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A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide injection and its preparation method

A technology of pyrrolidine acetamide and hydroxyl, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve problems such as easy crystallization during storage, poor patient compliance, and poor stability of finished products , to achieve the effect of less impurities, less pain and long validity period

Active Publication Date: 2018-12-14
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide injections mainly suffer from large pH changes in the solution during the sterilization process, poor stability of the finished product, easy crystallization during storage, obvious pain during the injection process, and patient compliance. gender issues

Method used

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  • A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide injection and its preparation method
  • A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide injection and its preparation method
  • A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide injection and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide injection prepared according to the following steps:

[0022]

[0023] Preparation process:

[0024] 1. Concentrated formulation: Add the above-mentioned raw and auxiliary materials into the batching tank, then add 2 / 3 of the prescription amount of sterile water for injection, stir, dissolve, and obtain a concentrated formulation;

[0025] 2. Dilute preparation: Take the concentrated preparation, add sodium phosphate buffer solution (precisely weigh 65.697g of disodium hydrogen phosphate and 2.346g of sodium dihydrogen phosphate, put it in a 1000ml volumetric flask, add purified water to dissolve, dilute to the scale , to get) adjust the pH to 6.8, add activated carbon of 0.1% to 0.3% (g / ml) of the total volume, absorb and decolorize, filter with a 0.45 μm filter membrane, collect the filtrate, add sterilized water for injection to the prescribed amount, and The intermediate product inspection is qualified;

[00...

Embodiment 2

[0065] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide injection prepared according to the following steps:

[0066]

[0067] Preparation process: prepared according to the preparation process of Example 1.

[0068] According to the test method of embodiment 1, the sample of embodiment 2 is carried out experimental investigation respectively, and the stability test result shows that accelerated 6 months sample quality is stable, long-term 18 months quality is stable, so this product is valid for at least 18 months. The results of the mouse writhing method to observe the pain during the injection showed that the pain of the sample of Example 2 was significantly weaker than that of the control sample during the injection. Experiments on the influence of different pH regulators on the pH of the solution before and after product sterilization showed that the pH of the solution of the sample prepared in Example 2 was basically unchanged before and after sterilization.

Embodiment 3

[0070] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide injection prepared according to the following steps:

[0071]

[0072] Preparation process: prepared according to the preparation process of Example 1.

[0073] According to the test method of embodiment 1, the sample of embodiment 3 is carried out experimental investigation respectively, and the stability test result shows that accelerated 6 months sample quality is stable, long-term 18 months quality is stable, so this product is valid for at least 18 months. The results of the mouse writhing method to observe the pain during the injection showed that the pain of the sample of Example 3 was significantly weaker than that of the control sample during the injection. Experiments on the influence of different pH regulators on the pH of the solution before and after product sterilization showed that the pH of the solution of the sample prepared in Example 3 did not change substantially before and after sterilization. ...

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Abstract

The invention provides (S)-4-hydroxyl-2-oxo-1-pyrrolidine acetamide for injection, which is prepared from the following raw and auxiliary materials: 65-85% of (S)-4-hydroxyl-2-oxo-1-pyrrolidine acetamide, 8-25% of propylene glycol, 5-25% of lecithin and 1-5% of benzyl alcohol. The pH value of the (S)-4-hydroxyl-2-oxo-1-pyrrolidine acetamide injection during sterilization is basically not changed, and the product has good stability, is free of crystallization during storage, has long effective period which can reach more than 18 months, is low in impurities during effective period with total impurity being lower than 0.36%, can reduce pain during injection to patients and has good patient compliance.

Description

technical field [0001] The invention mainly relates to the technical field of pharmacy, in particular to a stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide injection 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 China, and the main active...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/4015A61K47/10A61K47/24A61P25/00
CPCA61K9/0019A61K9/08A61K31/4015A61K47/10A61K47/24
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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