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(S)-4-hydroxy-2oxo-1-pyrrolidine acetamide sustained-release capsule with good stability and preparation method of sustained-release capsule

A technology of pyrrolidine acetamide and sustained-release capsules, which is applied in the directions of inactive medical preparations, pharmaceutical formulations, oil/fat/wax inactive ingredients, etc., can solve the problem of poor particle fluidity and large differences in loading , many granule powder layers and other problems, to achieve the effect of simple and feasible preparation process, reducing the number of doses, and good granule fluidity

Inactive Publication Date: 2018-02-06
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 drug. After the granulation, there are more granule powder layers, the yield of the finished product is low, and there are technical problems such as a large increase in the relevant substances during the storage process.

Method used

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  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide sustained-release capsule with good stability and preparation method of sustained-release capsule
  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide sustained-release capsule with good stability and preparation method of sustained-release capsule
  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide sustained-release capsule with good stability and preparation method of sustained-release capsule

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]

[0024] Preparation process:

[0025] 1. Pretreatment of raw and auxiliary materials: take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, lactose, hydroxypropylmethylcellulose K4M, carnauba wax, and sodium thiosulfate and mix them Mix and pulverize into fine powder in the pulverizer (the amount that passes through No. 5 sieve and can pass through No. 6 sieve must not be less than 95% of the total amount), and sieves;

[0026] 2. Granulation: Add povidone K30 ethanol solution, mix and granulate with 18-mesh sieve, place the prepared wet granules in a hot air oven, set the temperature at 40-60°C, and dry until the moisture content of the granules is ≤3%. Granules (through a 24-mesh sieve), set aside;

[0027] 3. Total blending: crush stearyl alcohol and magnesium stearate through a 100-mesh sieve, add to the granulated...

Embodiment 2

[0071] A stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide slow-release capsule is prepared according to the following steps:

[0072]

[0073] Preparation process: prepared according to the preparation process of Example 1. Test by the test method of Example 1, the yield test result shows that this product yield is up to more than 93%, the angle of repose result shows that this product has good fluidity, and the repose angle is less than 38 °, and the release measurement test result shows that (S)- 4-Hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsules are slow-release, and the release time is as long as 12 hours, which can meet the requirements of sustained-release preparations. The results of the stability test show that the quality of the sample is stable and the impurities increase in June. The content is only 0.06%, the quality is stable for 24 months in a long-term, and the impurity increment is only 0.05%, so the validity period of this product is at leas...

Embodiment 3

[0075] A stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide slow-release capsule is prepared according to the following steps:

[0076]

[0077] Preparation process: prepared according to the preparation process of Example 1. Test by the test method of Example 1, the yield test result shows that this product yield is up to more than 95%, the angle of repose result shows that this product has good fluidity, and the repose angle is less than 35 °, and the release measurement test result shows that (S)- 4-Hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsules are slow-release, and the release time is as long as 12 hours, which can meet the requirements of sustained-release preparations. The results of the stability test show that the quality of the sample is stable and the impurities increase in June. The amount of impurities is only 0.05%, the quality is stable for 24 months in a long-term, and the increase of impurities is only 0.06%, so the validity period of this p...

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Abstract

The invention provides a (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide sustained-release capsule with good stability. The sustained-release capsule is prepared from raw and auxiliary materials as follows: 1 part of (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide, 0.5-1.1 parts of lactose, 1.5-2.1 parts of hydroxypropyl methyl celluloseK4M, 0.8-1.3 parts of carnauba wax, 0.03-0.08 parts of stearyl alcohol,0.11-0.16 parts of magnesium stearate, 0.05-0.09 parts of sodium thiosulfate and 2.5-3.3 parts of a povidone K30 ethanol solution with mass fraction being 7%-10%. According to the (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide sustained-release capsule with good stability, particle fluidity is good, repose angle of particles is smaller than 37 degrees, few powder layers are produced after particle granulation, the finished product yield is as high as 92.6%, release speed is low, release period is as long as 12 h, meanwhile, the product is good in stability, related substances are only increased by 0.05% in the shelf life, and shelf life is as long as 24 months.

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 Applications(China)
IPC IPC(8): A61K9/52A61K31/4015A61K47/44A61K47/38A61K47/32A61K47/26A61K47/10A61P25/28A61P25/00
CPCA61K9/0002A61K9/1617A61K9/1623A61K9/1635A61K9/1652A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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