34 results about "Treprostinil" patented technology

Compositions and methods for treating chronic obstructive pulmonary disease, interstitial lung disease, asthma, bronchitis, pneumonia, cystic fibrosis, pulmonary edema, sarcoidosis, idiopathic pulmonary fibrosis, pulmonary arterial hypertension, acute respiratory distress syndrome, and respiratory syncytial virus in a patient are presented. Embodiments of the composition include a combination of diethylcarbamazine (DEC) and a prostacyclin analogue, such as Beraprost, Beraprost sodium, Iloprost, Treprostinil, Treprostinil Palmitil, and Cicaprost. Other embodiments include fluvoxamine and / or a phosphodiesterase (PDE) inhibitor. Some embodiments of the composition are in the form of an aerosol, include a propellent, or are in an inhalation delivery device.

The present disclosure provides aerosol properties of a powder composition applied by a dry powder inhaler and a spray drying method. Also provided is a method for treating pulmonary hypertension (PH) in a patient comprising administering an effective amount of the powder composition once a day to the lung of the patient by inhalation with the dry powder inhaler. Further provided is a system for treating PH using the powder composition and the dry powder inhaler.

The objective is to provide methods for treating interstitial lung disease, mitigating lung function decline in individuals with interstitial lung disease (ILD), and increasing forced vital capacity (FVC) in individuals suffering from ILD. [Solution] A method for treating pulmonary hypertension caused by a condition selected from chronic lung disease, hypoxia, and combinations thereof, comprising administering an effective amount of treprostinil, its prodrug, or a pharmaceutically acceptable salt thereof to a subject with pulmonary hypertension caused by a condition selected from chronic lung disease, hypoxia, and combinations thereof.

The invention relates to a treprostinil monohydrate crystal and a preparation method thereof. The present invention provides novel crystalline forms of treprostinil monohydrate, mixtures comprising the same, and methods of making the same.

Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

Methods of treating of interstitial lung disease, reducing pulmonary function decline in a subject with interstitial lung disease (ILD), and increasing forced vital capacity (FVC) in a subject suffering from ILD are provided, wherein the methods include administration of treprostinil.

This disclosure provides a dry powder composition of treprostol prodrug and a method of treating pulmonary hypertension (e.g., pulmonary arterial hypertension or PH associated with interstitial lung disease) in patients in need using said dry powder composition. The dry powder composition comprises: (a) about 0.5 wt% to about 5 wt% of a compound, its stereoisomers, or a pharmaceutically acceptable salt thereof; (b) about 10 wt% to about 61 wt% of leucine; and the remainder is (c) a sugar selected from the group consisting of trehalose and mannitol. The total of (a), (b), and (c) is 100 wt%, and R1 is tetradecyl, pentadecyl, hexadecyl, heptadecanyl, or octadecyl. The method of treating PH comprises administering an effective amount of the dry powder composition to the lungs of the patient by inhalation via a dry powder inhaler during an administration period.

A dry powder inhalation treatment for pulmonary arterial hypertension includes a dose of dry particles comprising greater than 25 micrograms of treprostinil enclosed in a capsule. The dry particles can include treprostinil, a wetting agent, a hydrophobicity modifying agent, a pH modifying agent and a buffer. A method of treating a patient having pulmonary arterial hypertension includes providing a patient a dry powder inhaler, providing the patient at least one capsule for use in the dry powder inhaler, the capsule including at least 25 micrograms of treprostinil.

Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

To provide treprostinil derivatives that can act as prodrugs of treprostinil.SOLUTION: The present invention discloses a compound of formula (I), or a pharmaceutically acceptable salt thereof or the like (where R1 and R2 are independently hydrogen, alkylcarbonyl, alkoxyalkylcarbonyl or the like, where, both R1 and R2 are not hydrogen, and neither -OR1 nor -OR2 form acetate, benzoate or the like).SELECTED DRAWING: None

Methods of treating of interstitial lung disease, reducing pulmonary function decline in a subject with interstitial lung disease (ILD), and increasing forced vital capacity (FVC) in a subject suffering from ILD are provided, wherein the methods include administration of treprostinil.

Treprostinil or a pharmaceutically acceptable salt or derivative thereof may be used in treating pulmonary hypertension in a subject at risk of developing pulmonary hypertension. The treatment may include administering to the subject a first liquid composition comprising Treprostinil or a pharmaceutically acceptable salt or derivative thereof in a first concentration in aerosolized form for a first treatment period, and administering to said subject a second liquid composition comprising Treprostinil or a pharmaceutically acceptable salt or derivative thereof in a second concentration in aerosolized form for a second treatment period following the first treatment period. The second concentration of the second liquid composition may be higher than the first concentration in the first liquid composition. The liquid compositions are administered using a soft mist inhaler.

The invention relates to the technical field of microneedle patches, in particular to a treprostinil precise injection system based on weekly dose microneedle drug loading and an intelligent regulation and control method. The precise injection system comprises a weekly dose micro-needle drug loading module, a precise injection execution module, an intelligent monitoring module and a portable regulation and control terminal, minimally invasive drug delivery is achieved through a degradable micro-needle, and by combining weekly dose design and intelligent regulation and control, precise injection is achieved. The core pain points that in a traditional subcutaneous pumping mode, equipment is heavy and difficult to carry, a needle head is sharp, many adverse reactions are caused, and patient compliance is poor are perfectly solved; according to the method, medication safety indexes are monitored in real time, administration parameters are dynamically adjusted, the curative effect is guaranteed, and meanwhile the problems of infection, pain, allergy and the like are avoided. According to the invention, the portability of equipment can be obviously improved, the medication pain and adverse reaction risk of patients can be reduced, the treatment compliance can be improved, and the device is suitable for long-term treprostinil treatment of pulmonary arterial hypertension patients, and has outstanding clinical application value.

The present disclosure relates to the treatment of diseases, such as pulmonary hypertension, by inhalation of a combination of iloprost and treprostinil.

The invention discloses treprostinil multivesicular liposome for treating pulmonary arterial hypertension. The multivesicular liposome is prepared from an inner water phase, an oil phase and an outer water phase through a double emulsification method, the treprostinil is dissolved in the inner water phase; the oil phase comprises soybean lecithin, cholesterol, glyceryl trioleate and electronegative lipid; the inner water phase and the outer water phase are body fluid isotonic solutions. The treprostinil multivesicular liposome disclosed by the invention has good stability and high encapsulation efficiency, obviously reduces burst release effect, shows obvious slow release characteristic, is beneficial to prolonging in-vivo drug half-life period, and can realize 48-hour treatment, reduce administration frequency, simplify administration method and improve patient compliance through simple subcutaneous injection. After the treprostinil multivesicular liposome is injected once, the inflammatory reaction of the injection part can be eliminated within 7 days, and the treprostinil multivesicular liposome has good safety.

The present disclosure provides dry powder compositions of treprostinil prodrugs and methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension or PH associated with interstitial lung disease) in patients in need of such treatment. The dry powder compositions include: (a) about 0.5 wt% to about 5 wt% of a compound of Formula (I); and (b) about 10 wt% to about 61 wt% of leucine, and the remainder (c) a sugar selected from the group consisting of trehalose and mannitol. The total of (a), (b), and (c) is 100 wt%, and R 1 is tetradecyl, pentadecyl, hexadecyl, heptadecyl, or octadecyl. A method for treating PH comprises administering an effective amount of the dry powder composition to the lungs of a patient by inhalation via a dry powder inhaler during an administration period. In certain compositions and methods provided herein, R 1 is hexadecyl, for example, linear hexadecyl. [Formula 1] JPEG2023548307000053.jpg40161

The application provides a hydroxyl-substituted treprostinil derivative, a synthesis method and application thereof, and belongs to the technical field of drugs.The compound is a coupling compound containing treprostinil and a nitric oxide donor, and is shown as follows.The hydroxyl-substituted treprostinil derivative is a combination drug of treprostinil and a NO donor, solves defects of weak curative effect of treprostinil, inconvenience of NO administration, and uncontrollable dosage, and improves the effectiveness of the drug and the compliance of patients through synergistic effect of the two, and the drug effectiveness control is also improved.

Provided are novel treprostinil derivatives, including treprostinil prodrugs and treprostinil analogs, as well as methods of making and using these compounds.

The invention belongs to the technical field of pharmaceutical preparations, and discloses a treprostinil soluble microcrystalline patch and a preparation method thereof. Existing treprostinil mainly depends on intravenous injection or subcutaneous injection, the administration mode needs to be operated by professional medical staff, pain is brought to a patient, and the problems of infection risk, inconvenience in long-term administration and the like exist. The invention provides a treprostinil soluble microcrystalline patch and a preparation method thereof. The patch is of a layered structure and comprises a backing layer, a microcrystal array layer, an adhesive layer and a protective layer, and the microcrystal array layer is composed of treprostinil, a biodegradable polymer matrix material and auxiliary materials. The preparation method comprises the following steps: dissolving the components in a solvent to form a microcrystal stock solution, injecting into a mold, curing microcrystals through vacuum drying, and laminating and assembling with each layer of material. The microcrystalline patch disclosed by the invention can penetrate through a skin cuticle painlessly and noninvasively, so that efficient and continuous transdermal administration of treprostinil is realized, and many defects of an existing administration mode of treprostinil are overcome.

Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.

The invention discloses a treprostinil prodrug with a structure as shown in a formula I, wherein n is an integer from 5 to 13. The treprostinil prodrug is modified by side chain fatty acid, so that the physicochemical property of treprostinil is improved, the fat solubility is improved, and the solubility is remarkably reduced. The invention discloses a treprostinil prodrug microcrystal, which is prepared by taking the treprostinil prodrug as a raw material and adopting a film hydration-ultrasonic method under the condition that a stabilizer is not added. The treprostinil prodrug microcrystal is prepared through a prodrug microcrystal delivery technology, the action time of the treprostinil prodrug microcrystal in vivo is remarkably prolonged after intramuscular injection, the administration dosage and the injection frequency are reduced, the effectiveness and the safety are improved, and the effective treatment concentration of 2 weeks can be maintained after single injection.

Provided are novel treprostinil based compounds, methods of treatment using the same, and their methods of making.

The invention discloses a treprostinil microcrystal / temperature-sensitive gel system, which is prepared by the following steps: preparing treprostinil and a stabilizer into treprostinil microcrystals, and combining the treprostinil microcrystals with temperature-sensitive gel to obtain the treprostinil microcrystal / temperature-sensitive gel system, the treprostinil microcrystal is prepared from treprostinil and a stabilizer through a film hydration-ultrasonic method. The temperature-sensitive gel is a blank gel solution prepared from methylcellulose, sodium chloride and an additive; the additive is selected from one of polyethylene glycol 4000, polyvinylpyrrolidone K30, hyaluronic acid and bovine serum albumin. The treprostinil microcrystal / temperature-sensitive gel system can slow down burst release of drug microcrystals, prolong drug action time and improve patient compliance and safety. The treprostinil microcrystal-temperature-sensitive gel system can maintain the effective treatment concentration for 3 days after being injected once, and the treatment effect is achieved by reducing the average pulmonary arterial pressure and improving pulmonary vascular remodeling and right heart remodeling.

Methods of treating of interstitial lung disease, reducing pulmonary function decline in a subject with interstitial lung disease (ILD), and increasing forced vital capacity (FVC) in a subject suffering from ILD are provided, wherein the methods include administration of treprostinil.

A process for manufacturing a Treprostinil-diketopiperazine dry powder for pharmaceutical use by spray drying a suspension without need to dissolve Treprostinil in an alcohol solution prior to processing. In some embodiments, the dry powder is for oral inhalation for pulmonary delivery using a dry powder inhaler.

The present disclosure encompasses combinations of ralinepag with a cGMP-elevating agent or prostanoid such as riociguat, treprostinil, or iloprost for treating PAH. The disclosed combination therapy provides for advantages such as improved efficacy, improved safety, reduced doses and / or frequency of ralinepag and / or riociguat, reduced doses and / or frequency of ralinepag and / or treprostinil, and reduced doses and / or frequency of ralinepag and / or iloprost. In some embodiments, the clinical effectiveness of a reduced dose combination is additive or synergistic compared to that provided by the corresponding ralinepag, riociguat, treprostinil, and / or iloprost monotherapies.

This disclosure provides aerosol properties of powder compositions administered via a dry powder inhaler, and a spray-drying process. Also provided is a method for treating pulmonary hypertension (PH) in a patient, comprising administering an effective amount of the powder composition to the patient's lungs once daily via inhalation using a dry powder inhaler. A system for treating PH is further provided using the powder composition and the dry powder inhaler. This disclosure addresses the need for novel therapeutic options for pulmonary hypertension (PH) (including pulmonary arterial hypertension (PAH) and PH associated with interstitial lung disease), portal pulmonary hypertension (PPH), and pulmonary fibrosis by providing improved powder compositions of treprostinil prodrugs administered via a dry powder inhaler, and methods for administering them to patients in need of treatment.

Disclosed are a new crystal form of treprostinil sodium salt (the structural formula thereof is shown as formula I) and a preparation method therefor. Specifically, disclosed are a five and half hydrates of the treprostinil sodium salt and some dehydrated crystal forms thereof. The new crystal form has better stability and hygroscopicity. As a treprostinil crude drug, the new crystal form can meet the requirements for storage and loading and transportation, is stable in terms of quality and can guarantee the controllable quality of subsequent preparation products.