(S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sterile powder and preparation method thereof

A technology of pyrrolidine acetamide and sterile powder, which can be used in powder delivery, pharmaceutical formulations, inorganic non-active ingredients, etc. It can solve the problems of poor product stability, poor patient compliance, and prone to spray bottles, etc., so as to reduce adverse drug reactions , Patient compliance is good, and the effect of improving safety

Inactive Publication Date: 2017-12-05
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the existing (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide aseptic powder has no fixed shape, is not easy to form a skeleton, is prone to spray bottle phenomenon in the freeze-drying process, and has product The problem of poor stability, before clinical use, it needs to be dissolved in 5% glucose injection or 0.9% sodium chloride injection 100 ~ 250ml, prepared as

Method used

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  • (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sterile powder and preparation method thereof
  • (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sterile powder and preparation method thereof
  • (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sterile powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The prescription of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide aseptic powder of embodiment 1 is shown in the table below:

[0021] prescription

weight percentage

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

50％

L-serine

24％

Mannitol

15％

sodium glutamate

5％

sodium bisulfite

5％

Benzyl alcohol

1％

[0022] The preparation method of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide aseptic powder of embodiment 1 comprises the following steps:

[0023] (1) Concentrated preparation: put the raw and auxiliary materials of the prescribed amount in the container, add (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide 10 times the weight of sterile water for injection and stir, after dissolving , adding 0.1% mass fraction of active carbon for needles, stirring for 30 minutes, then filtering with a 0.45 micron microporous membrane, collecting the filtrate, and setting aside;

[0024] (2) Dilute preparation: add ster...

Embodiment 2

[0028] The prescription of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide sterile powder of embodiment 2 is shown in the following table:

[0029] prescription

[0030] The preparation method of the sterile powder of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide in Example 2 is the same as that in Example 1.

Embodiment 3

[0032] The prescription of (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide sterile powder of embodiment 3 is shown in the following table:

[0033] prescription

[0034] The preparation method of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sterile powder of Example 3 is the same as that of Example 1.

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Abstract

The present invention discloses (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sterile powder and a preparation method thereof, wherein the sterile powder contains the following raw materials and the auxiliary materials by weight: 50-59% of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, 20-25% of L-serine, 10-17% of mannitol, 5-7% of sodium glutamate, 5-10% of sodium hydrogen sulfite, and 1-3% of benzyl alcohol. According to the present invention, by using the specific excipient combination, the prepared (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sterile powder has the fixed shape, and cannot be sprayed out of the bottle during the freeze drying, the stability of the product is good, the insoluble particles are obviously reduced and the size of the insoluble particles is obviously reduced, the pain of patients during the injection is less, the patient compliance is good, the drug use safety can be easily improved, and the adverse reaction of the drug can be reduced.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a sterile powder of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide and a preparation method thereof. Background technique [0002] The chemical name of levo-oxiracetam is: (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, which is a white microcrystalline powder with a melting point of 135-136°C and an optical rotation of -36° (C= 1.00in water), the solubility of levoxiracetam is obviously better than that of racemate. The chemical structural formula is as follows: [0003] [0004] 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 ingredients used are racemates. Ye Lei et al mentioned in the patent publication No. CN 103735545 A that levoxiracetam has an obvious wake-promoting effect on coma caused by alcohol...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4015A61K47/18A61K47/26A61K47/10A61K47/02A61P25/00A61P25/28
CPCA61K9/0019A61K9/19A61K31/4015A61K47/02A61K47/10A61K47/183A61K47/26
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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