Preparation method of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide lyophilized powder

Abstract

The invention discloses a preparation method of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide lyophilized powder. The lyophilized powder contains (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, methionine, lactose, triethanolamine and benzyl alcohol according to a mass ratio of 1:(0.4-0.6):(0.5-0.9):(0.2-0.4):(0.05-0.1). A specific excipient combination and a lyophilizing curve are used, so the sublimation temperature in a secondary drying stage is improved, the production cycle of the above preparation is shortened, the scattering phenomenon of the powder is avoided, the content and other indexes meet requirements, the aching feeling of patients in the injecting process is slight, the patients' compliance is good, and the untoward effects of the medicine are reduced.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a preparation method of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide freeze-dried powder. Background technique [0002] 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 can activate, protect or promote the functional recovery of nerve cells , to improve the memory and learning function of patients with mental retardation, and the drug itself has no direct vasoactive activity, nor does it have a central excitatory effect, and the effect on learning and memory ability is a lasting promotion effect. [0003] Oxiracetam (oxiracetam, CAS No.: 62613-82-5) chemical name is 4-hydroxy-2-oxo-1-pyrrolidineacetamide, which was synthesized for the first time in 1974 by the Italian company ISFS.P.A. Oxygen nootropic drug (compound disclosed in US411...

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Problems solved by technology

[0005] However, during the preparation of the existing (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide freeze-dried powder, the inventors found that in the secondary drying stage, the sublimation temperature is low, and the temperature cannot be high. At 20°C, this greatly prolongs the production cycle of the preparation. If the temperature in the secondary drying stage is increased, powder scattering will occur in the preparation, and its content will drop significantly

In addition, the existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide freeze-dried powder still has problems such as obvious pain during injection and poor patient compliance.

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