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 problem that the particle size is not easy to control, the particles have strong hygroscopicity and are easy to stick to the block. and other problems, to achieve the effect of simple and feasible preparation process, good content uniformity, 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

[0005] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules mainly exist that the impurities increase during the preparation process, the granulation process is easy to stick to the screen, the granulation is difficult, the granule powder layer is more, and the granulation is difficult. The diameter is not easy to control, the content uniformity is poor, the stability of the storage process is not good, the particles are hygroscopic, easy to stick and agglomerate, the shelf life is short, and the particle dissolution rate is slow.

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 , and set aside; another prescription amount of L-cysteine, mannitol, microcrystalline cellulose, sodium carboxymethyl cellulose, lactose, low-substituted hy...

Embodiment 2

[0094] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is prepared according to the following steps:

[0095]

[0096] 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 1%, and the difference test of the filling volume shows that the loading volume difference of this product is less than 5%, the loading volume of this product is stable and controllable, and the test results of the influence of product prescription on the incre...

Embodiment 3

[0098] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is prepared according to the following steps:

[0099]

[0100] 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 2%. The difference test of the filling volume shows that the filling volume difference of this product is less than 4%. The loading volume of this product is stable and controllable. The test result of the influence of product prescription on the increase of im...

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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, 0.8-1.3 parts of L-cysteine, 1.1-1.6 parts of mannitol, 0.8-1.2 parts of microcrystalline cellulose, 0.8-1.2 parts of carboxymethylcellulose sodium, 0.5-1.1 parts of lactose, 0.17-0.22 part of talcum powder, 0.6-1.1 parts of polyethylene glycol 4000, 0.7-1.3 parts of hydroxypropyl methylcellulose, 0.8-1.3 part of low-substituted hydroxypropyl cellulose, 0.05-0.10 part of polysorbate 80, 0.8-1.8 parts of sorbitol, 0.18-0.27 part of honey, 12-18 parts of 60-70% ethanol and 1-5 parts of 20-30% ethanol. The (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule prepared in the invention has the advantages of small impurity increasing amount only being 0.04%, no adhesion to a screen during granulation, small quantity of powder layers, uniform particle size, good fluidity, realization of the Xiuzi angle being less than 38 DEG, small loading difference being less than 5%, short complete-dissolution time being less than 30 s, good content uniformity, realization of the content RSD of multiple points being less than 2%, good stability during storage, 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): A61K9/50A61K47/38A61K47/10A61K47/26A61K47/18A61P25/00A61P25/28
CPCA61K9/5031A61K9/5047A61K9/5089A61K31/4015A61K47/18A61K47/26
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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