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Use of fargesin and its derivative in preparation of drugs for treating or preventing pulmonary hypertension

A technology for pulmonary arterial hypertension and octopylin, which is applied in the directions of drug combinations, active ingredients of heterocyclic compounds, cardiovascular system diseases, etc.

Inactive Publication Date: 2015-03-11
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above-mentioned drugs have the following problems in the treatment process: they are mainly aimed at arterial PAH, and the treatment target is single; there is not strong selectivity to the pulmonary artery, which causes serious side effects of systemic hypotension in patients; in addition, there are many adverse reactions and side effects. Decreased quality of life is also a common problem in clinical treatment
[0007] But so far no reports about the use of magnolipin in the treatment of PAH have been found.

Method used

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  • Use of fargesin and its derivative in preparation of drugs for treating or preventing pulmonary hypertension
  • Use of fargesin and its derivative in preparation of drugs for treating or preventing pulmonary hypertension
  • Use of fargesin and its derivative in preparation of drugs for treating or preventing pulmonary hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Make magnolipin slow-release tablet according to the following formula (all used contents are weight percentages)

[0032]

[0033]

[0034] The preparation method is as follows:

[0035] (1) Mix magnolipin, lactose, hydroxypropyl methylcellulose, microcrystalline cellulose, and polyvinylpyrrolidone evenly, and granulate with absolute ethanol;

[0036] (2) Put the wet granules in a drying oven at about 50°C, and control the moisture content to about 2%;

[0037] (3) After the dried granules are sized through a 20-mesh sieve, magnesium stearate is added, mixed evenly, and pressed into tablets according to the specifications.

Embodiment 2

[0039] Make xinyisu tablet according to following formula (contents used are weight percentages)

[0040]

[0041] The preparation method is as follows:

[0042] (1) Pulverize magnoliatrin and lactose respectively, pass through a 100-mesh sieve, and directly pass the starch through a 100-mesh sieve for subsequent use;

[0043] (2) Take an appropriate amount of starch and add an aqueous solution to prepare a starch paste for use as a binder;

[0044] (3) Mix magnoliatin, lactose and the remaining amount of starch, add a binder to make a soft material, and pass through a 20-mesh sieve to granulate;

[0045] (4) Place the wet granules in a drying oven at about 50°C, and control the moisture content to about 2%;

[0046] (5) After the dry granules are sized through a 20-mesh sieve, magnesium stearate is added, mixed evenly, and pressed into tablets according to the specifications.

Embodiment 3

[0048] Make magnolipin dispersible tablet according to the following formula (all contents used are weight percentages)

[0049]

[0050]

[0051] The preparation method is as follows:

[0052] (1) By magnesia, microcrystalline cellulose, sodium carboxymethyl starch, aspartame, cross 80 mesh sieves, for subsequent use;

[0053] (2) Take the full amount of polyvinylpyrrolidone K30, make an aqueous solution with a concentration of 5%, stir until it is completely dissolved, and prepare it as an adhesive;

[0054] (3) Mix magnolipin, microcrystalline cellulose, sodium carboxymethyl starch, and aspartame evenly, make a soft material with a binder, and pass through a 20-mesh sieve to granulate;

[0055] (4) Dry the wet granules at about 60°C, and control the moisture to about 2%

[0056] (5) After the dried granules are sized through a 20-mesh sieve, add talcum powder and magnesium stearate, mix well, and press into tablets according to the specifications.

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Abstract

The invention relates to a novel medical use of fargesin and its derivative and especially relates to a use of fargesin and its derivative in preparation of drugs for treating or preventing pulmonary hypertension. Fargesin, fargesin derivative, fargesin salt or fargesin solvate as a single active component or one of active components is compounded to one or more excipients, the composition is processed to form tablets, capsules, particulates, an oral liquid and an injection by conventional methods, is suitable for whole body administration and is used for preventing or treating idiopathic pulmonary hypertension, left-side cardiac disease-related pulmonary hypertension, pulmonary hypertension caused by lung disease and / or low oxygen, chronic thromboembolic pulmonary hypertension or pulmonary hypertension caused by unknown reasons.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, and relates to a new application of xinyixin, in particular to a new application of xinyixin and its derivatives in the preparation of treatment / prevention of pulmonary hypertension. Background technique [0002] Pulmonary Arterial Hypertension (PAH) is a common clinical and extremely malignant disease involving the pulmonary circulatory system. Its main feature is the progressive increase of pulmonary artery pressure and pulmonary vascular resistance, which can eventually lead to right heart failure and death of patients. In the latest evidence-based clinical practice guidelines for the diagnosis and treatment of pulmonary arterial hypertension issued by the American College of Chest Physicians, PAH is defined as mean pulmonary arterial pressure ≥ 25 mmHg, capillary pressure or left atrial pressure ≤ 15 mmHg. The study found that: the average age of onset of the disease is 36 years old...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/36A61P9/12A61P11/00
CPCA61K31/36
Inventor 李小强曹蔚招明高
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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