Composition and therapy for treatment of gag reflexes

Abstract

To provide a composition for controlling a gag reflex in a patient.SOLUTION: A composition for controlling a gag reflex in a patient, the composition comprising sodium chloride and an acidulant in a 3:1 volume ratio.SELECTED DRAWING: None

Description

[Background technology]

[0001] The pharyngeal reflex (gag reflex), or laryngeal spasm (collectively referred to herein as the "gag reflex"), is a reflex contraction of the back of the throat triggered by touching the palate, the area around the tonsils, the uvula, and the back of the throat. The gag reflex is the end result of a reflex arc, which consists of a series of physiological steps occurring in rapid succession to produce a reflex. Generally, sensory receptors receive environmental stimuli, such as objects reaching the nerves at the back of the throat, which then send a message via afferent nerves to the central nervous system (CNS). The CNS receives this message and sends an appropriate response via efferent nerves to effector cells in the same area as the initial stimulus, which then execute the appropriate physical response (i.e., the gag reflex). The gag reflex is a type of cough, and along with other aerodigestive reflexes, such as reflex pharyngeal swallowing, it prevents objects from entering the mouth from the throat, except during normal swallowing. Therefore, the gag reflex is an important physiological response for preventing choking.

[0002] Gag reflex sensitivity can vary widely. For example, some people lack a gag reflex, while others experience an overactive gag reflex. This sensitivity can be problematic in a variety of situations, including when swallowing medication pills, swallowing large pieces of food, and even when undergoing oral examinations, such as at the dentist. In many cases, an overactive gag reflex results in choking, nausea, and vomiting.

[0003] Various systems and methods currently exist that attempt to reduce the gag reflex. For example, local anesthetics are commonly used to control the gag reflex, where the drug numbs the sensory receptors responsible for initiating the gag reflex. In some instances, this method is undesirable and / or ineffective because it generally numbs the patient's mouth and throat (which can lead to further anxiety in the patient). Other medications, such as tranquilizers, may also be used to relieve anxiety and tension, which can contribute to the gag reflex. However, this solution has limited effectiveness based on the patient's specific needs and may be incompatible with other medications the patient takes. Acupuncture and acupuncture techniques also exist for the treatment of dry vomiting, but these methods are time-consuming and not effective for all patients.

[0004] U.S. Patent No. 4,634,591 (Westerman) provides a method for treating or suppressing dry vomiting or nausea in a patient by sublingually administering a water-soluble tablet containing electrolytes in the same proportions as those present in the patient's bloodstream and / or gastric juices. These electrolytes may include sodium, potassium, calcium, magnesium, chloride, bicarbonate, and phosphate. This method requires placing the tablet under the patient's tongue for 2 to 5 minutes to allow a substantial portion of the tablet to dissolve and be absorbed into the patient's system. If the patient experiences severe dry vomiting, it may be necessary to subsequently administer a second tablet to achieve the desired results. Thus, although Westerman's formulation is reported to suppress and stop the gag reflex, these methods are inefficient, tedious, and may not be suitable for use by children and other patients for whom sublingual administration is difficult.

[0005] Thus, although systems and methods for treating the gag reflex currently exist, challenges remain. The present invention meets and overcomes these challenges. Summary of the Invention

[0006] Any of the features described herein may be combined to deliver a desired structure in accordance with the expressly stated and intended operation of the present invention. The use of the transitional phrases "in some embodiments" and "in some examples" herein is not intended to limit the scope of any embodiment to a particular feature or set of features disclosed thereby. Rather, the intent of all the various embodiments described herein is to provide a contextual framework within which a particular feature or set of features may be understood as a whole in the context of the inventive concept. Thus, the entire present disclosure should be understood as a body of interchangeable and modular elements (to the extent required by those skilled in the art) that can be selected and combined to achieve devices, systems, or methods within the scope of the overall inventive concept disclosed herein.

[0007] In a first aspect of the present invention, a composition for controlling a patient's gag reflex is provided, wherein the composition comprises sodium chloride and an acidulant. In some examples, the composition comprises sodium chloride and an acidulant in a ratio of 1:4. In some examples, the composition is in a powder form. In some examples, the composition is in a form selected from the group consisting of powder, liquid, dissolvable film, and orally disintegrating tablet. In some examples, a composition is provided that comprises citric acid as an acidulant.

[0008] A second aspect of the present invention features a method for controlling a patient's gag reflex, the method comprising: i) preparing a composition of the present invention; and ii) administering the composition to the patient's tongue. In some instances, the method of the present invention further comprises, after administering the composition to the patient's tongue, a step of delaying oral administration. In some instances, the step of delaying oral administration comprises a delay of less than 20 seconds. In some instances, the therapeutic effect of the composition of the present invention lasts for more than 12 hours. DETAILED DESCRIPTION OF THE INVENTION

[0009] The present invention relates to compositions and methods for controlling a patient's gag reflex. In particular, the present invention relates to an oral composition that is applied to a patient's tongue immediately before accessing the patient's oral cavity, particularly in a manner that can trigger the gag reflex. Generally, the compositions of the present invention are fast-acting oral formulations that contain a mixture of sodium chloride and an acidulant. Without wishing to be bound by any particular theory, it is believed that one potential mechanism by which the present invention operates is a combination of i) increased saliva secretion by sodium chloride and ii) stimulation of the swallowing reflex by the acidulant, where these combined physiological responses mask or otherwise suppress the patient's gag reflex.

[0010] The compositions of the present invention comprise sodium chloride. The sodium chloride may be used in any suitable form, including, but not limited to, powder, crystalline, liquid suspension, and slurry. In some embodiments, the compositions of the present invention comprise sodium chloride in the form of table salt.

[0011] The compositions of the present invention further comprise an acidulant. As used herein, the term "acidulant" is intended to describe any compound, ingredient, chemical, or other substance that, when placed on a patient's tongue, imparts a sour or acidic taste to the patient. The acidulant may be used in any suitable form, including, but not limited to, powder, liquid, crystalline, liquid suspension, and slurry. Non-limiting examples of acidulants include citric acid, lemon juice, lemon juice powder, lime juice, lime juice powder, mango powder (amchur), sour plum, sour plum juice, sour plum juice powder, sumac, tamarind, tamarind powder, vinegar, vinegar powder, pickled plum vinegar, pickled plum vinegar powder, verjuice, verjuice powder, and the like. In some embodiments, the compositions comprise a mixture of sodium chloride and two or more acidulants. In some embodiments, the compositions comprise a mixture of sodium chloride and one acidulant.

[0012] In some embodiments, compositions are provided that include a mixture of sodium chloride and an acidulant, wherein the ratio of the two components is selected to provide a therapeutic benefit of suppressing a patient's gag reflex. In some embodiments, compositions are provided that include a mixture of sodium chloride and an acidulant, wherein the ratio of sodium chloride to acidulant is 20:1, 15:1, 10:1, 9:1, 8:1, 7:1, 6:1, 5:1, 4:1, 3:1, 2:1, or 1:1. In some embodiments, compositions are provided that include a mixture of sodium chloride and an acidulant, wherein the ratio of acidulant to sodium chloride is 20:1, 15:1, 10:1, 9:1, 8:1, 7:1, 6:1, 5:1, 4:1, 3:1, 2:1, or 1:1.

[0013] In some embodiments, a composition comprising sodium chloride and citric acid is provided.

[0014] In some embodiments, sodium chloride is present in the composition in an amount of about 90 parts by volume, about 80 parts by volume, about 70 parts by volume, about 60 parts by volume, about 50 parts by volume, or less than 50 parts by volume, based on 100 parts by volume of the composition. In some embodiments, sodium chloride is present in the composition in an amount of about 80 parts by volume, based on 100 parts by volume of the composition.

[0015] In some embodiments, citric acid is present in the composition in an amount of about 5 parts by volume, about 10 parts by volume, about 15 parts by volume, about 20 parts by volume, about 25 parts by volume, about 30 parts by volume, about 35 parts by volume, about 40 parts by volume, about 45 parts by volume, about 50 parts by volume, or more than 50 parts by volume, based on 100 parts by volume of the composition. In some embodiments, citric acid is present in the composition in an amount of about 20 parts by volume, based on 100 parts by volume of the composition.

[0016] In some embodiments, the sodium chloride is present in the composition in an amount of about 80 parts by volume, based on 100 parts by volume of the composition, and the citric acid is present in the composition in an amount of about 20 parts by volume, based on 100 parts by volume of the composition.

[0017] In some embodiments, the composition comprises about 15%, about 20%, about 25%, about 30%, about 35%, about 40%, about 45%, about 50%, or more than 50% by weight of sodium chloride relative to the total weight of the composition, hi some embodiments, the composition comprises about 38% by weight of sodium chloride relative to the total weight of the composition.

[0018] In some embodiments, the composition comprises about 90%, about 80%, about 75%, about 70%, about 65%, about 60%, about 55%, about 50%, or less than 50% by weight of citric acid, based on the total weight of the composition. In some embodiments, the composition comprises about 62% by weight of citric acid, based on the total weight of the composition.

[0019] In some embodiments, the composition comprises about 38% by weight of sodium chloride, based on the total weight of the composition, and about 62% by weight of citric acid, based on the total weight of the composition.

[0020] In some embodiments, a composition is provided that includes a dry powder form. In some embodiments, the composition is a dry powder form of a mixture of sodium chloride and an acidulant in one or more ratios disclosed herein. In some examples, the composition is a dry powder form of a mixture of sodium chloride and citric acid.

[0021] In some embodiments, a dry powder composition is provided by mixing specific volumes and / or weights of sodium chloride and an acidulant to achieve the desired ratio of ingredients in the final composition. The blending may be accomplished mechanically or manually. In some embodiments, one or more of the components of the composition are pre-processed to achieve a desired physical state of the component prior to blending the component into the final composition. For example, in some embodiments, it may be desirable to pre-process one or more of the components by, for example, milling, grinding, and / or filtering through a sieve to achieve a desired granule size. In some embodiments, one or more processing steps may be required to produce a powder form of the acidulant, such as dehydrating or freeze-drying a liquid form of the acidulant. As discussed below, some embodiments of the present invention further include additives or other excipients.

[0022] In some embodiments, a composition is provided that includes a rapidly dissolving film or oral drug strip on a patient's tongue. In some examples, the dissolving film is a polymer that includes sodium chloride and an acidulant, such as citric acid. In some examples, the dissolving film further includes one or more excipients selected from the group consisting of a strip-forming polymer, a plasticizer, a sweetener, a saliva stimulating agent, a flavoring agent, a coloring agent, a stabilizer, a thickener, and other suitable excipients, and the excipient is suitable for use in an oral pharmaceutical dosage form.

[0023] In some embodiments, a composition is provided comprising an orally disintegrating tablet configured to rapidly dissolve on a patient's tongue. In some embodiments, the orally disintegrating tablet of the present invention is a loose compression tablet comprising sodium chloride and an acidulant, such as citric acid. In some embodiments, the orally disintegrating tablet of the present invention is provided in a single-dose dosage form in a sealed blister pack to protect the tablet from damage, moisture, and oxidation.

[0024] In some embodiments, a composition is provided that comprises an oral spray, the spray comprising sodium chloride and an acidulant, such as citric acid, in liquid form, the oral spray configured for application to the patient's tongue.

[0025] In some embodiments, a composition is provided that includes an oral paste or ointment comprising sodium chloride and an acidulant, such as citric acid, the oral paste or ointment being configured for application to the patient's tongue.

[0026] In some embodiments, a composition is provided that includes a mouthwash containing sodium chloride and an acidulant, such as citric acid, configured to be passively held in a patient's mouth for an effective treatment period or applied to the patient's tongue by swish in the patient's mouth. In some embodiments, the effective treatment period is less than 1 second, approximately 1 second, approximately 2 seconds, approximately 3 seconds, approximately 4 seconds, approximately 5 seconds, approximately 6 seconds, approximately 7 seconds, approximately 8 seconds, approximately 9 seconds, approximately 10 seconds, more than 10 seconds, or less than 20 seconds. In some embodiments, an effective volume of the mouthwash of the present invention is 1 ml, approximately 1 ml, approximately 2 ml, approximately 3 ml, approximately 4 ml, approximately 5 ml, approximately 6 ml, approximately 7 ml, approximately 8 ml, approximately 9 ml, approximately 10 ml to 20 ml, approximately 10 ml to 30 ml, approximately 15 ml to 25 ml, or approximately 15 ml to 20 ml. In some instances, the patient may swallow the mouthwash after treatment. In some instances, the patient is instructed to expectorate the mouthwash after treatment.

[0027] In some embodiments, a method for preventing or suppressing the gag reflex is provided, comprising applying a composition of the present invention to a patient's tongue immediately before accessing the patient's oral cavity. In embodiments in which the composition is provided in powder form, the composition may be applied to the patient's tongue by wetting an applicator and then contacting it with the powder composition, wherein the wetting of the applicator results in a therapeutic amount of the powder composition adhering to the wetted applicator. The wetted applicator and the adhering powder composition are then applied to the patient's tongue. In some embodiments, the applicator comprises at least one of a tongue depressor, a cotton swab, a gloved finger, or a patient's ungloved finger. In some embodiments, a metered portion of the powder composition is applied directly to the patient's tongue.

[0028] In embodiments in which the composition is provided in paste, ointment, or gel form, the composition is applied directly to the patient's tongue using a suitable applicator. In embodiments in which the composition is provided in liquid form, a metered dose of the composition may be sprayed directly onto the patient's tongue. In embodiments in which the composition is provided in a dissolving film form or an orally disintegrating tablet form, these dosage forms are prepared with a therapeutically effective amount of the composition, where these dosage forms are applied directly to the patient's tongue.

[0029] The therapeutically effective dose of the composition may vary depending on the patient's needs and / or the selected dosage form. In some embodiments, a therapeutically effective dose of the composition of the present invention comprises less than 0.5 g of sodium chloride and less than 0.12 g of citric acid in a volume of 0.125 teaspoons, or 0.616 ml, less than 0.25 g of sodium chloride and less than 0.06 g of citric acid in a volume of 0.0625 teaspoons, or 0.308 ml, less than 0.125 g of sodium chloride and less than 0.003 g of citric acid in a volume of 0.03125 teaspoons, or 0.154 ml, or less than 0.0625 g of sodium chloride and less than 0.0015 g of citric acid in a volume of 0.015625 teaspoons, or 0.077 ml.

[0030] In some embodiments, the methods of the present invention include a delay between application or administration of the composition to the patient's tongue and access to the patient's oral cavity. In some instances, the delay is less than 10 seconds, less than 8 seconds, less than 5 seconds, less than 3 seconds, or less than 1 second. In some embodiments, the therapeutic effect of the composition lasts for more than 30 minutes, more than 1 hour, more than 2 hours, more than 4 hours, more than 8 hours, more than 12 hours, more than 16 hours, more than 20 hours, or more than 24 hours. [Example]

[0031] Anti-Gag Composition The anti-gag composition was prepared by mixing the dry ingredients of sodium chloride and enoic acid in a ratio of 1: 4. Single doses of the anti-gag composition were prepared and sealed in individual single-use packages.

[0032] Anti-pharyngeal reflex treatment A patient with acute pharyngeal hypersensitivity was treated with the anti-gag reflex composition of the present invention before undergoing an oral examination as part of dental treatment. A tongue depressor was wetted and contacted with the anti-gag reflex composition, thereby adhering a therapeutically effective dose of the anti-gag reflex composition to the wetted tongue depressor. The tongue depressor and the therapeutically effective dose of the anti-gag reflex composition were then applied to the upper surface of the patient's tongue, whereupon the anti-gag reflex composition dissolved on the patient's tongue. An oral examination of the patient began within less than 30 seconds of administering the anti-gag reflex composition. The patient was able to undergo an oral examination and complete dental treatment without exhibiting a gag reflex.

[0033] Those skilled in the art will understand that various features and elements of various embodiments of the present invention can be modified and / or combined within the spirit of the present invention to provide a composition for preventing or suppressing a patient's gag reflex. For example, the active agents of the present invention may include and / or be substituted with any suitable analog or pharmaceutically acceptable salt thereof, including any stereoisomer, including enantiomeric and diastereomeric forms, all of which are contemplated within the scope of the present disclosure. Individual stereoisomers of the compounds of the present disclosure may, for example, be essentially free of other isomers or may be mixed, as applicable, as a racemate or with all other or selected stereoisomers. Specific component ratios may be adjusted as disclosed herein and as desired to meet the specific needs of a patient. The inclusion and / or exclusion of various additives is also contemplated within the scope of the present disclosure.

[0034] The present invention may be embodied in other specific forms without departing from its structure, method, or other essential characteristics as broadly described herein and as hereinafter claimed. The described embodiments are, therefore, to be considered in all respects only as illustrative and not restrictive. The scope of the invention is, therefore, indicated by the appended claims, rather than by the foregoing description. All changes that come within the meaning and range of equivalency of the claims are to be embraced within their scope.

Claims

1. 1. A composition for controlling the gag reflex in a patient, the composition comprising: sodium chloride, and Acidulant A composition comprising:

2. 10. The composition of claim 1, wherein the composition comprises sodium chloride and an acidulant in a ratio of 1:

4.

3. The composition of claim 1 , comprising a powder form.

4. The composition of claim 1 , comprising a liquid form.

5. The composition of claim 1 comprising a dissolvable film.

6. The composition of claim 1 comprising an orally disintegrating tablet.

7. The composition of claim 1 , wherein the acidulant is citric acid.

8. 1. A method of controlling the gag reflex in a patient, the method comprising: To prepare the composition according to the invention, and administering the composition to the tongue of the patient. A method comprising:

9. 10. The method of claim 8, further comprising delaying processing of the oral cavity after said step of administering the composition to the patient's tongue.

10. 10. The method of claim 9, wherein the step of delaying intraoral treatment comprises a delay of less than 20 seconds.

11. 9. The method of claim 8, wherein the therapeutic effect of the composition lasts for more than 12 hours.