Stable enalapril maleate capsules and preparation method thereof

Abstract

The invention relates to stable enalapril maleate capsules and a preparation method thereof, and belongs to the technical field of medicine. Enalapril maleate, lactose monohydrate, microcrystalline cellulose, startch, hydroxypropyl methyl cellulose, sodium alga acid, poloxamer 407, polyethylene glycol 4000 and L-arginine are preferably used as medical components of the stable enalapril maleate capsules, the degradation speed of the enalapril maleate is remarkably decreased through the mutual synergistic effect, the stability of the enalapril maleate capsules is greatly improved, and it is ensured that clinical medicine is safe, effective and capable of being stored for a long time.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a stable enalapril maleate tablet and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Enalapril maleate, the chemical name is N~[(S)~1~(ethoxycarbonyl)~3~phenylpropyl]~L~alanyl~L~proline maleate , the structural formula is as follows: [0003] [0004] Enalapril maleate is the second angiotensin-converting enzyme inhibitor drug to be marketed after captopril. As a prodrug, it is rapidly hydrolyzed in the liver to an active diacid metabolite after oral administration. Enalaprilat exerts its role as an angiotensin-converting enzyme inhibitor, so that angiotensin Ⅰ cannot be converted into angiotensin Ⅱ, which causes the relaxation of blood vessels throughout the body, and finally achieves the effect of lowering blood pressure, and can effectively treat For congestive heart failure, it has obvious antihypertensive effect o...

AI Technical Summary

Problems solved by technology

[0005] Existing enalapril maleate is mostly tablets, such as Yuedingning produced by China-US Hangzhou Merck Pharmaceutical Co., Ltd. and Yisu produced by Jiangsu Yangzijiang Pharmaceutical Group Co., Ltd., but the following problems exist in the production of tablets: Malay Enalapril acid may undergo hydrolysis reaction due to the structure itself. Although the raw material itself is very stable, it is particularly easy to degrade in the preparation to produce two impurities, enalaprilat and enalapril diketone, indicating that the excipients in the preparation Accelerated the degradation of enalapril

But generally speaking, the effect is not satisfactory, and the problems in the production of enalapril maleate tablets still cannot be solved

According to research data, among the products on the market, the proportion of products with unqualified substances in 1 to 2 years after production can reach 70%, and the proportion of products with unqualified substances in 2 to 3 years after production is as high as nearly 90%, resulting in degradation during the shelf life Therefore, the degradation of enalapril maleate tablets is still a common problem, which restricts the quality of existing enalapril maleate tablets, and cannot guarantee safe clinical use and long-term storage

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