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Stable method for preparing repaglinide compressed tablets

A stabilizer and mixing technology, applied in the field of preparation of repaglinide ordinary tablets, can solve the problems of difficult temperature control, increase of related substances, difference in content between particles and the like

Inactive Publication Date: 2012-02-22
SUZHOU CHUNGHWA CHEM & PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the two preparation methods can make repaglinide dissolve and take effect in 15 minutes, the common wet granulation process takes a long time to dry, the temperature is not easy to control, and the uneven size distribution of the particles is likely to cause content differences between particles, content decline and related problems. The problem of the increase of substances, and the ordinary direct mixing and tableting process is likely to cause uneven mixing of the main drug, affecting its content uniformity
[0006] Chinese patent CN101822672 discloses a compound preparation containing metformin and repaglinide and its preparation method and application. It exemplifies the preparation method of dispersible tablets and orally disintegrating tablets. The drug and pharmaceutical excipients are mixed in equal increments After uniformity, add a binder to make granules, which is a common wet granulation method, and has the same problems as the above-mentioned patents, such as decreased content, increased related substances, etc.

Method used

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  • Stable method for preparing repaglinide compressed tablets
  • Stable method for preparing repaglinide compressed tablets
  • Stable method for preparing repaglinide compressed tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 1mg Repaglinide Ordinary Tablets

[0024]

[0025] Preparation:

[0026] Example 1: Povidone K30, meglumine, and poloxamer were dissolved in 70ml of purified water, repaglinide was dissolved in 50ml of ethanol, and repaglinide ethanol solution was added to the pure aqueous solution to dissolve completely. Using lactose and calcium hydrogen phosphate as fillers, the fluidized bed top spray granulation, the particle size is over 40 mesh. The granules are added with croscarmellose sodium and magnesium stearate, mixed evenly, and compressed into tablets.

Embodiment 2

[0037] 0.5mg Repaglinide Ordinary Tablets

[0038]

[0039] Preparation:

[0040] Example 2: Dissolve hydroxypropyl cellulose, meglumine, and sodium lauryl sulfate in 70ml of purified water, dissolve repaglinide in 50ml of ethanol, add repaglinide ethanol solution to the above-mentioned pure aqueous solution Dissolve completely. Using mannitol and calcium hydrogen phosphate as fillers, fluidized bed top spray granulation, the particle size is over 40 mesh. The granules are added with croscarmellose sodium and magnesium stearate, mixed evenly, and compressed into tablets.

Embodiment 3

[0050] After 1.0 mg and 0.5 mg of repaglinide tablets of Examples 1 and 2 and Comparative Examples 1 and 2 were placed under certain conditions for 10 days, HPLC was used to analyze the content of repaglinide and related substances.

[0051] 1) High temperature test

[0052] The test sample was placed in a suitable clean container with the open top open, and placed at a temperature of 60° C. for 10 days, and the content of repaglinide in the test sample was detected. The results are shown in Table 5.

[0053] Table 5 High temperature (60°C) comparative test results

[0054]

[0055]

[0056] 2) High humidity test

[0057] Put the test product in a closed container with constant humidity, and place it at 25°C and 75.0% relative humidity for 10 days.

[0058] Detect the content and related substances of repaglinide in the test product, and the results are shown in Table 6.

[0059] Table 6 High humidity (RH75.0%) comparative test results

[0060]

[0061] It can be kn...

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Abstract

The invention relates to the field of medicine medicinal preparation, in particular to a stable method for preparing repaglinide compressed tablets, which is characterized in that the pelletizing process includes the following steps: adding repaglinide into adhesive solution and making the pellets with fillers through a fluidized bed in ejecting mode. Particles of the repaglinide tablets can rapidly disperse when the epaglinide tablets disintegrate, and active ingredient repaglinide evenly dispersed in the particles can rapidly dissolve out. The prepared repaglinide particles can be evenly mixed with auxiliary materials such as disintegrating agents, lubricating agents and the like and pressed into tablets. Tablet cores can completely disintegrate within two minutes.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a method for preparing stable repaglinide ordinary tablets. Background technique [0002] Repaglinide: English name Repaglinide, chemical name (S)-2-ethoxy-4-[2-[[3-methyl-1-[2-(1-piperidine)phenyl]butyl ]amino]-2-oxoethyl]benzoic acid. [0003] Repaglinide is white or off-white crystalline powder; odorless. Soluble in chloroform, slightly soluble in ethanol or acetone, almost insoluble in water, slightly soluble in 0.1mol / L hydrochloric acid solution. It is unstable in aqueous solution and unstable to strong alkali, so it should be stored at low temperature and protected from light. [0004] Repaglinide is a non-sulfonylurea insulin-stimulating agent. This product binds to specific receptors on the islet β-cell membrane, closes the ATP-sensitive potassium channel, inhibits the outflow of potassium ions, and causes cell membrane depolarization, resulting in Extracel...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/451A61P3/10
Inventor 李远福陈娟顾川江
Owner SUZHOU CHUNGHWA CHEM & PHARMA IND
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