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

A technology of pyrrolidine acetamide and freeze-dried powder, which is applied in freeze-dried delivery, powder delivery, nervous system diseases, etc. It can solve the problems of prolonging the production cycle of preparations, the temperature cannot be higher than 20°C, and the sublimation temperature is low, so as to reduce the The effect of adverse drug reactions, shortening the production cycle of preparations, and increasing the sublimation temperature

Inactive Publication Date: 2018-01-05
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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....

Method used

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

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The prescription of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide freeze-dried powder of embodiment 1 is shown in the table below:

[0019] prescription

weight percentage

(S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide

100g

Methionine

50g

lactose

70g

Triethanolamine

30g

Benzyl alcohol

8g

Water for Injection

Add to 500mL

[0020] The preparation method of the (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide freeze-dried powder of embodiment 1 comprises the following steps:

[0021] (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide, methionine, lactose, triethanolamine and benzyl alcohol were dissolved in water for injection, adjusted with 0.1mol / L hydrochloric acid solution pH to 4.5, then lyophilized as follows:

[0022] (1) Pre-freezing stage: Freeze the temperature to -15°C within 5 minutes; then raise the temperature to -9°C for 30 minutes; freeze the temperature to -32°C within 5 minutes again; then raise ...

Embodiment 2

[0026] The prescription of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide freeze-dried powder of embodiment 2 is shown in the table below:

[0027] prescription

weight percentage

(S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide

100g

Methionine

40g

lactose

50g

Triethanolamine

20g

Benzyl alcohol

5g

Water for Injection

Add to 500mL

[0028] The preparation method of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide freeze-dried powder of embodiment 2 comprises the following steps:

[0029] (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide, methionine, lactose, triethanolamine and benzyl alcohol were dissolved in water for injection, adjusted with 0.1mol / L hydrochloric acid solution pH to 5.0, then lyophilized as follows:

[0030] (1) Pre-freezing stage: freeze the temperature to -15°C within 10 minutes; then raise the temperature to -10°C, and the heating time is 40 minutes; freeze the temperature to -35°C within 10 minute...

Embodiment 3

[0034] The prescription of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide freeze-dried powder of embodiment 3 is shown in the table below:

[0035] prescription

weight percentage

(S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide

100g

Methionine

60g

lactose

90g

Triethanolamine

40g

Benzyl alcohol

10g

Water for Injection

Add to 500mL

[0036] The preparation method of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide freeze-dried powder of embodiment 3 comprises the following steps:

[0037] (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide, methionine, lactose, triethanolamine and benzyl alcohol were dissolved in water for injection, adjusted with 0.1mol / L hydrochloric acid solution pH to 5.0, then lyophilized as follows:

[0038] (1) Pre-freezing stage: freeze the temperature to -18°C within 15 minutes; then raise the temperature to -8°C, and the heating time is 60 minutes; freeze the temperature to -36°C within 15 minute...

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4015A61K47/20A61K47/26A61K47/18A61K47/10A61P25/28
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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