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(S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof

A pyrrolidineacetamide and stability technology, applied in the field of 4-hydroxy-2-oxo-1-pyrrolidineacetamide granules and its preparation, can solve the problems of difficult particle size control, easy adhesion and caking, and short shelf life and other problems, to achieve the effect of simple and feasible preparation process, not easy to absorb moisture and agglomerate, and the amount of particle powder layer is small

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

[0003] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules mainly have a large increase in impurities during the preparation process, more granule powder layers, difficult control of particle size, poor stability during storage, and granule moisture absorption. Strong resistance, easy to stick and agglomerate, short shelf life, poor grain taste, difficult to be accepted by patients and other technical problems

Method used

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  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof
  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof
  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0025]

[0026] Preparation process:

[0027] 1. Pretreatment of raw and auxiliary materials: take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, L-cysteine, mannitol, microcrystalline cellulose, carboxymethyl cellulose Sodium, lactose, sucrose, and ethyl maltol are placed in a universal grinder, crushed through a 100-mesh sieve, and set aside;

[0028]2. Granulation: Take the mixed powder obtained after pretreatment, put it in a wet granulator, add starch slurry, start the granulator (install 18-mesh nylon sieve), and start granulation;

[0029] 3. Drying: Put the wet granules into the fluidized bed, set the temperature of the hot bed at 50°C to 70°C, and start drying; observe the boiling and blasting conditions of the granules at any time to prevent the granules from sticking to the bottom of the pot, causing coking or gelatinization o...

Embodiment 2

[0081] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide granule is prepared according to the following steps:

[0082]

[0083] Preparation process: prepared according to the preparation process of Example 1. Carry out the test by the test method of embodiment 1, the Hughes angle test measurement result shows that this product granule fluidity is good, and the Hughes angle is lower than 36 °, and the loading difference test shows that the loading difference of this product is less than ± 4%. The amount is stable and controllable, and the test results of the influence of product prescription on the increase of impurities in the preparation process show that the increase of impurities in the preparation process of this product is small, and the related substances in the preparation process only increase by 0.04%. The quality is stable for a long period of 24 months, so the validity period of this product is at least 24 months. The taste survey shows that this product tast...

Embodiment 3

[0085] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0086]

[0087] Preparation process: prepared according to the preparation process of Example 1. Carry out the test by the test method of embodiment 1, the Hughes angle test measurement result shows that this product granule fluidity is good, and the Hughes angle is lower than 35 °, and the loading difference test shows that the loading difference of this product is less than ± 5%. The amount is stable and controllable, and the test results of the influence of product prescription on the increase of impurities in the preparation process show that the increase of impurities in the preparation process of this product is small, and the related substances in the preparation process only increase by 0.02%. The quality is stable for a long period of 24 months, so the validity period of this product is at least 24 months. The taste survey shows that this product tast...

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Abstract

The invention relates to a (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle. The particle is prepared from the following materials: 1 part of (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide, 0.6-1.2 parts of L-cysteine, 1.0-1.6 parts of mannitol, 1.2-1.7 parts of microcrystalline cellulose, 0.6-1.2 parts of sodium carboxymethyl cellulose, 0.7-1.3 parts of lactose, 0.11-0.17 part of talcum powder, 1.1-1.6 parts of polyethylene glycol 4000, 1.0-1.7 parts of hydroxypropyl methylcellulose, 1-5 parts of sucrose, 0.4-0.9 part of ethylmaltol, and 9-15 parts of 6%-8% starch slurry. The particle prepared according to the invention has impurity increase of only 0.04% in the preparation process, low powder layer content, uniform particle size, good fluidity, a repose angle of less than 38 degrees, a load difference of less than 5%, good storage process stability, difficult moisture absorption and caking, a shelf life up to 24 months, and good taste, and can be accepted by most patients.

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 granule and a preparation method thereof. Background technique [0002] Oxiracetam (S-oxiracetam) is a synthetic hydroxyaminobutyric acid (BABOB) cyclic derivative. The drug was launched in Italy in 1987. 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 alcoholism, while dextro-oxiracetam has basically no effect. The wake-up effect is twice that of racemic oxiracetam; levo-oxiracetam has significant awakening effects on trauma and coma induced by anesthesia. Zhang Feng et al disclosed in the patent with the publicatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4015A61K47/38A61K47/10A61K47/34A61P25/00
CPCA61K9/5031A61K9/5042A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD