Uniform-content (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule wand preparation method thereof

A technology of pyrrolidine acetamide and hydroxyl group, which is applied in the field of -4-hydroxy-2 oxo-1-pyrrolidine acetamide particles and their preparation, and can solve the problems of poor stability during storage, slow particle dissolution and particle size. The problem of strong hygroscopicity, etc., can achieve the effect of simple and feasible preparation process, fast dissolution speed and good content uniformity.

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 the problems of easy adhesion to the screen during the granulation process, difficulty in granulation, many particle powder layers, difficult control of particle size, and poor content uniformity. Poor, poor stability during storage, strong hygroscopicity of particles, easy to stick and agglomerate, short shelf life, slow particle dissolution speed and other technical problems

Method used

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  • Uniform-content (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule wand preparation method thereof
  • Uniform-content (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule wand preparation method thereof
  • Uniform-content (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule wand preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is 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 ethanol with a volume fraction of 60% to 80% of the prescription amount, stir to dissolve, and set aside;

[0031] 2. Pre-treatment of raw and auxiliary materials: take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide and polysorbate 80 and dissolve them in a 20% to 30% ethanol solution with a volume fraction of the prescribed amount , set aside; another prescription amount of mannitol, microcrystalline cellulose, sodium carboxymethyl cellulose, lactose, low-substituted hydroxypropyl cell...

Embodiment 2

[0086] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is prepared according to the following steps:

[0087]

[0088]

[0089] 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 Hughes angle is lower than 36 °, and the content uniformity test result shows that this product content uniformity is good, each after its total mixing The content RSD of point granules is less than 1%. The loading difference test shows that the loading difference of this product is less than 4%. The loading of this product is stable and controllable. The results of the dissolution test show that the dissolution time of this product is less tha...

Embodiment 3

[0091] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is prepared according to the following steps:

[0092]

[0093] 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 Hughes angle is lower than 38 °, and the content uniformity test result shows that this product content uniformity is good, each after its total mixing The content RSD of point granules is less than 2%. The loading difference test shows that the loading difference of this product is less than 5%. The loading of this product is stable and controllable. The results of the dissolution test show that the dissolution time of this product is less than 30 seconds...

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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, 1.3-1.9 parts of mannitol, 1.1-1.6 parts of microcrystalline cellulose, 0.5-1.0 part of carboxymethylcellulose sodium, 0.8-1.3 parts of lactose, 0.15-0.21 part of talcum powder, 0.7-1.3 parts of polyethylene glycol 4000, 0.8-1.5 parts of hydroxypropyl methylcellulose, 0.5-1.2 parts of low-substituted hydroxypropyl cellulose, 0.03-0.09 part of polysorbate 80, 1-5 parts of sorbitol, 0.15-0.21 part of honey, 8-13 parts of a 60-80% ethanol solution and 2-6 parts of a 20-30% ethanol solution. The (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule prepared in the invention has the advantages of easiness in granulation, small quantity of powder layers, uniform particle sizes, good fluidity, realization of the Xiuzi angle being less than 38 DEG and the loading difference being less than 5%, fast dissolution speed, short complete-dissolution time being less than 30 s, good content uniformity, realization of the determination RSD of the content in multiple points being less than 2%, good stability, no moisture absorbing caking, and long shelf life reaching up to 24 months.

Description

technical field [0001] The invention mainly relates to the technical field of pharmacy, in particular to (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide particles with uniform content and a preparation method thereof. Background technique [0002] Oxiracetam was launched in Italy in 1987 in the form of tablet, 800mg; capsule, 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 103735545 A that levoxiracetam has an obvious wake-promoting effect on coma caused by alcoholism, while dextro-oxiracetam has basically no effect. The wake-up effect is twice that of racemic oxiracetam; levo-oxiracetam has significant awakening effects on trauma and coma induced by anesthesia. Zhang Feng et al disclosed in the patent with the publication number CN103599101 A that levoxiracetam can significantly improve the learning, memory and co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4015A61K47/38A61K47/46A61K47/26A61P25/00A61P25/28
CPCA61K9/5031A61K9/5047A61K31/4015
Inventor 叶雷
Owner 武汉恒信源药业有限公司
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