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Oxiracetam drug activity composition and preparation method thereof

A technology of drug activity and composition, applied in the field of medicine, can solve the problems of unqualified drug quality control, poor product stability, unstable quality, etc., and achieve the effect of ensuring clinical efficacy, drug safety, and stable quality

Active Publication Date: 2013-01-02
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] To sum up, the active oxiracetam pharmaceutical products disclosed in the prior art all have two common shortcomings: (1) the product ingredients are complex, and the composition of impurities cannot be determined except for the active ingredient; Systematic research on the content of impurities in the drug; the safety of medication cannot be guaranteed; (2) The product has poor stability. During the placement process, the content of active ingredients is significantly reduced, and the content of impurities is significantly increased. The quality is very unstable, uncontrollable, and does not meet the quality of drugs Controllable requirements; therefore, the oxiracetam pharmaceutical active product provided in the prior art cannot be used as a medicine

Method used

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  • Oxiracetam drug activity composition and preparation method thereof
  • Oxiracetam drug activity composition and preparation method thereof
  • Oxiracetam drug activity composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0065] Preparation Example 1: Oxiracetam pharmaceutical active product, prior art product, prepared according to the preparation method disclosed in Japanese Patent JP62026267

[0066] Under the protection of nitrogen, add 11.1Kg of glycinamide hydrochloride, 100L of absolute ethanol and 10.6Kg of anhydrous sodium carbonate into the reaction tank equipped with mechanical stirring, then slowly add 4-chloro-3-hydroxybutyric acid into the reaction solution 16.7Kg of ethyl ester was added in 60 minutes. Then start timing after warming up to reflux, and the reaction time is 24h; after the reaction is completed, filter under reduced pressure while hot, and wash the filter cake with absolute ethanol; take the filtrate, distill the solvent under reduced pressure; evaporate to dryness to obtain a brown viscous liquid, and Dissolve it in 25L of water, pass the above-mentioned aqueous solution through a strong acidic styrene-based cation exchange resin and collect it, then use a strong...

preparation example 2

[0067] Preparation Example 2: Oxiracetam pharmaceutical active product, prior art product, according to the preparation method disclosed in Chinese patent CN101723871

[0068]5h。 Under the protection of nitrogen, add glycinamide hydrochloride 16.6Kg, absolute ethanol 100L and anhydrous sodium carbonate 40Kg to the reaction tank equipped with mechanical stirring, add Tween-20 0.50Kg, react at room temperature for 0. 5h. Next, 23.3 Kg of methyl 4-chloro-3-hydroxybutyrate was added slowly, and the addition was completed in 40 minutes. Then start timing after heating up to reflux, the reaction time is 20h; after 20h of reaction, filter under reduced pressure while hot, and wash the filter cake with absolute ethanol. The filtrate was taken, and the solvent was distilled off under reduced pressure. Evaporate to dryness to obtain a brown viscous liquid, which is recrystallized by adding 25L of absolute ethanol. The solid was precipitated, filtered under reduced pressure, the filt...

Embodiment 1

[0073] Embodiment 1: Oxiracetam pharmaceutically active composition

[0074] Oxiracetam crude product: Oxiracetam crude product prepared according to the method of Preparation Example 1

[0075] A. Dissolution: Dissolve 200g of crude oxiracetam in 600ml of purified water, add 1.0g of activated carbon, heat up to 40°C, control the temperature at 40~50°C, stir and decolorize for 0.5 hours, filter, and collect the filtrate;

[0076] B. Chromatographic separation: Put the collected filtrate on the chromatographic separation column, use water as the mobile phase, and the stationary phase is silica gel with embedded amino polar groups. The flow rate is 40ml / min, the column temperature is 30°C, and the eluent is collected in sections , combining the eluate with a purity greater than 95%;

[0077] C. Concentration by nanofiltration: Concentrate the eluent by nanofiltration to 1 / 2 of the volume;

[0078] D. Crystallization: Add 15.0L of acetone to the concentrated solution to pre...

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Abstract

The present invention provides an oxiracetam drug activity composition, which comprises the following components: a component I, a component II and a component III, wherein the component I is oxiracetam, the component I content is more than or equal to 98.0%, the component II is glycine anhydride, the component II content is more than 0 and is less than or equal to 0.3%, the component III is one or a plurality materials selected from 4-hydroxy-2-oxo-1-pyrrolidineacetic acid, 4-hydroxy-2-oxo-1-pyrrolidine, ethyl 4-hydroxy-2-oxopyrrolidine-1-acetate, methyl 4-hydroxy-2-oxopyrrolidine-1-acetate, and piracetam, the component III content is more than 0 and is less than or equal to 1.5%, the 4-hydroxy-2-oxo-1-pyrrolidineacetic acid content is more than 0 and is less than or equal to 0.5%, and the total content of the component II and the component III is less than or equal to 1.5%. The drug activity composition of the present invention has stable quality, and can completely meet quality requirements on the drug activity composition by oxiracetam preparations. In addition, the prepared preparation has characteristics of safety, effectiveness, and controllable quality, and clinical therapy effects and medication safety of the oxiracetam preparation are ensured.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a pharmaceutically active composition containing 4-hydroxy-2-oxo-1-pyrrolidineacetamide (oxiracetam) and a preparation method thereof. Background technique [0002] Oxiracetam, whose chemical name is 4-hydroxyl-2-oxo-1-pyrrolidineacetamide, has a chemical structural formula as shown in formula 1. It is a nootropic drug that can improve the cognitive function of patients with senile dementia and memory impairment. Memory and learning function, research results show that oxiracetam can promote the synthesis of phosphorylcholine and phosphorylethanolamine, increase the ratio of ATP / ADP in the brain, increase the synthesis of protein and nucleic acid in the brain, and is clinically used for brain injury and the treatment of neurological deficits, memory and mental disorders caused by [0003] . [0004] Oxiracetam was developed by the Italian ISF company and was launc...

Claims

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Application Information

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IPC IPC(8): A61K31/4015A61P25/28
Inventor 李瑞建张朝晖孙成勇郑雪清王绕赵亚楠
Owner CSPC OUYI PHARM CO LTD
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