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A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsule and its preparation method

A technology of pyrrolidine acetamide and sustained-release capsules, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, etc. The problems such as large difference in quantity can be achieved, and the effect of simple and feasible preparation process, good particle fluidity, and reduction of the number of doses can be achieved.

Active Publication Date: 2020-08-11
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsules mainly have the problems that the release rate cannot be well controlled, and the requirements for sustained-release preparations cannot be met, the fluidity of the particles is not good, and the filling process is difficult. There are large differences in the filling volume, which affects the dosage of the medicine. After the granulation, the granule powder layer is more, and the yield of the finished product is low. Technical problems such as

Method used

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  • A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsule and its preparation method
  • A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsule and its preparation method
  • A stable (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsule and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide slow-release capsule is prepared according to the following steps:

[0023] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy lactose 0.8 parts Hypromellose K4M 1.5 servings carnauba wax 0.7 parts stearyl alcohol 0.06 parts Magnesium stearate 0.06 parts 8% povidone K30 ethanol solution 1.9 servings

[0024] Make 1000 capsules

[0025] Preparation process:

[0026] 1. Pretreatment of raw and auxiliary materials: Take the main drug, slow-release matrix material and blocker in the prescription amount, mix and grind them into fine powder (the amount that can pass through the No. 5 sieve and the No. 6 sieve must not be less than the total 95% of the amount), sieved;

[0027] 2. Granulation: Add binder, mix and granulate with 18-mesh sieve, place the wet granules in a hot air oven, set the temperature at 40-60°C, dry until the moisture content o...

Embodiment 2

[0073] A stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide slow-release capsule is prepared according to the following steps:

[0074] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy lactose 1.1 copies Carboxypropylmethylcellulose K4M 1.9 servings carnauba wax 0.9 parts stearyl alcohol 0.08 parts Magnesium stearate 0.09 parts 8%~9% povidone K30 ethanol solution 2.1 parts

[0075] Make 1000 capsules

[0076] Preparation process: prepared according to the preparation process of Example 1. According to the test method of Example 1, the yield measurement, angle of repose measurement, release measurement and sample stability test were carried out respectively. The yield test results showed that the yield of this product was as high as more than 94%, and the angle of repose result showed that this product has good fluidity , the angle of repose is less than 38°, and the release test results show that (...

Embodiment 3

[0078] A stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide slow-release capsule is prepared according to the following steps:

[0079] Element Dosage (S)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide 1 copy lactose 1.0 copies Carboxypropylmethylcellulose K4M 1.7 servings carnauba wax 0.8 parts stearyl alcohol 0.07 copies Magnesium stearate 0.08 parts 9% ethanol solution of povidone K30 2.0 copies

[0080] Make 1000 capsules

[0081] Preparation process: prepared according to the preparation process of Example 1. According to the test method of Example 1, the yield measurement, angle of repose measurement, release measurement and sample stability test were carried out respectively. The yield test results showed that the yield of this product was as high as more than 95%, and the angle of repose result showed that this product has good fluidity , the angle of repose is less than 37°, and the release test results show that...

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Abstract

The invention provides an (S)-4-hydroxy-dioxo-1-pyrrolidine acetamide sustained-release capsule with good stability. The (S)-4-hydroxy-dioxo-1-pyrrolidine acetamide sustained-release capsule is characterized by being prepared from the following raw materials and auxiliary materials in parts by weight: 1 part of (S)-4-hydroxy-dioxo-1-pyrrolidine acetamide, 0.7-1.2 parts of lactose, 1.2-2.5 parts of hydroxypropyl methyl cellulose K4M, 0.6-1.0 part of carnauba wax, 0.05-0.09 part of stearyl alcohol, 0.05-0.10 part of magnesium stearate, and 1.8-2.2 parts of povidone K30 ethanol solution with the mass fraction being 7%-10%. The sustained-release capsule prepared by the method provided by the invention has good particle mobility, the repose angle of the particles is smaller than 38 degrees, the layering seldom occurs after size stabilization of the particles, the yield of the finished product is 94% or above, the release rate is low, and the release period is 12h; meanwhile, the product is good in stability, the shelf life is 24 months, the preparation process is simple and feasible, and product is suitable for market promotion.

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 sustained-release capsule and a preparation method thereof. Background technique [0002] Oxiracetam (S-oxiracetam) is a synthetic cyclic derivative of hydroxyaminobutyric acid (BABOB), which is only used in the central nervous system, mainly distributed in the cerebral cortex and hippocampus, and has the function of activating, protecting or promoting nerve cells. Functional recovery can improve the memory and learning functions of patients with mental retardation, and the drug itself has no direct vasoactive or central excitatory effect, and its effect on learning and memory is a lasting promotion effect. [0003] 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 Chi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/4015A61K47/38A61K47/32A61K47/36A61K47/34A61K47/26A61P25/28
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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