Method for improving stability of benserazide hydrochloride oral administration solid composition

A technology of benserazide hydrochloride and solid composition, which is applied in the field of pharmaceutical preparations, can solve the problems of solid preparation impurity detection exceeding the standard, accelerated long-term test research, and poor bioavailability, etc., to achieve shortened heating time, good protection effect, and complete granules Effect

Pending Publication Date: 2021-05-04
NANJING GRITPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because benserazide hydrochloride is very sensitive to air, light, temperature, and humidity, it is a raw material drug with poor stability. The conventional wet granulation process of benserazide hydrochloride has already deteriorated and degraded, resulting in the...

Method used

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  • Method for improving stability of benserazide hydrochloride oral administration solid composition
  • Method for improving stability of benserazide hydrochloride oral administration solid composition
  • Method for improving stability of benserazide hydrochloride oral administration solid composition

Examples

Experimental program
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Effect test

Embodiment 1-4

[0043] The benserazide hydrochloride-levodopa compound tablet was prepared by wet granulation and vacuum drying.

[0044] prescription composition Prescription mass ratio (%) Levodopa 36.4 Benserazide Hydrochloride 10.2 microcrystalline cellulose 30.8 Mannitol 1.8 Calcium hydrogen phosphate anhydrous 1.8 pregelatinized starch 5 Crospovidone 5 povidone 7 Micropowder silica gel 1 Magnesium stearate 1

[0045] Preparation:

[0046] 1) Weigh the prescription amount of levodopa, microcrystalline cellulose, 2 / 3 prescription amount of crospovidone and mix, make soft material with 5% povidone ethanol solution, granulate with 24 mesh sieve, dry in convection oven for about 2 hours.

[0047] 2) Weigh the prescription amount of benserazide hydrochloride, mannitol, anhydrous calcium hydrogen phosphate, pregelatinized starch, mix with 1 / 3 of the prescription amount of cross-linked povidone, and make soft material wi...

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Abstract

The invention belongs to the field of drug preparations, and particularly relates to a method for improving the stability of an oral administration solid composition containing benserazide hydrochloride. The benserazide hydrochloride is a peripheral decarboxylase inhibitor, and the benserazide hydrochloride and levodopa are always prepared into a compound preparation and are combined to be mainly used for treating the Parkinson' s disease (essential paralysis agitans), and postencephalitic or the symptomatic Parkinson' s syndrome (non-drug-induced paralysis agitans syndrome) combined with cerebral arteriosclerosis. The property of the benserazide hydrochloride is extremely unstable, and the benserazide hydrochloride is extremely sensitive to change of PH, ray, temperature and humidity. Since the ways of wet granulation and vacuum drying are adopted, the stability of the benserazide hydrochloride in an oral administration solid preparation containing the benserazide hydrochloride can be improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a stable oral solid composition of benserazide hydrochloride and a preparation process thereof. Background technique [0002] Parkinson's syndrome, also known as Parkinson's paralysis, is a disease with a very high incidence rate, which causes dysfunction of the extrapyramidal system of the central nervous system. Parkinson's patients lack dopamine in the basal nerve, and levodopa can pass through the blood brain The barrier enters the center to replace dopamine, but levodopa is rapidly decarboxylated into dopamine in the periphery, and only a small amount enters the brain, which will cause adverse reactions. Benserazide hydrochloride is a peripheral decarboxylase inhibitor, and it can be combined with levodopa. Effective treatment of Parkinson's syndrome, and symptomatic Parkinson's syndrome after encephalitis or combined with cerebral arteriosclerosis. ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/165A61K31/198A61P25/16A61P9/10
CPCA61K31/165A61K31/198A61K9/1652A61P25/16A61P9/10A61K2300/00
Inventor 张倩倩芦彩萍何红燕朱飞周静罗琦赵卿霍立茹李战
Owner NANJING GRITPHARMA CO LTD
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