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Itopride hydrochloride fast-release preparation and preparation method thereof

A rapid technology of itopride hydrochloride, which is applied in the field of chemical medicine, can solve the problems of weak dopamine D2 receptor blocking effect and no pharmacological correlation, etc., and achieve the effect of fast release speed

Pending Publication Date: 2020-02-07
CHENGDU HENGRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Itopride hydrochloride is converted into metabolites M1, M2 and M3 mainly through the flavin monooxygenase pathway in the liver. Among the three metabolites, only one of them has a weak dopamine D2 receptor blocking effect, and has no pharmacological relevance

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The rapid release preparation of itopride hydrochloride comprises 50 mg of itopride hydrochloride, 10 mg of croscarmellose sodium, 100 mg of starch and 1 mg of magnesium stearate in parts by weight.

[0023] Utilize above-mentioned components to carry out preparation of itopride hydrochloride rapid release preparation, the steps are:

[0024] S1. First pass itopride hydrochloride and croscarmellose sodium through a planetary grinder at a weight ratio of 1:1 to form grinding powder;

[0025] S2. Put the grinding powder, starch and magnesium stearate into the mixer and mix evenly. After mixing for a period of time, add a part of water and continue mixing;

[0026] S3, and then use a tablet press to compress the tablet and dry it.

[0027] Further, in the step S1, grind at a speed of 150-250 revolutions per minute, 4 times×30 minutes for cyclic grinding.

[0028] Preferably, when grinding in the step S3, tablet compression is performed at 151 mg / tablet, and the tablet co...

Embodiment 2

[0030] The rapid-release preparation of itopride hydrochloride, in parts by weight, comprises 100 mg of itopride hydrochloride, 50 mg of croscarmellose sodium, 150 mg of starch, and 2 mg of magnesium stearate.

[0031] Utilize above-mentioned components to carry out preparation of itopride hydrochloride rapid release preparation, the steps are:

[0032] S1. First pass itopride hydrochloride and croscarmellose sodium through a planetary grinder at a weight ratio of 1:1 to form grinding powder;

[0033] S2. Put the grinding powder, starch and magnesium stearate into the mixer and mix evenly. After mixing for a period of time, add a part of water and continue mixing;

[0034] S3, and then use a tablet press to compress the tablet and dry it.

[0035] Further, in the step S1, grind at a speed of 150-250 revolutions per minute, 4 times×30 minutes for cyclic grinding.

[0036] Preferably, in the step S3, tablet compression is performed at 151 mg / tablet, and the tablet compression ...

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PUM

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Abstract

The invention relates to an itopride hydrochloride fast-release preparation and a preparation method thereof. The itopride hydrochloride fast-release preparation comprises the following components inparts by weight: 50-100 parts of itopride hydrochloride, 10-50 parts of croscarmellose sodium, 20-150 parts of starch and 1-2 parts of magnesium stearate. The invention achieves the following beneficial effects: in order to release an effective drug component, namely the itopride hydrochloride, as soon as possible, the types of other auxiliary materials are few, a small amount of croscarmellose sodium is used as a swelling agent, a small amount of thickening agent is used, and the only auxiliary material with a higher content is the starch, which is beneficial to human digestion, so that the release speed of the whole tablet is very high.

Description

technical field [0001] The invention relates to the field of chemical medicine, in particular to an itopride hydrochloride fast-release preparation and a preparation method thereof. Background technique [0002] Itopride hydrochloride has dopamine D2 receptor antagonistic activity and acetylcholinesterase inhibitory activity, and exerts gastrointestinal prokinetic effect through the synergistic effect of the two; in addition, due to the effect of antagonizing dopamine D2 receptor activity, this product still has certain It is clinically used for dyspepsia symptoms caused by slowed gastrointestinal motility (such as functional dyspepsia, chronic gastritis, etc.), including epigastric fullness, epigastric pain, loss of appetite, nausea and vomiting Wait. Itopride hydrochloride is converted into metabolites M1, M2 and M3 mainly through the flavin monooxygenase pathway in the liver. Among the three metabolites, only one of them has a weak dopamine D2 receptor blocking effect, a...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/36A61K47/38A61K31/166A61P1/08A61P1/14
CPCA61K9/2054A61K9/2059A61K31/166A61P1/08A61P1/14
Inventor 刘辉
Owner CHENGDU HENGRUI PHARMA
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