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

A technology of pyrrolidine acetamide and sustained-release capsules is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. The problems of slow-release preparations cannot be achieved, and the preparation process is simple and feasible, the number of doses is reduced, and the granule fluidity is good.

Active Publication Date: 2018-10-23
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-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsules mainly have the disadvantages that the release degree cannot be well controlled, and the requirements for sustained-release preparations cannot be met, the particle fluidity is not good, and the filling process is difficult. There is a large difference in the filling volume, which affects the dosage of the drug, and the capsules are easy to stick and agglomerate during storage and other technical problems

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide slow-release capsules, prepared according to the following steps:

[0024]

[0025] Preparation process:

[0026] 1. Pretreatment of raw and auxiliary materials: take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, lactose, hydroxypropylmethylcellulose, carnauba wax, calcium hydrogen phosphate, and micronized silica gel Mix and pulverize into fine powder in the mixing pulverizer (the amount that can pass through No. 5 sieve and No. 6 sieve must not be less than 95% of the total amount), and sieve;

[0027] 2. Granulation: Add ethanol solution, 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 of the granules is ≤3%, and granulate (over 24 Mesh sieve), spare;

[0028] 3. Total blending: crush stearyl alcohol and magnesium stearate through a 100-mesh sieve, add to the granulated granules, and mix with ...

Embodiment 2

[0067] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide slow-release capsules, prepared according to the following steps:

[0068]

[0069]

[0070] Preparation process: prepared according to the preparation process of Example 1. Tested by the test method of Example 1, the angle of repose result shows that this product has good fluidity, and the angle of repose is less than 36 °, and the release measurement test result shows that (S)-4-hydroxyl-2 oxo-1-pyrrolidine acetamide Sustained-release capsules are released slowly, with a release time of up to 12 hours, which can meet the requirements of sustained-release preparations. The results of the stability test show that the sample quality is stable in six months of acceleration, and no capsule adhesion occurs. The quality is stable for a long period of 24 months, and no capsules Adhesion phenomenon, so this product is valid for at least 24 months.

Embodiment 3

[0072] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide slow-release capsules, prepared according to the following steps:

[0073]

[0074] Preparation process: prepared according to the preparation process of Example 1. Tested by the test method of Example 1, the angle of repose result shows that this product has good fluidity, and the angle of repose is less than 37 °, and the release measurement test result shows that (S)-4-hydroxyl-2 oxo-1-pyrrolidine acetamide Sustained-release capsules are released slowly, with a release time of up to 12 hours, which can meet the requirements of sustained-release preparations. The results of the stability test show that the sample quality is stable in six months of acceleration, and no capsule adhesion occurs. The quality is stable for a long period of 24 months, and no capsules Adhesion phenomenon, so this product is valid for at least 24 days.

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Abstract

The invention discloses a sustained-release capsule with (S)-4-hydroxyl-2-oxo-1-pyrrolidine acetamide. The sustained-release capsule is prepared by the following raw materials and auxiliary materials in parts by weight: 1 part of (S)-4-hydroxyl-2-oxo-1-pyrrolidine acetamide, 1.1-1.6 parts of lactose, 1.8-2.5 parts of hydroxypropyl methyl cellulose K4M, 0.7-1.1 parts of carnauba wax, 0.03-0.07 part of stearyl alcohol, 0.02-0.08 part of magnesium stearate, 0.5-1.1 parts of calcium hydrophosphate, 1.0-1.7 parts of micro-powder silica gel and 3.2-4.7 parts of alcohol solution with the concentration of 50%-70%. The sustained-release capsule disclosed by the invention has the advantages that the particle fluidity is good, the repose angles of the particles are less than 37 degrees, the release speed is slow, and the release period is 12 hours, therefore, compared with the traditional preparation, the taking times can be reduced and the sustained-release capsule only needs to be taken once a day; simultaneously, the stability is good, the capsule cannot be adhered in the storage process, and the shelf life can reach 24 months.

Description

technical field [0001] The invention mainly relates to the technical field of pharmacy, in particular to a (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide sustained-release capsule and a preparation method thereof. Background technique [0002] The chemical name of levo-oxiracetam is: S-(-)-4-hydroxy-2-oxopyrrolidine-N-acetamide. It is a white microcrystalline powder with a melting point of 135-136°C and an optical rotation of -36°( C=1.00in water), the solubility of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide is obviously better than that of the racemate. The chemical structural formula is shown in the figure below: [0003] [0004] 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 China, and the main active ingredients used are racemates. Ye Lei et al mentioned in the patent of CN 103735545 A that (S)-4-hydroxyl-2-oxo-1-pyrroli...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/4015A61K47/38A61K47/26A61K47/32A61K47/10A61K47/36A61P25/28
CPCA61K9/0002A61K9/1623A61K9/1635A61K9/1641A61K9/1652A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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