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

A technology of pyrrolidine acetamide and oxo, which is applied in the directions of nervous system diseases, capsule delivery, microcapsules, etc., can solve the problems of easy-adhesion screen, easy-adhesion block, slow particle dissolving speed, etc., and achieves a simple preparation process. Feasible, not easy to absorb moisture and agglomerate, and the effect of fast dissolution

Inactive Publication Date: 2017-12-26
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules mainly have the problems of easy sticking to the screen during the granulation process, difficulty in granulation, poor stability during product storage, strong hygroscopicity of the granules, and easy sticking Linked blocks, short shelf life, slow dissolution of particles and other technical problems

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0028] Element

Dosage

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

1 copy

Mannitol

1.5 servings

microcrystalline cellulose

1.1 copies

Sodium carboxymethyl cellulose

0.7 parts

lactose

0.6 parts

Magnesium stearate

0.11 parts

polyethylene glycol 4000

0.7 parts

hypromellose

0.9 parts

Low-substituted hydroxypropyl cellulose

0.7 parts

Polysorbate 80

0.05 parts

Honey

0.5 parts

50% ethanol by volume

4 parts

[0029] Make 1000 bags

[0030] Preparation process:

[0031] 1. Preparation of adhesive: Take the prescribed amount of honey, put it in an iron pot, add purified water with 2 times the weight of honey, stir evenly, heat to 100-105°C, keep warm for 20-25 minutes, take it out, and use 80 Filter through a mesh sieve, take t...

Embodiment 2

[0067] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0068] Element

Dosage

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

1 copy

Mannitol

1.7 servings

microcrystalline cellulose

1.3 parts

Sodium carboxymethyl cellulose

1.0 copies

lactose

0.9 parts

Magnesium stearate

0.13 parts

polyethylene glycol 4000

1.1 copies

hypromellose

1.3 parts

Low-substituted hydroxypropyl cellulose

0.9 parts

Polysorbate 80

0.08 parts

Honey

0.8 parts

70% volume fraction ethanol solution

7 copies

[0069] Make 1000 bags

[0070] Preparation process: prepared according to the preparation process of Example 1. Observing the granulation process of the product did not find the phenomenon of sticking to the screen, and the product was easy to granulate. Tested by the test method of Example 1, the disso...

Embodiment 3

[0072] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0073] Element

Dosage

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

1 copy

Mannitol

1.6 servings

microcrystalline cellulose

1.2 parts

Sodium carboxymethyl cellulose

0.9 parts

lactose

0.7 parts

Magnesium stearate

0.12 parts

polyethylene glycol 4000

0.9 parts

hypromellose

1.1 copies

Low-substituted hydroxypropyl cellulose

0.8 parts

Polysorbate 80

0.07 parts

Honey

0.7 parts

70% volume fraction ethanol solution

6 servings

[0074] Make 1000 bags

[0075] Preparation process: prepared according to the preparation process of Example 1. Observing the granulation process of the product did not find the phenomenon of sticking to the screen, and the product was easy to granulate. Tested by the test method of Example 1, the diss...

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PUM

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Abstract

An (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule is prepared from, by weight, 1 part of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, 1.3-1.8 parts of mannitol, 0.9-1.5 parts of microcrystalline cellulose, 0.6-1.2 parts of carboxymethylcellulose sodium, 0.5-1.1 parts of lactose, 0.08-0.15 part of magnesium stearate, 0.5-1.2 parts of polyethylene glycol 4000, 0.8-1.6 parts of hydroxypropyl methylcellulose, 0.5-1.0 part of low-substituted hydroxypropyl cellulose, 0.03-0.09 part of polysorbate 80, 0.3-0.9 part of honey and 2-8 parts of an ethanol solution with the volume fraction being 50-70%. The (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide prepared in the invention has the advantages of no adhesion to a screen and easy granulation during granulation, fast dissolution speed, short complete-dissolution time not exceeding 30 s, good stability during storage, no moisture absorbing caking, and long shelf life reaching up to 24 months.

Description

technical field [0001] The invention mainly relates to the field of pharmaceutical technology, in particular to (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules and a preparation method thereof. Background technique [0002] The chemical name of levo-oxiracetam is: S-(-)-4-hydroxy-2-oxopyrrolidine-N-acetamide. It is a white microcrystalline powder with a melting point of 135-136°C and an optical rotation of -36°( C=1.00inwater), the solubility of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide is obviously better than that of the racemate. The chemical structural formula is shown in the following formula: [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 CN 103735545A that (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetami...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/4015A61K47/38A61K47/10A61P25/00A61P25/28
CPCA61K9/5031A61K9/5047A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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