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Bosentan solid pharmaceutical composition and preparation method thereof

A composition and technology of bosentan, applied in the field of bosentan pharmaceutical composition and its preparation, can solve problems such as low dissolution rate and difficulty in medication for children

Pending Publication Date: 2022-05-27
苏州海景医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] A dispersible bosentan tablet is disclosed in the patent CN101175484B, which is mainly used to solve the problem of difficult drug use of existing tablets for children, so as to improve the tablet, but the problem of low dissolution rate has not been fundamentally solved

Method used

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  • Bosentan solid pharmaceutical composition and preparation method thereof
  • Bosentan solid pharmaceutical composition and preparation method thereof
  • Bosentan solid pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0056] Using the jet pulverization method, the bosentan raw material is subjected to high-speed shear pulverization by a pulverizer, and then added to an air pulverizer for ultra-fine pulverization to obtain micronized bosentan, and the final particle size is controlled to be 10nm-20nm.

example 2

[0058] Prescribing information is as follows:

[0059]

[0060] The preparation method is as follows:

[0061] 1) Mix the prescribed amount of bosentan with PPVVA64 for 10 to 15 minutes, pass through a 40-mesh sieve for later use;

[0062] 2) Use a hot melt extruder, preheat at 130-160°C, add the mixed powder in step 1) after stabilization, adjust the feeding speed to 50-150 RPM, collect the solid dispersion, pass through an 80-mesh sieve after pulverization, and set aside;

[0063] 3) Lactose, microcrystalline cellulose, sodium saccharin, xanthan gum, sodium citrate and orange essence of recipe quantity are mixed after 10 minutes, add magnesium stearate and mix for 3 minutes to obtain mixed powder;

[0064] 4) dry granulating the mixed powder of step 3), pressure 5~8MPa, feed rotation speed 2RPM, roller rotation speed 1RPM, pass through an 18-mesh sieve after pulverization, and collect the granular powder;

[0065] 5) Mix the solid dispersion of step 2) with the granular...

example 3

[0067] Prescribing information is as follows:

[0068]

[0069]

[0070] The preparation method is as follows:

[0071] 1) Mix the prescribed amount of bosentan with PPVVA64 for 10 to 15 minutes, pass through a 40-mesh sieve for later use;

[0072] 2) Use a hot melt extruder, preheat at 130-160°C, add the mixed powder in step 1) after stabilization, adjust the feeding speed to 50-150 RPM, collect the solid dispersion, pass through an 80-mesh sieve after pulverization, and set aside;

[0073] 3) Mix the lactose, microcrystalline cellulose, sodium saccharin, xanthan gum, sodium dihydrogen phosphate, orange essence and the solid dispersion of step 2) in the recipe amount for 10 to 15 minutes, then add talc and mix for 3 minutes to obtain mixed powder;

[0074] 4) The solid dispersion of step 2) and the mixed powder of step 3) are mixed for 10 to 15 minutes, and then the mixture is obtained.

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Abstract

The invention relates to a bosentan solid pharmaceutical composition and a preparation method thereof, and belongs to the technical field of pharmacy. According to the technical scheme, the bosentan solid pharmaceutical composition comprises a bosentan solid dispersion, a filling agent, a suspending aid, a sweetening agent, buffer salt, a flavoring agent and a lubricating agent, and the bosentan solid dispersion is prepared through a hot melt extrusion method. The invention overcomes the defect of poor use compliance of children in the prior art, and has a good clinical application prospect. The preparation method is simple and convenient, is suitable for industrial production, and has great practical value.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a bosentan pharmaceutical composition and a preparation method thereof. Background technique [0002] Pulmonary arterial hypertension (PAH) is a hemodynamic and pathophysiological state in which pulmonary arterial pressure rises above a certain threshold, leading to right heart failure, and can be an independent disease, a complication, or a Syndrome is a common and frequently-occurring disease with high morbidity and mortality. Pulmonary hypertension is common in congenital heart disease and can occur at any age in childhood. [0003] Bosentan is a dual endothelin receptor antagonist with affinity for both endothelin receptor A (ETA) and endothelin receptor B (ETB). Bosentan reduces pulmonary vascular and systemic vascular resistance and increases cardiac output without increasing heart rate. Bosentan competes with endothelin for binding to ETA and ETB rec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K9/14A61K9/16A61P9/00A61P9/12
CPCA61K31/506A61K9/146A61K9/145A61K9/1652A61P9/12A61P9/00
Inventor 胡建旭谈邹念王一鸣吕世亮张金英孙培培
Owner 苏州海景医药科技有限公司
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