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, 0.8-1.3 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...

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.

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