19 results about "Prostacyclin" patented technology

The invention discloses a combined evaluation method for in-vitro and in-vivo red fading and relieving effects of cosmetic raw materials, which comprises the following steps: in-vitro model evaluation: inducing a human immortalized umbilical vein endothelial cell model by adopting TNF-alpha, and detecting the secretion amount of a prostacyclin I2 factor to obtain a score of an in-vitro model; in-vivo model evaluation: adopting a chick embryo chorioallantoic membrane model, and obtaining a score of the in-vivo model according to the degree of vasoconstriction caused by the to-be-detected raw material sample acting on the chick embryo chorioallantoic membrane; and comprehensive evaluation: based on the score of the in-vitro model and the score of the in-vivo model, comprehensively evaluating the red fading and relieving efficacy of the raw material sample to be tested. According to the technical scheme, the defect that in the prior art, no cosmetic raw material soothing efficacy evaluation method for the vascular reactivity increasing mechanism exists is overcome, efficacy evaluation is more accurate, the method has the advantages of being comprehensive, short in test period, easy to operate, economical and convenient, and an effective reference basis is provided for screening and compounding schemes of red fading and soothing raw materials.

The present invention relates to an injectable pre-formulation comprising:a) at least one of a mono-, di- or tri-acyl lipid and / or a tocopherol;b) optionally at least one phospholipid;c) at least one biocompatible, organic solvent; andd) at least one prostacyclin analogue or a salt thereof;wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. Such compositions may additionally comprise polar co-solvents. Methods of treatment, particularly for management of pulmonary artery hypertension (PAH), severe PAH, Raynaud's disease, ischemia and related conditions are provided, as well as corresponding uses of the compositions. Administration devices comprising the formulations and kits comprising the devices are also provided.

Described herein are crystalline forms of a prostacyclin (IP) receptor agonist compound, as well as pharmaceutical compositions thereof, and methods of use thereof in the treatment of diseases or conditions that would benefit from treatment with a prostacyclin (IP) receptor agonist compound.

The invention discloses blood filtration replacement liquid as well as a preparation method and application thereof. The displacement liquid comprises low molecular weight heparin calcium, prostaglandin E1, prostacyclin, electrolyte with specific concentration, glucose and an interleukin-1 receptor antagonist. The preparation method comprises the following steps: weighing the raw materials according to the proportion, dissolving to a constant volume, removing pyrogen and heat, and carrying out aseptic packaging. During clinical application, replacement liquid and blood are filtered according to the replacement rate of 1: 1-2: 1 according to the condition of a patient, 4-6 hours each time and 2-3 times each week, and related indexes are monitored. Animal tests show that the replacement liquid has good safety under the effective dosage, and has potential influence on part of organs under the high dosage. A stability test shows that the compound can be stably stored under a certain condition. The invention provides the replacement liquid which can achieve anticoagulation and blood vessel protection, maintain electrolyte balance and relieve inflammatory response, is expected to improve the prognosis of hemodialysis patients, and has important clinical significance and wide application prospects.

A treprostol derivative and its uses are provided. Specifically, a compound of formula (I) or a pharmaceutically acceptable salt thereof is provided, wherein each group is as defined in the specification. The compound of formula (I) or a pharmaceutically acceptable salt thereof can be used to treat pulmonary hypertension.

Provided herein in some embodiments are pharmaceutical compositions comprising a prostacyclin (PGI2) receptor agonist selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1) and pharmaceutically acceptable salts, solvates, and hydrates thereof, as disclosed herein. In some embodiments the pharmaceutical compositions comprise a compound selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), and pharmaceutically acceptable salts, solvates, and hydrates thereof, in an amount equivalent to a therapeutically effective amount of Compound 1, the composition having a release rate by weight of the compound in an aqueous medium that is one or more of release rates (a), (b) and (c) as disclosed herein. The compositions of the present invention are useful in the treatment of PGI2 related disorders, such as those disclosed herein.

The invention discloses application of scopalactone in treatment of pulmonary arterial hypertension, and relates to the technical field of medicinal chemistry. The scoparone is applied to preparation of the medicine for treating pulmonary arterial hypertension. The medicine comprises scopalactone, a pharmaceutically acceptable carrier, a diluent and an excipient, the medicine further comprises other medicines for treating the pulmonary arterial hypertension, and the other medicines for treating the pulmonary arterial hypertension are selected from a prostacyclin medicine, an endothelin receptor antagonist and a phosphodiesterase-5 inhibitor. The scopalactone is applied to preparation of the medicine for treating pulmonary arterial hypertension, right heart insufficiency caused by hypoxia can be remarkably reversed, and the right heart function is effectively improved by reducing the transverse diameter of the right ventricle and the transverse diameter of the right atrium and improving the indexes such as tricuspid valve ring plane contraction displacement; the average pulmonary arterial pressure and right ventricular systolic pressure can be obviously reduced, and hemodynamic parameters are improved; the area and thickness of a blood vessel wall can be remarkably reduced, the blood vessel structure is improved, and pulmonary arteriole reconstruction is relieved.

The present invention relates to methods for treating systemic sclerosis and frost bite, by administering a pharmaceutical composition by inhalation. The pharmaceutical composition comprises a plurality of liposomes, encapsulating prostacyclin or a prostacyclin analogue. The treatment method of the present invention is convenient for home care and can be delivered for over 5 days to effectively treat systemic sclerosis and frost bite.

The present invention relates to a nebulizer kit, comprising a pharmaceutical composition including a prostaglandin, prostacyclin and the analogue thereof and a nebulizer to deliver a prostaglandin, prostaglandin analogue, prostacyclin or prostacyclin analogue with a higher drug delivery efficiency. Also disclosed are methods for treating a respiratory disease and heart failure, using the nebulizer kit disclosed herein.

Described herein are ralinepag prodrugs, as well as pharmaceutical compositions thereof, and methods of use thereof in the treatment of diseases or conditions that would benefit from treatment with a prostacyclin (IP) receptor agonist compound, such as but not limited to pulmonary hypertension (PH) diseases.

The disclosure relates to methods of reducing the risk of disease progression in a patient with pulmonary arterial hypertension (PAH), comprising administering to a patient in need thereof, an initial triple combination therapy of an endothelin receptor antagonist (ERA), a phosphodiesterase type 5 (PDE-5) inhibitor, and a prostacyclin receptor agonist (IP receptor agonist).

Provided herein in some embodiments are pharmaceutical compositions comprising a prostacyclin (PGI2) receptor agonist selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1) and pharmaceutically acceptable salts, solvates, and hydrates thereof, as disclosed herein. In some embodiments the pharmaceutical compositions comprise a compound selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), and pharmaceutically acceptable salts, solvates, and hydrates thereof, in an amount equivalent to a therapeutically effective amount of Compound 1, the composition having a release rate by weight of the compound in an aqueous medium that is one or more of release rates (a), (b) and (c) as disclosed herein. The compositions of the present invention are useful in the treatment of PGI2 related disorders, such as those disclosed herein.

Provided herein in some embodiments are pharmaceutical compositions comprising a prostacyclin (PGI2) receptor agonist selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1) and pharmaceutically acceptable salts, solvates, and hydrates thereof, as disclosed herein. In some embodiments the pharmaceutical compositions comprise a compound selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy) acetic acid (Compound 1), and pharmaceutically acceptable salts, solvates, and hydrates thereof, in an amount equivalent to a therapeutically effective amount of Compound 1, the composition having a release rate by weight of the compound in an aqueous medium that is one or more of release rates (a), (b) and (c) as disclosed herein. The compositions of the present invention are useful in the treatment of PGI2 related disorders, such as those disclosed herein.

The invention relates to processes for preparing carbaprostacyclin analogues and intermediates prepared from the processes. The invention also relates to cyclopentenone intermediates in racemic or optically active form.

The present invention relates to a nebulizer kit, comprising a pharmaceutical composition including a prostaglandin, prostacyclin and the analogue thereof and a nebulizer to deliver a prostaglandin, prostaglandin analogue, prostacyclin or prostacyclin analogue with a higher drug delivery efficiency. Also disclosed are methods for treating a respiratory disease and heart failure, using the nebulizer kit disclosed herein.

The invention discloses a dexheptane structure prostacyclin-loaded nano transdermal patch and a preparation method, the dexheptane structure prostacyclin-loaded nano transdermal patch comprises 10-30 parts of dexheptane precursor liposome, 10-20 parts of a prostacyclin nano-structure lipid carrier and 50-70 parts of an acrylate pressure-sensitive adhesive, the dexheptane precursor liposome comprises 8-12 parts of dexheptane and 36-54 parts of hydrogenated soya bean lecithin, and the prostacyclin nano-structure lipid carrier comprises a prostacyclin nano-structure lipid carrier and an acrylate pressure-sensitive adhesive. The prostacyclin injection comprises the following components in parts by weight: 36-54 parts of mannitol, 80-240 parts of absolute ethyl alcohol, 150-450 parts of purified water, 0.150-0.200 part of prostacyclin, 80-150 parts of glyceryl monostearate, 20-50 parts of oleic acid, 10-30 parts of soybean lecithin and the balance of purified water, wherein the total amount of the prostacyclin injection, the glyceryl monostearate, the oleic acid, the soybean lecithin and the purified water is 1000 parts. According to the invention, the dextroheptane is used as a functional penetration enhancing component in transdermal drug delivery, the dextroheptane and the prostacyclin are synergistically integrated in the nano-lipid carrier, the transdermal penetration rate and the cumulative penetration amount of the prostacyclin are improved, the treatment effect is improved, and continuous and stable release of the prostacyclin is realized under the combined action of the nano-structure lipid carrier and the patch matrix.

The application discloses a combined evaluation method for the in-vitro and in-vivo redness-reducing soothing effect of a cosmetic raw material, which comprises in-vitro model evaluation, adoption of a human immortalized umbilical vein endothelial cell model induced by TNF-alpha, acquisition of the in-vitro model score by detecting the secretion amount of prostacyclin I2 factor, in-vivo model evaluation, adoption of a chicken embryo chorioallantoic membrane model, acquisition of the in-vivo model score by the degree of blood vessel contraction caused by the action of the sample to be tested on the chicken embryo chorioallantoic membrane, and comprehensive evaluation of the redness-reducing soothing effect of the sample to be tested based on the in-vitro model score and the in-vivo model score. The technical scheme of the application makes up for the defect of the prior art that there is no cosmetic raw material soothing effect evaluation method for the mechanism of increased vascular reactivity, the effect evaluation is more accurate, and the method has the advantages of comprehensiveness, short test cycle, simple operation, economy and convenience, and provides an effective reference for the screening and compounding scheme of redness-reducing soothing raw materials.

Provided herein in some embodiments are pharmaceutical compositions comprising a prostacyclin (PGI2) receptor agonist selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1) and pharmaceutically acceptable salts, solvates, and hydrates thereof, as disclosed herein. In some embodiments the pharmaceutical compositions comprise a compound selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), and pharmaceutically acceptable salts, solvates, and hydrates thereof, in an amount equivalent to a therapeutically effective amount of Compound 1, the composition having a release rate by weight of the compound in an aqueous medium that is one or more of release rates (a), (b) and (c) as disclosed herein. The compositions of the present invention are useful in the treatment of PGI2 related disorders, such as those disclosed herein.

The invention relates to the technical field of function testing of cosmetic raw materials, and particularly discloses a method and a model for evaluating in-vitro red fading and relieving effects of cosmetic raw materials, and the method comprises the following steps: inducing human immortalized umbilical vein vascular endothelial cells by adopting a TNF-alpha inducer to establish a red fading and relieving in-vitro model; the method specifically comprises the following steps: after inoculating and culturing human immortalized umbilical vein vascular endothelial cells, setting a control group, a modeling group, a positive drug group and a sample group, respectively adding special culture mediums into the control group and the modeling group, adding an epoxidase inhibitor into the positive drug group, adding a raw material sample to be detected into the sample group, and pre-treating; then adding a TNF-alpha inducer into each group except the control group, and carrying out induction culture; the prostacyclin I2 factor is adopted as a detection index to evaluate the red fading and relieving effects of the raw material sample to be detected. The method is short in test period, simple to operate, economical and convenient, and provides reliable data for further research of efficacy verification in the cosmetic industry.