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(S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule having good stability, and preparation method thereof

A pyrrolidine acetamide and stability technology, which is applied in the field of -4-hydroxy-2 oxo-1-pyrrolidine acetamide particles and their preparation, can solve the problem that the particle size is not easy to control, the particles have strong hygroscopicity and easy adhesion. In order to achieve the effect of simple and feasible preparation process, uniform particle size, and not easy to absorb moisture and agglomerate

Inactive Publication Date: 2017-12-26
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules mainly have a large increase in impurities during the preparation process, and the granulation process is easy to stick to the screen, making granulation difficult, and the granule powder layer is more during the preparation process , the particle size is difficult to control, the stability of the storage process is poor, the particles are hygroscopic, easy to stick and agglomerate, the shelf life is short, the taste of the particles is poor, and it is not easy to be accepted by patients.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide granule is prepared according to the following steps:

[0026]

[0027]

[0028] Preparation process:

[0029] 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 ethanol in the prescribed amount, stir to dissolve, and set aside;

[0030] 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, sucrose, and ethyl maltol are placed in a universal grinder, crushed through a 100-mesh sieve, and set aside;

[0031] 3. Granulation: Take the mixed powder obtained after pretreatment, put it in a wet granulator, add the previously...

Embodiment 2

[0087] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide granule is prepared according to the following steps:

[0088]

[0089]

[0090]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. Carry out the test by the test method of embodiment 1, the Hughes angle test measurement result shows that this product granule fluidity is good, and the Hughes angle is lower than 37 °, and the loading difference test shows that the loading difference of this product is less than ± 5%. The amount is stable and controllable, and the test results of the influence of product prescription on the increase of impurities in the preparation process show that the increase of impurities in the preparation process of this product is small, and the related substances in the preparation process only increase by 0.03%. The qu...

Embodiment 3

[0092] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0093]

[0094] 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. Carry out the test by the test method of embodiment 1, the Hughes angle test measurement result shows that this product granule fluidity is good, and the Hughes angle is lower than 35 °, and the loading difference test shows that the loading difference of this product is less than ± 4%. The amount is stable and controllable, and the test results of the influence of product prescription on the increase of impurities in the preparation process show that the increase of impurities in the preparation process of this product is small, and the related substances in the preparation process only increase by 0.03%. The quality is st...

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Abstract

An (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide having a good stability is prepared from, by weight, 1 part of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, 0.6-1.1 parts of L-cysteine, 0.7-1.3 parts of mannitol, 0.5-1.1 parts of microcrystalline cellulose, 0.9-1.5 parts of carboxymethylcellulose sodium, 0.5-1.0 part of lactose, 0.13-0.18 part of talcum powder, 1.3-1.8 parts of polyethylene glycol 4000, 1.0-1.5 parts of hydroxypropyl methylcellulose, 1-5 parts of sucrose, 0.3-0.9 part of ethyl maltol, 1.0-1.5 parts of honey and 10-16 parts of ethanol with the volume fraction being 55-70%. The (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule prepared in the invention has the advantages of small impurity increasing amount being only 0.03% in the preparation process, no adhesion to a screen and easiness in granulation during granulation, small quantity of powder layers, uniform particle size, good fluidity, realization of the Xiuzi angle being less than 37 DEG and the loading difference being less than 5%, good stability during storage, no moisture absorption caking, long shelf life reaching up to 24 months, and good mouthfeel, and can be received by most patients.

Description

technical field [0001] The invention mainly relates to the technical field of pharmacy, in particular to a stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule and a preparation method thereof. Background technique [0002] Oxiracetam (S-oxiracetam) is a synthetic hydroxyaminobutyric acid (BABOB) cyclic derivative. The drug was launched in Italy in 1987. 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 publication No. CN 103735545A that levoxiracetam has an obvious effect of promoting awakening on the coma caused by alcoholism, while dextro-oxiracetam has basically no effect. The above-mentioned awakening effect of levoxiracetam The effect is 2 times that of racemic oxiracetam; Levo-oxiracetam has significant wake-promoting effects on trauma and coma induced by anesthes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/38A61K47/46A61K31/4015A61P25/00A61P25/28
CPCA61K9/1652A61K9/1664A61K9/1682A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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