(S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule and preparation method thereof

A technology of pyrrolidine acetamide and oxo, which is used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Slow speed and other problems, to achieve the effect of simple and feasible preparation process, not easy to absorb moisture and agglomerate, and to dissolve quickly

Active Publication Date: 2017-12-26
武汉恒信源药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules mainly have impurities that increase significantly during the preparation process, are easy to stick to the screen during the granulation process, and are difficult to granulate, and the product has poor stability during storage. Particles have strong hygroscopicity, easy to stick and agglomerate, short shelf life, slow particle dissolution speed and other technical problems

Method used

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  • (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule and preparation method thereof
  • (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule and preparation method thereof
  • (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0028]

[0029] Preparation process:

[0030] 1. Preparation of adhesive: Take the prescribed amount of honey, put it in an iron pot, add purified water with 2 times the weight of honey, stir evenly, heat to 100-105°C, keep warm for 20-25 minutes, take it out, and use 80 Filter through a mesh sieve, take the filtrate, let it cool, add the ethanol of the prescription amount, stir and dissolve, and get final product;

[0031] 2. Pretreatment of raw and auxiliary materials: take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, L-cysteine, mannitol, microcrystalline cellulose, carboxymethyl cellulose Sodium, lactose, and low-substituted hydroxypropyl cellulose are placed in a universal pulverizer, pulverized through a 100-mesh sieve, and set aside;

[0032] 3. Granulation: Take the mixed powder obtained after the pretreatment, place it in a w...

Embodiment 2

[0075] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0076]

[0077] Preparation process: prepared according to the preparation process of Example 1. Observing the granulation process of the product did not find the phenomenon of sticking to the screen, and the product was easy to granulate. Tested by the test method of Example 1, the dissolution time measurement shows that this product has a fast dissolution rate, and the dissolution time of multiple samples is less than 30 seconds. The product prescription has an impact on the increase of impurities in the preparation process. The test results show that the impurities in the preparation process of this product The increase is small, and the related substances only increase by 0.02% in the preparation process; the stability test results show that the quality of the sample is stable in six months of acceleration, and stable in 24 months in a long-term period, so...

Embodiment 3

[0079] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0080]

[0081] Preparation process: prepared according to the preparation process of Example 1. Observing the granulation process of the product did not find the phenomenon of sticking to the screen, and the product was easy to granulate. Tested by the test method of Example 1, the dissolution time measurement shows that this product dissolves quickly, and the dissolution time of multiple samples is all less than 30 seconds. The test results of the impact of product prescription on the increase of impurities in the preparation process show that the impurities in the preparation process of this product The increase is small, and the related substances only increase by 0.03% in the preparation process; the stability test results show that the quality of the sample is stable in six months of acceleration, and stable in 24 months in a long-term period, so the val...

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Abstract

An (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule is prepared from, by weight, 1 part of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, 0.7-1.3 parts of L-cysteine, 1.0-1.5 parts of mannitol, 0.7-1.2 parts of microcrystalline cellulose, 0.9-1.5 parts of carboxymethylcellulose sodium, 0.7-1.3 parts of lactose, 0.13-0.18 part of magnesium stearate, 0.6-1.1 parts of polyethylene glycol 4000, 0.9-1.7 parts of hydroxypropyl methylcellulose, 0.8-1.3 part of low-substituted hydroxypropyl cellulose, 0.06-0.11 part of polysorbate 80, 0.5-1.2 parts of honey and 8-13 parts of an ethanol solution with the volume fraction being 50-70%. The (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide prepared in the invention has the advantages of small impurity increasing amount only being 0.03%, no adhesion to a screen and easy granulation during granulation, fast dissolution speed, short complete-dissolution time not exceeding 30 s, good stability during storage, no moisture absorbing caking, and long shelf life reaching up to 24 months.

Description

technical field [0001] The invention mainly relates to the field of pharmaceutical technology, in particular to (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules and a preparation method thereof. Background technique [0002] The chemical name of levo-oxiracetam is: S-(-)-4-hydroxy-2-oxopyrrolidine-N-acetamide. It is a white microcrystalline powder with a melting point of 135-136°C and an optical rotation of -36°( C=1.00inwater), the solubility of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide is obviously better than that of the racemate. The chemical structural formula is shown in the following formula: [0003] [0004] The drug was launched in Italy in 1987, and the listed dosage forms are tablets, 800mg; capsules, 800mg; injection, 1g / 5ml. At present, only oxiracetam capsules and injections are on the market in China, and the main active ingredients used are racemates. Ye Lei et al. mentioned in the patent CN 103735545A that (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetami...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4015A61K47/38A61K47/10A61P25/00A61P25/28
CPCA61K9/5031A61K9/5047A61K31/4015
Inventor 叶雷
Owner 武汉恒信源药业有限公司
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