(S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets having good stability and preparation method of effervescent tablets

A technology of pyrrolidine acetamide and stability, which is applied in the field of -4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablet and its preparation, and can solve the problem that the particle size is not easy to control, the particle is not easy to form, and the particle powder is not easy to control. Problems such as multiple layers, etc., to achieve the effect of simple and feasible preparation process, not easy to absorb moisture and deteriorate, and good particle formability

Active Publication Date: 2017-06-27
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-hydroxyl-2-oxo-1-pyrrolidineacetamide effervescent preparation mainly has the following problems: the granules are not easy to form in the granulation process, the granule powder layer is more, the particle size is not easy to control, and the tableting process is easy to stick and punch. The finished product has slow gas production and disintegration, and the product is easy to absorb moisture and deteriorate during storage, resulting in poor stability and short shelf life.

Method used

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  • (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets having good stability and preparation method of effervescent tablets
  • (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets having good stability and preparation method of effervescent tablets
  • (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets having good stability and preparation method of effervescent tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide effervescent tablet is prepared according to the following steps:

[0025] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy tartaric acid 5 copies sodium bicarbonate 5 copies Sodium chloride 0.5 parts polyethylene glycol 6000 0.75 parts dextrin 5 copies sucrose 5 copies 8% mass fraction of PVP / VA64 ethanol solution 17 copies Sodium carboxymethyl cellulose 5 copies microcrystalline cellulose 8 servings

[0026] Made into 1000 pieces

[0027] Preparation process:

[0028]1. Take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, tartaric acid, dextrin, sucrose, sodium carboxymethyl cellulose, microcrystalline cellulose and mix them in a universal pulverizer During, pulverize, collect the mixed powder after passing through a 100-mesh sieve, put the mixed powder in a wet granulator, add a binder, start t...

Embodiment 2

[0072] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide effervescent tablet is prepared according to the following steps:

[0073] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy tartaric acid 7 copies sodium bicarbonate 7 copies Sodium chloride 0.8 parts polyethylene glycol 6000 1.2 parts dextrin 8 servings sucrose 7 copies 12% mass fraction of PVP / VA64 ethanol solution 23 copies Sodium carboxymethyl cellulose 8 servings microcrystalline cellulose 11 copies

[0074] Made into 1000 pieces

[0075] Preparation process: prepared according to the preparation process of Example 1. According to the test method of Example 1, the measurement of the particle size of the preparation process, the measurement of the moisture absorption and weight gain of the finished product, the inspection of the disintegration time limit and the stability test of the sample were carried out respect...

Embodiment 3

[0077] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide effervescent tablet is prepared according to the following steps:

[0078] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy tartaric acid 6 servings sodium bicarbonate 6 servings Sodium chloride 0.7 parts polyethylene glycol 6000 1.05 parts dextrin 6 servings sucrose 6 servings 12% mass fraction of PVP / VA64 ethanol solution 21 copies Sodium carboxymethyl cellulose 7 copies microcrystalline cellulose 10 copies

[0079] Made into 1000 pieces

[0080] Preparation process: prepared according to the preparation process of Example 1. According to the test method of Example 1, the measurement of the particle size of the preparation process, the measurement of the moisture absorption and weight gain of the finished product, the inspection of the disintegration time limit and the stability test of the sample were carried out re...

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Abstract

(S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets having good stability are made from the following raw and auxiliary materials, according to a weight ratio, 1 part of (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide, 4-9 parts of tartaric acid, 4-9 parts of sodium bicarbonate, 0.3-0.9 part of sodium chloride, 0.45-1.35 parts of polyethylene glycol 6000, 2-9 parts of dextrin, 3-8 parts of sucrose, 15-25 parts of a PVP/VA64 ethanol solution with the mass percentage being 8-16%, 3-9 parts of sodium carboxymethylcellulose, and 7-12 parts of microcrystalline cellulose. During preparation, the prepared (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide effervescent tablets are good in particle formability and less in powder layer amount, and have less than 4% by weight of particles that don't conform to the standard of particle granularity detection. The effervescent tablet product is fast in gas generation and disintegration speed, and has the disintegration time no more than 30 s. The effervescent tablet product is not prone to absorb moisture and go bad and is easy to store and long in shelf life. The preparation method is simple and feasible and is worth market popularization.

Description

technical field [0001] The invention mainly relates to the field of pharmaceutical technology, in particular to a stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide effervescent tablet and a preparation method thereof. Background technique [0002] Nootropic drug, also known as brain activator, is a new type of central nervous system drug that promotes learning and enhances memory. Nootropic drugs are required to selectively act on the cerebral cortex, and have the characteristics of selectively activating, protecting and promoting the recovery of damaged nerve cell functions. The difference from other neurological drugs is that their above-mentioned effects do not pass through the reticular system or the olfactory bulb, but directly act on the cortex. It neither affects behavior nor has sedative and exciting effects, so this class of drugs has attracted widespread attention and interest, and the demand for this class of drugs is also increasing day by day. [0003] Oxirace...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/46A61K31/4015A61K47/38A61P25/28A61P25/00A61P35/00
CPCA61K9/0007A61K9/2059A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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