(S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets having good stability and preparation method of effervescent tablets

Abstract

(S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets having good stability are made from the following raw and auxiliary materials, according to a weight ratio, 1 part of (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide, 4-9 parts of tartaric acid, 4-9 parts of sodium bicarbonate, 0.3-0.9 part of sodium chloride, 0.45-1.35 parts of polyethylene glycol 6000, 2-9 parts of dextrin, 3-8 parts of sucrose, 15-25 parts of a PVP/VA64 ethanol solution with the mass percentage being 8-16%, 3-9 parts of sodium carboxymethylcellulose, and 7-12 parts of microcrystalline cellulose. During preparation, the prepared (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets are good in particle formability and less in powder layer amount, and have less than 4% by weight of particles that don't conform to the standard of particle granularity detection. The effervescent tablet product is fast in gas generation and disintegration speed, and has the disintegration time no more than 30 s. The effervescent tablet product is not prone to absorb moisture and go bad and is easy to store and long in shelf life. The preparation method is simple and feasible and is worth market popularization.

Description

technical field [0001] The invention mainly relates to the field of pharmaceutical technology, in particular to a stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide effervescent tablet and a preparation method thereof. Background technique [0002] Nootropic drug, also known as brain activator, is a new type of central nervous system drug that promotes learning and enhances memory. Nootropic drugs are required to selectively act on the cerebral cortex, and have the characteristics of selectively activating, protecting and promoting the recovery of damaged nerve cell functions. The difference from other neurological drugs is that their above-mentioned effects do not pass through the reticular system or the olfactory bulb, but directly act on the cortex. It neither affects behavior nor has sedative and exciting effects, so this class of drugs has attracted widespread attention and interest, and the demand for this class of drugs is also increasing day by day. [0003] Oxirace...

AI Technical Summary

Problems solved by technology

[0005] The existing (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide effervescent preparation mainly has the following problems: the granules are not easy to form in the granulation process, the granule powder layer is more, the particle size is not easy to control, and the tableting process is easy to stick and punch. The finished product has slow gas production and disintegration, and the product is easy to absorb moisture and deteriorate during storage, resulting in poor stability and short shelf life.

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