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(S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide particles having uniform content, and preparation method thereof

A technology of pyrrolidine acetamide and hydroxyl group, which is applied in the field of -4-hydroxy-2 oxo-1-pyrrolidine acetamide particles and their preparation, and can solve the problems of poor stability during storage, slow particle dissolution and particle size. The problem of strong hygroscopicity, etc., can achieve the effect of simple and feasible preparation process, fast dissolution speed and good content uniformity.

Inactive Publication Date: 2017-05-10
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Existing (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide granules mainly exist in the preparation process with many granule powder layers, difficult to control particle size, poor content uniformity, poor stability during storage, and granules Strong hygroscopicity, easy to stick and agglomerate, short shelf life, slow particle dissolution and other technical problems

Method used

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  • (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide particles having uniform content, and preparation method thereof
  • (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide particles having uniform content, and preparation method thereof
  • (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide particles having uniform content, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is prepared according to the following steps:

[0027] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy Mannitol 0.6 parts microcrystalline cellulose 1.3 parts Sodium carboxymethyl cellulose 0.9 parts lactose 0.8 parts talcum powder 0.13 parts polyethylene glycol 4000 1.2 parts hypromellose 0.7 parts Low-substituted hydroxypropyl cellulose 1.2 parts Polysorbate 80 0.09 parts Sorbitol 2 copies Starch slurry with a mass fraction of 6% 9 servings 20% ethanol solution by volume fraction 3 copies

[0028] Make 1000 bags

[0029] Preparation process:

[0030] 1. Pre-treatment of raw and auxiliary materials: take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide and dissolve it in the prescribed amount of ethanol solution, and set aside; additionally take th...

Embodiment 2

[0085] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is prepared according to the following steps:

[0086] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy Mannitol 0.8 parts microcrystalline cellulose 1.6 servings Sodium carboxymethyl cellulose 1.2 parts lactose 1.0 copies talcum powder 0.16 parts polyethylene glycol 4000 1.4 parts hypromellose 0.9 parts Low-substituted hydroxypropyl cellulose 1.4 parts Polysorbate 80 0.12 parts Sorbitol 4 parts Starch slurry with a mass fraction of 8% 12 copies 30% ethanol solution by volume fraction 5 copies

[0087] Make 1000 bags

[0088] Preparation process: prepared according to the preparation process of Example 1. According to the test method of embodiment 1, carry out particle Hughes angle measurement, content uniformity measurement, load difference inspection, sample stabilit...

Embodiment 3

[0090] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granule with uniform content is prepared according to the following steps:

[0091] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy Mannitol 0.7 parts microcrystalline cellulose 1.5 servings Sodium carboxymethyl cellulose 1.9 servings lactose 0.9 parts talcum powder 0.15 parts polyethylene glycol 4000 1.3 parts hypromellose 0.8 parts Low-substituted hydroxypropyl cellulose 1.3 parts Polysorbate 80 0.10 parts Sorbitol 3 copies Starch slurry with a mass fraction of 8% 11 copies 20% ethanol solution by volume fraction 4 parts

[0092]Make 1000 bags

[0093] Preparation process: prepared according to the preparation process of Example 1. According to the test method of embodiment 1, carry out particle Hughes angle measurement, content uniformity measurement, load difference inspection, sample stabili...

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Abstract

The invention relates to (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide particles having uniform content, wherein the particles are prepared from the following raw materials by weight: 1 part of (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide, 0.5-0.9 part of mannitol, 1.2-1.7 parts of microcrystalline cellulose, 0.8-1.3 parts of sodium carboxymethyl cellulose, 0.6-1.0 part of lactose, 0.12-0.16 part of talc powder, 0.9-1.5 parts of polyethylene glycol 4000, 0.5-0.9 part of hydroxypropyl methyl cellulose, 0.9-1.5 parts of low substituted hydroxypropyl cellulose, 0.08-0.13 part of polysorbate 80, 1-5 parts of sorbitol, 8-13 parts of starch slurry with a mass fraction of 6-8%, and 3-5 parts of an ethanol solution with a volume fraction of 20-30%. According to the present invention, the (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide particles prepared according to the preparation method have the following characteristics that the powder layer amount is less, the repose angle is less than 38 DEG, the content uniformity is less than 4%, the particle dissolving and scattering is fast, the whole dissolving and scattering time of the particles is less than 30 s, the content uniformity is good, the RSD determined at multiple points is less than 2%, the storage process has good stability, and the preparation process is simple and feasible, and is worthy of marketing.

Description

technical field [0001] The invention mainly relates to the technical field of pharmacy, in particular to (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide particles with uniform content and a preparation method thereof. Background technique [0002] Oxiracetam was launched in Italy in 1987 in the form of tablet, 800mg; capsule, 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 publication number CN 103599101 A that levoxiracetam can significantly improve the learning, memory and c...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4015A61K47/38A61K47/34A61K47/26A61K47/10A61K47/04A61P9/10A61P25/00A61P25/28A61P35/00
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD