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A kind of bosentan pharmaceutical composition

A technology of composition and bosentan, which is applied in the direction of drug combination, pharmaceutical formula, respiratory diseases, etc., can solve the problems of poor dissolution rate of pharmaceutical composition, affecting the bioavailability of preparations, high content of impurities in products, etc., and achieve dissolution rate Good, stable preparation and high product quality

Active Publication Date: 2016-09-07
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Bosentan has poor water solubility, and the dissolution rate of the pharmaceutical composition containing bosentan is not good, and it is not easy to be absorbed after entering the human body, which affects the bioavailability of the preparation, thereby reducing the curative effect
In order to improve the dissolution rate of bosentan preparations, CN102114005 discloses a bosentan capsule and a preparation method thereof, the capsule includes 31.25-125 parts of bosentan, 6-15 parts of solid dispersion, 55-80 parts of filler, 6-13 parts of disintegrant, appropriate amount of binder, 0.4-1.0 part of lubricant, wherein the solid dispersion is selected from polyethylene glycol 6000, polyvinylpyrrolidone or a mixture of polyethylene glycol 6000 and polyvinylpyrrolidone, Although the addition of solid dispersion improves the dissolution rate of bosentan capsules, it is still unsatisfactory and leads to high impurity content in the product, which may easily cause adverse reactions and adverse events in patients

Method used

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  • A kind of bosentan pharmaceutical composition
  • A kind of bosentan pharmaceutical composition
  • A kind of bosentan pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039]

[0040] Preparation:

[0041] a. preparing bosentan with d(0.9) as 80 μm by shearing method;

[0042] b. Mix bosentan, lactose, low-substituted hydroxypropyl cellulose and povidone obtained in step a uniformly to obtain mixed powder;

[0043] c. Add ethanol to the above mixed powder, sieve, and make wet granules;

[0044] d. Dry at 40-50°C until the water content is lower than 5%, and granulate;

[0045] e. Pressed into tablets or packed into capsules.

Embodiment 2

[0047]

[0048] Preparation:

[0049] a. prepare bosentan with d(0.9) as 60 μm by spray drying method;

[0050] b. mixing bosentan, mannitol, sodium starch glycolate and hypromellose obtained in step a uniformly to prepare a mixture;

[0051] c. Add water to the above mixture, sieve, and make wet granules;

[0052] d. Dry at 40-50°C until the water content is lower than 5%, and granulate;

[0053] e. Add magnesium stearate and glyceryl behenate, and mix well;

[0054] f. Pressed into tablets or packed into capsules.

Embodiment 3

[0056]

[0057] Preparation method: prepared according to the method in Example 2.

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Abstract

The invention relates to a pharmaceutical composition of Bosentan, and dissolution rate of the composition is increased, thereby improving stability of the preparation; the invention also relates to the preparation method of the Bosentan pharmaceutical composition, and the preparation method is simple and easy to be operated, and is suitable for industrial production.

Description

technical field [0001] The invention relates to a bosentan pharmaceutical composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Pulmonary hypertension is a group of clinical pathophysiological syndromes caused by various reasons in which the average pulmonary artery pressure measured by right heart catheterization is greater than or equal to 25mmHg in a resting state. Patients are physically and mentally healthy and are major diseases that increase the social medical burden. [0003] Bosentan is a dual endothelin receptor antagonist with affinity for ETA and ETB receptors, which can reduce pulmonary and systemic vascular resistance, thereby increasing cardiac output without increasing heart rate, clinically used Treatment of pulmonary hypertension in patients with WHO stage III and IV primary pulmonary hypertension or pulmonary hypertension caused by scleroderma. Its chemical name is N-[6-(2-hydro...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61P9/12A61P11/00
Inventor 黄玉锋彭小玲宋金红王帅杨西邈徐艳华
Owner BEIJING WINSUNNY PHARMA CO LTD
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