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Enalapril maleate granules and preparation method thereof

A technology of enalapril maleate and granules, which is applied in the field of medicine and can solve problems such as difficult preparation of stable preparations

Inactive Publication Date: 2015-04-01
万全万特制药(厦门)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] US Patent US 4374829 reports that enalapril maleate is easily decomposed by most excipients, making it difficult to prepare stable preparations

Method used

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  • Enalapril maleate granules and preparation method thereof
  • Enalapril maleate granules and preparation method thereof
  • Enalapril maleate granules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Preparation of Enalapril Maleate Granules (2.5mg)

[0027]

[0028] Preparation Process:

[0029] (1) Add the enalapril maleate raw material into the saturated aqueous solution of β-cyclodextrin, stir and mix for 30 minutes, filter, dry at 50°C, and control the water content to 2%;

[0030] (2) Pulverize the β-cyclodextrin inclusion compound of enalapril maleate and pass through a 80-mesh sieve;

[0031] (3) The pulverized cyclodextrin inclusion complex of enalapril maleate is mixed with spray-dried lactose, mannitol, sucralose, and talc in equal amounts;

[0032] (4) Dry granulate the above mixture, granulate through a 18-mesh sieve, and pack separately to obtain enalapril maleate granules.

Embodiment 2

[0033] Example 2 Preparation of Enalapril Maleate Granules (5mg)

[0034]

[0035] Preparation Process:

[0036] (1) Add the enalapril maleate raw material into the saturated aqueous solution of β-cyclodextrin, stir and mix for 30 minutes, filter, dry at 50°C, and control the water content to 2%;

[0037] (2) Pulverize the β-cyclodextrin inclusion compound of enalapril maleate and pass through a 80-mesh sieve;

[0038] (3) The pulverized cyclodextrin inclusion complex of enalapril maleate is mixed with spray-dried lactose, mannitol, stevioside, and talc in equal amounts;

[0039] (4) Dry granulate the above mixture, granulate through a 18-mesh sieve, and pack separately to obtain enalapril maleate granules.

Embodiment 3

[0040] Example 3 Preparation of Enalapril Maleate Granules (10mg)

[0041]

[0042] Preparation Process:

[0043] (1) Add the enalapril maleate raw material into the saturated aqueous solution of β-cyclodextrin, stir and mix for 30 minutes, filter, dry at 50°C, and control the water content to 2%;

[0044] (2) Pulverize the β-cyclodextrin inclusion compound of enalapril maleate and pass through an 80-mesh sieve;

[0045](3) The pulverized enalapril maleate cyclodextrin inclusion complex is mixed with spray-dried lactose, dextrin, sucralose, and talc in equal amounts;

[0046] (4) Dry granulate the above mixture, granulate through a 18-mesh sieve, and pack separately to obtain enalapril maleate granules.

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Abstract

The invention discloses enalapril maleate granules and aims to provide a granule prescription which can improve the drug stability. The enalapril maleate granules prepared by the method have the advantages that the enalapril maleate granules can be directly swallowed and can be further mixed in water to drink and can be quickly dissolved when coming across water; the enalapril maleate granules are good in taste, convenient to apply and carry, accurate to quantify, quick to take effect and high in availability. Meanwhile, the invention further discloses a preparation method of the enalapril maleate granules. By adopting a cyclodextrin inclusion technique, medicinal raw materials are included by virtue of a saturated aqueous solution method, so that the drug stability is improved. The process is simple to operate and low in cost, and the industrial amplifying application is increased.

Description

technical field [0001] The invention relates to a granule for treating essential hypertension and a preparation method thereof, in particular to an enalapril maleate granule and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] The chemical name of Enalapril maleate is N-[(S)-1-(ethoxycarbonyl)-3-phenylpropyl]-L-alanyl-L-proline butene Diacid salt, molecular formula C 20 h 28 N 2 o 5 ·C 4 h 4 o 4 , molecular weight 492.52, CAS accession number 76095-16-4. Enalapril was successfully developed by Merck, and in 1985, the FDA approved enalapril maleate unilateral tablet to go on the market. Enalapril is a second-generation angiotensin-converting enzyme inhibitor (ACEI). Unlike captopril in the first-generation ACEI, enalapril does not contain a sulfhydryl group (-SH), which reduces the first Side effects of decaptopril, such as abnormal cough, rash, proteinuria, and neutropenia. At the same time, enalapril is a pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K38/05A61K47/40A61P9/12A61P9/04
Inventor 姚丽华刁媛媛马苏峰
Owner 万全万特制药(厦门)有限公司
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