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

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, 0.7-1.2 parts of L-cysteine, 0.6-1.0 part of mannitol, 1.1-1.6 parts of microcrystalline cellulose, 0.5-1.2 parts of carboxymethylcellulose sodium, 0.8-1.3 parts of lactose, 0.13-0.18 part of talcum powder, 1.1-1.7 parts of polyethylene glycol 4000, 0.9-1.5 parts of hydroxypropyl methylcellulose, 0.6-1.3 parts of low-substituted hydroxypropyl cellulose, 0.05-0.11 part of polysorbate 80, 1-5 parts of sorbitol, 10-16 parts of a 6-8% starch slurry and 2-5 parts of a 20-30% ethanol solution. The (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule prepared in the invention has the advantages of small impurity increasing amount only being 0.03%, 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 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 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 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...

AI Technical Summary

Problems solved by technology

[0005] Existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules mainly have a significant increase in impurities during the preparation process, more particle powder layers, difficult particle size control, poor content uniformity, and stability during storage Not good, the particles have strong hygroscopicity, easy to stick and agglomerate, short shelf life, slow particle dissolution speed and other technical problems

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