High-stability (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide sustained release capsule and preparation method thereof

Abstract

The invention provides a high-stability (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide sustained release capsule, which is prepared from the following raw and auxiliary materials: 1 part of (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide, 0.5 to 1.1 parts of lactose, 1.8 to 2.7 parts of hydroxypropyl methyl cellulose K4M, 0.3 to 0.9 part of carnauba wax, 0.03 to 0.08 part of octadecanol, 0.12 to 0.18 part of magnesium stearate, 0.3 to 0.8 part of calcium hydrophosphate, 0.2 to 0.9 part of superfine silica gel powder and 2.8 to 3.9 parts of 7 to 10 percent polyvidone K30 ethanol solutions. The (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide sustained release capsule provided by the invention has the advantages that the particle flowability is high; the particle rest angle is smaller than 37 degrees; the powder layer is few after the particle sorting; the finished product yield is as high as 93.9 percent; the release speed is low; the release period is as long as 12 hours; meanwhile, the product stability is high; the capsule adhesion phenomenon cannot occur in the storage process; and the shelf life is as long as 24 months.

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 sustained-release capsule and a preparation method thereof. Background technique [0002] Oxiracetam (S-oxiracetam) is a synthetic cyclic derivative of hydroxyaminobutyric acid (BABOB), which is only used in the central nervous system, mainly distributed in the cerebral cortex and hippocampus, and has the function of activating, protecting or promoting nerve cells. Functional recovery can improve the memory and learning functions of patients with mental retardation, and the drug itself has no direct vasoactive or central excitatory effect, and its effect on learning and memory is a lasting promotion effect. [0003] The drug was launched in Italy in 1987, and the listed dosage forms are tablets, 800mg; capsules, 800mg; injection, 1g / 5ml. At present, only oxiracetam capsules and injections are on the market in Chi...

AI Technical Summary

Problems solved by technology

[0004] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsules mainly have the problems that the release rate cannot be well controlled, and the requirements for sustained-release preparations cannot be met, the fluidity of the particles is not good, and the filling process is difficult. There is a large difference in the filling volume, which affects the dosage of the drug. There are more granular powder layers after the granulation, the yield of the finished product is low, and the capsules are easy to stick and agglomerate during storage and other technical problems.

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