47 results about "Treprostinil" patented technology

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.

A process for manufacturing a Treprostinil-diketopiperazone 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.

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 the technical field of health management, and discloses a pulmonary hypertension patient medication guidance system and method based on multi-modal adaptive fusion, and the system comprises a construction module which is used for training a support vector machine regression model through the sample data of each medication mode in each body weight interval, and obtaining a plurality of infusion parameter prediction models; the processing module is used for obtaining a target infusion parameter prediction model according to the medication mode and the weight value of the patient, and inputting the current hemodynamic index into the target infusion parameter prediction model to generate initial infusion parameters of treprostinil of the patient in the medication mode; and the guidance module is used for generating a medication guidance scheme of the patient in the medication mode based on the current cardiac function parameters, the environmental parameters and the genotype correction initial infusion parameters. According to the method, personalized medication guidance is provided for the pulmonary hypertension patients, the risks of adverse reaction or poor medication effect and the like caused by individual differences of the patients are reduced, and then doctors are assisted to make more scientific and reasonable medication decisions for the patients.

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 methods of producing compounds, which are useful in synthesizing prostacyclin derivatives, such as treprostinil.

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.

The invention provides a synthesis method and application of a treprostinil chiral intermediate and a synthesis method of treprostinil, and relates to the technical field of pharmaceutical chemical synthesis. According to the synthesis method of the treprostinil chiral intermediate, provided by the invention, efficient synthesis of a key intermediate is realized by chemical synthesis methods of constructing a cyclopentanaphthalene skeleton through a Dieckmann reaction catalyzed by LiHMDS and the like in combination with a chiral alcohol preparation technology through asymmetric reduction of carbonyl reductase. The method is efficient, low in cost and environmentally friendly, the total yield is larger than or equal to 75%, the chiral purity ee is larger than or equal to 99%, the method is suitable for large-scale production, and core technical support is provided for large-scale patent medicine 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 a dry powder inhalation treatment for pulmonary arterial hypertension, a method of treating a patient suffering from pulmonary arterial hypertension, a dry powder inhalation composition for treatment, and a method of producing particles for delivering a dry powder to the lungs of a patient with pulmonary arterial hypertension.SOLUTION: The dry powder inhalation treatment for pulmonary arterial hypertension includes a dose of dry particles comprising more than 25 micrograms of treprostinil enclosed in a capsule. The dry particles may include treprostinil, a wetting agent, a hydrophobicity modifying agent, a pH modifying agent, and a buffer. A method of treating a patient suffering from pulmonary arterial hypertension comprises the steps of providing the patient with a dry powder inhaler, and providing the patient with at least one capsule for use in the dry powder inhaler, the capsule containing at least 25 micrograms of treprostinil.SELECTED DRAWING: Figure 1

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.

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.

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 invention concerns a soluble insulin preparation comprising NϵB29-hexadecandioyl-γ-Glu-(desB30) human insulin in a concentration from 1800 nmol / ml to 4200 nmol / ml, Zinc ions in a concentration from 4.0 Zn / 6Ins to 7.0 Zn / 6Ins, Niacinamide in a concentration from 110 mM to 220 mM or treprostinil in a concentration from 0.02 μg / ml to 1 μg / ml, Citrate in a concentration from 6 mM to 40 mM, and pH in the range from 7.0 to 8.0. The invention further comprises a method for using the soluble insulin preparation for reducing the blood glucose level in a mammal and a process for preparing the soluble insulin preparations.

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.