition contains no more than 0.5% DMC (after storage); (iii) the composition contains no more than 0.5% DMCF (after storage); (iv) the composition contains no more than 0.5% of α-hydroxy olopatadine (after storage); (v) the composition contains no more than 0.5% of the E-isomer of Petition 870260061385, dated 06 / 23 / 2026, pp. 51 / 67 44 / 54 olopatadine (after storage); (vi) the composition contains no more than 0.5% of Compound B related to olopatadine (after storage); and / or (vii) the composition contains no more than 0.2% of other olopatadine impurities (after storage). (viii) the composition contains no more than 8-DM (after storage).

[00165] In a further embodiment, the pharmaceutical compositions described herein, when dispensed from a dispensing device described herein, may provide a spray pattern having a longer geometric axis of about 15-75 mm, a shorter geometric axis of about 10-65 mm, and an ellipticity of about 1-2. The spray pattern may be determined by several known techniques, such as with an ADSA with NSPUA configuration (Innova System), and the droplet size distribution of the spray may be determined by several known techniques such as with a Malvern Spraytec with NSPUA configuration (Innova System).

[00166] The following describes a typical procedure for characterizing the droplet size distribution of a spray. The sprayer is loaded with a composition as described in this document and primed by a pump actuated by an actuator until a fine mist appears from the sprayer nozzle. A commercially available laser diffraction instrument is positioned so that the nozzle is approximately 3 cm or approximately 6 cm below the laser beam of the laser diffraction instrument. The pump is actuated with an actuator using a constant force. The resulting spray of the composition crosses the laser beam. Data are collected for D10, D50, D90, and SPAN (D90 - D10 / D50). Average values ​​for each of these parameters for three sprays are calculated.

[00167] In an additional mode, the compositions Petition 870260061385, dated 06 / 23 / 2026, pp. 52 / 67 45 / 54 pharmaceuticals described in this document, when dispensed from the dispensing device, may provide the following droplet size distribution: D10: approximately 5 pm - 3:35 pm, more preferably approximately 10 pm - 30 pm, and most preferably approximately 10 pm - 25 pm at a distance of 3 cm, and approximately 5 pm - 40 pm, more preferably approximately 10 pm - 3:5 pm, and most preferably approximately 10 pm - 30 pm at a distance of 6 cm; D50: approximately 10 pm - 90 pm, more preferably approximately 20 pm - 80 pm, and with maximum preference approximately 25 pm - 75 pm at a distance of 3 cm or 6 cm; D90: approximately 30 pm - 180 pm, more preferably approximately 40 pm - 170 pm, and with maximum preference approximately 50 pm - 160 pm at a distance of 3 cm or 6 cm; SPAN: no more than about 4, more preferably no more than about 3, such as about 2-3;

[00168] where D10 is the droplet size distribution of 10% of the droplets, D50 is the droplet size distribution of 50% of the droplets, D90 is the droplet size distribution of 90% of the droplets; SPAN is the ratio of (D90 - D10) / Dõü. In a further embodiment, the pharmaceutical compositions described herein, when dispensed from the dispensing device, may provide a delivered dose or uniformity of spray content collected at the beginning of the unit's life and the number of measured sprays from each of 10 separate containers, meeting the following acceptance criteria: no more than 2 of the 20 doses are outside the range of about 80% to about 120% of the label indication, and none are outside the range of about 75% to about 125% of the label indication, while the average for each of the initial and final doses is within the range of about 85% to about 115% of the label indication.If 3-6 doses out of the 20 doses collected are outside of approximately 80% to approximately 120% of the target. Petition 870260061385, dated 06 / 23 / 2026, pp. 53 / 67 46 / 54 label indication, but none are outside of approximately 75% to approximately 125% of the label indication, and the means for each of the initial and final doses are within approximately 85% to approximately 115% of the label indication, select 20 additional containers for second-level testing. For second-level testing, the requirements are met if no more than 6 of the 60 doses collected are outside the range of approximately 80% to approximately 120% of the label indication, none are outside the range of approximately 75% to approximately 125% of the label indication, and the means for each of the initial and final doses are within the range of approximately 85% to approximately 115% of the label indication.

[00169] To ensure reproducible in-vitro dose collection, a mechanical means of actuating the pump assembly may be employed to deliver doses for collection. The mechanical actuation procedure must have adequate controls for critical mechanical actuation parameters (e.g., actuation force, actuation speed, stroke length, rest periods, etc.). The test is performed on units that have been prepared according to the patient's instructions for use. The test unit should be actuated in a vertical or near-vertical position, with the valve upwards. The two doses collected at the beginning and end of the container's life should be the dose immediately after preparation and the dose corresponding to the last dose number indicated on the container label.

[00170] The delivered dose or spray content uniformity can be determined by delivering the dose into a suitable container (e.g., scintillation vial) where quantitative transfer from the container under test can be achieved. A validated analytical method is employed to determine the amount of drug in each delivered dose, and data are reported. EXAMPLES Examples 1 and 2 Petition 870260061385, dated 06 / 23 / 2026, pp. 54 / 67 47 / 54 TABLE 1 Serial No. Material Example 1 Example 2 % w / w % w / w 1 Mometasone furoate 0.025 0.025 2 Opatadine hydrochloride 0.665 0.665 3 Mixture of microcrystalline cellulose and sodium carboxymethylcellulose (Avicel RC-591) 1.20 1.20 4 Sodium carboxymethylcellulose 0.50 0.50 5 Glycerin - 0.1 6 Sodium chloride 0.41 0.41 7 Disodium edetate 0.01 0.01 8 Dibasic sodium phosphate 0.940 0.940 9 Polysorbate 80 0.01 0.01 10 Benzalkonium chloride 0.02 0.02 11 Hydrochloric acid qs to adjust pH qs to adjust pH 12 Sodium hydroxide qs to adjust pH qs to adjust pH 13 Water for injection qs to 100 qs to 100

[00171] Manufacturing procedure: For Example 1: 1. A mixture of microcrystalline cellulose and sodium carboxymethylcellulose was added to water for injection, homogenized, and allowed to hydrate. 2. Sodium carboxymethylcellulose was dispersed in water for injection and added to the product from step 1. 3. Dibasic sodium phosphate heptahydrate, sodium chloride, disodium edetate, and olopatadine HCl were dissolved in water. The pH was adjusted to 2.8–3.2 with hydrochloric acid. Petition 870260061385, dated 06 / 23 / 2026, pp. 55 / 67 48 / 54 4. The product from step 3 was added to the product from step 1 with homogenization. 5. Polysorbate 80 was dissolved in water for injection. Mometasone furoate monohydrate was added and stirred to form a fluid paste. 6. The product from step 5 was added to the product from step 4 with homogenization. 7. Benzalkonium chloride was dissolved in water for injection. 8. The product from step 7 was added to the product from step 6 with homogenization. 9. The pH was checked and adjusted to 3.5-3.9 with HCl / NaOH, and the total weight was adjusted with water for injection. The osmolarity of the composition was approximately 250-350 mOsm / kg. The composition was subjected to stability studies under different conditions. For Examples-2: 1. A mixture of microcrystalline cellulose and sodium carboxymethylcellulose was added to water for injection, homogenized, and allowed to hydrate. 2. Sodium carboxymethylcellulose was dispersed in water for injection and added to the product from step 1. 3. Dibasic sodium phosphate heptahydrate, sodium chloride, disodium edetate, and olopatadine HCl were dissolved in water. The pH was adjusted to 2.8–3.2 with hydrochloric acid. 4. The product from step 3 was added to the product from step 1 with homogenization. 5. Polysorbate 80 was dissolved in water for injection. Mometasone furoate monohydrate was added and stirred to form a fluid paste. 6. The product from step 5 was added to the product from step 4 with homogenization. Petition 870260061385, dated 06 / 23 / 2026, pp. 56 / 67 49 / 54 7. Benzalkonium chloride was dissolved in water for injection. 8. The product from step 7 was added to the product from step 6 with homogenization. 9. Glycerol was dissolved in water. 10. The product from step 9 was added to the product from step 3 with homogenization. 11. The pH was checked and adjusted to 3.5-3.9 with HCl / NaOH, and the total weight was adjusted with water for injection. The osmolarity of the composition was approximately 250-350 mOsm / kg. The composition was subjected to stability studies under different conditions.

[00172] The formulation of Examples 1 and 2 was tested for the problem of clogging in a dispensing device. Package size: 240 doses Study duration: 30 days TABLE 2 Formulation details Packaging details (240 MD) Sample details - 8 daily sprays / number of samples With cap Without cap Example 1 30 ml HDPE in bottle + pump + actuator + with and without cap 50 samples 50 samples Example 2 - Batch 1 30 ml HDPE in bottle + pump + actuator + without cap - 50 samples Example 2 - Batch 2 30 ml HDPE in bottle + pump + actuator + without cap - 50 samples Example 2 - Batch 3 30 ml HDPE in bottle + pump + actuator + without cap - 50 samples Petition 870260061385, dated 06 / 23 / 2026, pp. 57 / 67 50 / 54 Formulation details Packaging details (240 MD) Sample details - 8 daily sprays / number of samples With cap Without cap Cap #3 Batches were manufactured using the formulation from example 2.

[00173] Study procedure A) Sample without cap 1. The study began with the bottles in an open condition (i.e., without a cap after spraying) and, as a control, with a cap (a cap was placed on the actuator after spraying). The study continued for 30 days at room temperature. 2. Before the study began, all actuators were primed 6 times. 3. Each bottle was sprayed daily with 8 sprays for 30 days. 4. The spray pattern was visually observed during spraying. 5. Obstruction of each actuator was observed during spraying. 6. If obstruction was observed, the bottle was set aside and the following day, the same procedure was performed to check if the actuator was still obstructed or not. 7. If any obstruction was observed (partial or complete), such bottles were set aside and the observation was recorded. B) Sample with lid: 1. The procedure described above was followed for the study of the capped sample. 2. The cover was placed on the actuator and the instructions below were followed. a) Clean the nozzle of the spray pump with a dry cloth or tissue. Petition 870260061385, dated 06 / 23 / 2026, pp. 58 / 67 51 / 54 clean. b) Hold the spray pump unit and press the dust cap back onto the spray pump nozzle of the bottle. Study of actuator and / or immersion tube obstruction: visual observations and conclusion. TABLE 3 Serial number Sample quantity Batch details Summary of details and observation 1 50 No. Ex 1 - with lid No obstruction observed. 2 50 No. Ex 1 - without lid 11 actuators were obstructed - 8 opened the next day, 3 actuators completely obstructed. 3 50 No. Ex 2 - batch 1 without lid 1 bottle actuator was obstructed, but opened the next day. No additional obstruction observed. 4 50 No. Ex 2 - batch 2 without lid No obstruction observed. 5 50 No. Ex 2 - batch 3 without lid No obstruction observed.

[00174] As can be seen, a formulation containing 0.1% w / w glycerol (or glycerin) controls an actuator against clogging during 30 days of use. 2. Stability data for Example 2: A) 25 °C ± 2 °C and 60% RH ± 5% RH TABLE 4 Test Specifications Initial 1 M 3 M 6 M DESCRIPTION Physical appearance Conformity Conformity Conformity Conformity Test (by HPLC) Petition 870260061385, dated 06 / 23 / 2026, pp. 59 / 67 52 / 54 Test Specifications Initial 1 M 3 M 6 M a) Mometasone furoate 90.0%-110.0% of label indication. 103.3 100.7 101.2 102.8 b) Olopatadine 90.0%-110.0% of label indication. 100.2 99.7 100.8 100.7 Related substances for mometasone furoate by HPLC 8DM impurity Not more than 0.5% ND ND ND ND DMC impurity Not more than 0.5% ND ND ND ND DMCF impurity Not more than 0.5% ND ND ND 0.06 Any other impurity Not more than 0.5% ND ND ND ND Total impurities Not more than 1.0% ND ND ND 0.06 Related substances for olopatadine HCl by HPLC α-hydroxy olopatadine Not more than 0.5% ND ND ND BLOQ (0.005) E-Isomer of olopatadine Not more than 0.5% 0.18 0.14 0.16 0.18 Related Compound B Not more than 0.5% ND 0.01 ND 0.04 (z) Olopatadine carbaldehyde isomer Not more than 0.2% BLOCK 0.03 0.08 0.02 Any other impurity Not more than 0.2% 0.07 0.06 0.09 0.06 Total impurities Not more than 1.0% 0.28 0.32 0.41 0.40 Droplet size distribution by laser diffraction Parameters Distance from tip to laser Distance from tip to laser A) At 3.0 cm distance 3 cm 6 cm 3 cm 6 cm 3 cm 6 cm 3 cm 6 cm 3 cm 6 cm B) At 6.0 cm distance D 10 10-25 pm. 10-30 pm. 14.71 16.12 14.27 16.12 14.14 16.56 13.93 15.58 C) At 3.0 cm distance D 50 25-75 pm. 25-65 pm. 37.63 34.54 35.13 33.22 36.08 33.32 34.26 32.40 % of droplets < 10 pm D 90 65-155 pm 50-145 pm 94.03 73.29 87.21 66.43 90.46 67.61 84.19 63.84 10 units x 3 sprays (n = 30) SPAN NMT 3.0 NMT 3.0 2.11 1.65 2.06 1.51 2.12 1.53 2.05 1.49 Not more than 10.0% 2.60 2.91 3.50 3.55 Petition 870260061385, dated 06 / 23 / 2026, pp. 60 / 67 53 / 54 B) 40 °C ± 2 °C and 75% RH ± 5% RH TABLE 5 Tests Specifications Initial 1M 3M 6M DESCRIPTION Physical appearance Conformity Conformity Conformity Conformity Assay (by HPLC) a) Mometasone furoate 90.0%-110.0% of label indication. 103.3 101.7 100.4 104.8 b) For Olopatadine 90.0%-110.0% of label indication. 100.2 100.1 100.8 100.8 Related substances for mometasone furoate by HPLC 8DM impurity Not more than 0.5% ND ND ND ND DMC impurity Not more than 0.5% ND ND ND ND DMCF impurity Not more than 0.5% ND ND 0.17 0.38 Any other impurity Not more than 0.5% ND ND ND ND Total impurities Not more than 1.0% ND ND 0.17 0.38 Related substances for olopatadine HCl by HPLC α-hydroxy olopatadine Not more than 0.5% ND ND 0.01 0.01 E-isomer of olopatadine Not more than 0.5% 0.18 0.12 0.14 0.17 Related Compound B Not more than 0.5% ND BLOCK 0.01 0.05 (z) Olopatadine carbaldehyde isomer Not more than 0.2% BLOCK 0.04 0.19 0.06 Any other impurity Not more than 0.2% 0.17 0.06 0.08 0.06 Total impurities Not more than 1.0% 0.28 0.31 0.53 0.47 Laser diffraction droplet size distribution Parameters Distance from tip to laser Distance from tip to laser A) At 3.0 cm distance 3 cm 6 cm 3 cm 6 cm 3 cm 6 cm 3 cm 6 cm 3 cm 6 cm B) At 6.0 cm distance D 10 10-25 pm 10-30 pm 14.71 16.12 14.13 16.41 13.45 15.95 13.30 15.80 C) At 3.0 cm distance D 50 25-75 pm 25-65 pm 37.63 34.54 34.61 33.41 33.02 33.33 32.12 32.33 % of droplets < 10 pm D 90 65-155 pm 50-145 pm 94.03 73.29 85.69 66.35 81.79 66.71 78.59 63.73 Petition 870260061385, dated 06 / 23 / 2026, pp. 61 / 67 54 / 54 Test Specifications Initial 1M 3M 6M 10 units x 3 sprays (n = 30) SPAN NMT 3.0 NMT 3.0 2.11 1.65 2.07 1.49 2.07 1.53 2.03 1.48 Not more than 10.0% 2.60 2.92 4.12 4.32 Petition 870260061385, dated 06 / 23 / 2026, pp. 62 / 67

Claims

1 / 4 CLAIMS 1. Pharmaceutical composition, characterized in that it is suitable for a nasal spray device comprising an actuator and a dip tube through which the composition is to be delivered, wherein (a) the composition is in the form of an aqueous suspension suitable for nasal administration, and (b) the composition comprises mometasone furoate in an amount of about 0.025% w / w in particulate form, olopatadine hydrochloride in an amount of about 0.665% w / w in dissolved form, and a decongestant, which is glycerol in an amount of about 0.05% w / w to about 1.5% w / w, wherein the decongestant prevents clogging of the actuator and dip tube for at least 5 days.

2. Pharmaceutical composition, according to claim 1, characterized in that the unblocking agent is present in a sufficient quantity to prevent the actuator and immersion tube from becoming clogged for at least 10 days.

3. Pharmaceutical composition, according to claim 1 or 2, characterized in that the unblocking agent is present in a sufficient quantity to prevent the actuator and immersion tube from becoming clogged for approximately 20 days.

4. Pharmaceutical composition, according to claim 1 or 2, characterized in that the unblocking agent is present in a sufficient quantity to prevent the actuator and immersion tube from becoming clogged for approximately 30 days.

5. Pharmaceutical composition, according to claim 1, characterized in that the amount of the unclogging agent is sufficient to prevent the actuator and the immersion tube from becoming clogged for about 5 days to about 30 days, when the dispensing device remains open without a dust cap.

6. Pharmaceutical composition, according to claim 1, Petition 870260061385, dated 06 / 23 / 2026, page 63 / 67 2 / 4 characterized in that the unclogging agent is present in an amount of approximately 0.1% w / w 1% w / w.

7. Pharmaceutical composition, according to claim 1, characterized in that the unclogging agent is present in an amount of about 0.05% w / w to about 1% w / w.

8. Pharmaceutical composition according to claim 1, characterized in that the unclogging agent is present in an amount of approximately 0.1% w / w.

9. Pharmaceutical composition, according to any one of claims 1 to 8, characterized in that mometasone furoate is present as mometasone furoate monohydrate.

10. Pharmaceutical composition, according to any one of claims 1 to 9, characterized in that the composition further comprises a hydrocolloid in an amount of about 0.3% w / w to about 3% w / w.

11. Pharmaceutical composition, according to claim 10, characterized in that the hydrocolloid is selected from sodium carboxymethylcellulose and xanthan gum.

12. Pharmaceutical composition, according to any one of claims 1 to 11, characterized in that the pharmaceutical composition is free of cyclodextrin.

13. Use of mometasone furoate, olopatadine hydrochloride and a decongestant, characterized in that it is in the manufacture of a medicament for the treatment of a patient suffering from allergic rhinitis, wherein the medicament comprises a pharmaceutical composition suitable for a nasal spray device comprising an actuator and a dip tube through which the composition is to be delivered, wherein (a) the composition is in the form of an aqueous suspension suitable for nasal administration, and Petition 870260061385, dated 23 / 06 / 2026, p. 64 / 67 3 / 4 (b) the composition comprises mometasone furoate in an amount of about 0.025% w / w in particulate form, olopatadine hydrochloride in an amount of about 0.665% w / w in dissolved form, and the unblocking agent which is glycerol in an amount of about 0.05% w / w to about 1.5% w / w, wherein the unblocking agent prevents clogging of the actuator and immersion tube for at least 5 days.

14. Use of mometasone furoate, olopatadine hydrochloride, a hydrocolloid, a chelating agent, an isotonic agent, a surfactant, a preservative, a buffer, and a decongestant which is glycerol, characterized in that it is in the manufacture of a medicament for use in the treatment of a human individual suffering from allergic rhinitis, the medicament comprising a pharmaceutical composition and the treatment comprising administering an effective amount of the pharmaceutical composition intranasally to the human individual via a nasal spray device, wherein the nasal spray device comprises a container, an actuator, a dipping tube, and a dispensing orifice through which the pharmaceutical composition is delivered, wherein: (a) the composition is within the container and is in the form of an aqueous suspension suitable for nasal administration, and (b) the pharmaceutical composition comprises: mometasone furoate in an amount of about 0.0.25% w / w in particulate form, olopatadine hydrochloride in an amount of about 0.665% w / w in dissolved form, and a hydrocolloid in an amount of about 0.3% w / w to about 3% w / w, wherein the hydrocolloid is selected from sodium carboxymethylcellulose and xanthan gum; a chelating agent in an amount of about 0.0002% to about 0.5% w / w; an isotonicity agent of about 0.001% to about 1% w / w; Petition 870260061385, dated 23 / 06 / 2026, p. 65 / 67 4 / 4 a surfactant in an amount of about 0.001% to about 1% w / w; a preservative in an amount of about 0.005% to about 0.2% w / w; a buffer in an amount of about 0.005% to about 1% w / w; and a de-clogging agent which is glycerol in an amount of about 0.05% w / w to about 1.5% w / w, wherein the glycerol substantially prevents the actuator, the immersion tube and the dispensing orifice from becoming clogged for up to about 30 days.when the nasal spray device remains open without a dust cap. Petition 870260061385, dated 06 / 23 / 2026, pp. 66 / 67.

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