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Composition containing repaglinide and metformin hydrochloride and preparation thereof

A technology for metformin hydrochloride and a composition, applied in the field of medicine, can solve the problems of difficult control of repaglinide content uniformity, poor compressibility and plasticity, poor water solubility of repaglinide, etc. High degree and good stability

Active Publication Date: 2012-01-18
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the development of compound preparations of repaglinide and metformin hydrochloride, both repaglinide and metformin hydrochloride are immediate-release ingredients, and the ratio of the two main ingredients is very different. The content uniformity of repaglinide is difficult to control
The mixing process generally adopts the equal amount incremental method, but its operation is cumbersome, the production efficiency is low, and it is difficult to achieve satisfactory results
Repaglinide has extremely poor water solubility and is generally dissolved in organic solvents. This process is prone to organic solvent residues and safety issues
The dosage of metformin hydrochloride in the compound is 500mg. In order to control the size of the tablet and increase the compliance of patients, the dosage of excipients should be reduced as much as possible. On the other hand, metformin hydrochloride has poor compressibility and plasticity

Method used

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  • Composition containing repaglinide and metformin hydrochloride and preparation thereof
  • Composition containing repaglinide and metformin hydrochloride and preparation thereof
  • Composition containing repaglinide and metformin hydrochloride and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]

[0038] Preparation Process:

[0039] A. The raw and auxiliary materials except repaglinide and meglumine are screened separately and set aside;

[0040] B. Weigh the repaglinide and meglumine of the prescribed amount, add hot water, stir and dissolve until clear; add povidone K-30 (preparation solution) to the above solution to dissolve, add hot water, and make the concentration of 5% (g / g) povidone K-30 aqueous solution; the temperature of the aqueous solution is 50°C;

[0041] C. Weigh the prescribed amount of metformin hydrochloride, microcrystalline cellulose, povidone k-30 (internal addition) and cross-linked povidone (internal addition) and place them in a rapid granulator, mix well, and add the solution in step B to wet French granulation;

[0042] D. Drying and sizing: Take out the wet granules in step C, dry at about 50°C until the moisture content of the granules is <5%, and sizing;

[0043] E. External addition and total blending: add the granules in ...

Embodiment 2

[0046]

[0047] Preparation Process:

[0048] A. The raw and auxiliary materials except repaglinide and meglumine are screened separately and set aside;

[0049] B. Weigh the repaglinide and meglumine of the prescribed amount, add hot water, stir and dissolve until clear; add povidone K-30 (preparation solution) to the above solution to dissolve, add hot water, and make the concentration of 5% (g / g) povidone K-30 aqueous solution; the temperature of the aqueous solution is 65°C;

[0050] C. Weigh the prescribed amount of metformin hydrochloride, microcrystalline cellulose, povidone k-30 (internal addition) and cross-linked povidone (internal addition) and place them in a rapid granulator, mix well, and add the solution in step B to wet French granulation;

[0051] D. Drying and sizing: Take out the wet granules in step C, dry at about 50°C until the moisture content of the granules is <5%, and sizing;

[0052] E. External addition and total blending: add the granules in st...

Embodiment 3

[0055]

[0056] Preparation Process:

[0057] A. The raw and auxiliary materials except repaglinide and meglumine are screened separately and set aside;

[0058] B. Weigh the repaglinide and meglumine of the prescribed amount, add hot water, stir and dissolve until clear; add povidone K-30 (preparation solution) to the above solution to dissolve, add hot water, and make the concentration of 5% (g / g) povidone K-30 aqueous solution; the temperature of the aqueous solution is 70°C;

[0059] C. Weigh the prescribed amount of metformin hydrochloride, microcrystalline cellulose, povidone k-30 (internal addition) and cross-linked povidone (internal addition) and place them in a rapid granulator, mix well, and add the solution in step B to wet French granulation;

[0060] D. Drying and sizing: Take out the wet granules in step C, dry at about 50°C until the moisture content of the granules is <5%, and sizing;

[0061] E. External addition and total mixing: add the granules in st...

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PUM

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Abstract

The invention relates to a composition containing repaglinide and metformin hydrochloride and a preparation method thereof, belonging to the technical field of medicines. The composition containing repaglinide and metformin hydrochloride consists of repaglinide, metformin hydrochloride, a filling agent, a disintegrating agent, a bonding agent, a latent solvent and a lubricant, wherein the repaglinide is added into the metformin hydrochloride and auxiliary materials in the form of aqueous solution for wet granulation. The preparation method has the advantages of simple and efficient process, small using quantity of auxiliary materials, capability of solving the problem of poor content uniformity caused by small using amount of the repaglinide and increase in the dissolution rate; and moreover, a preparation has a smaller unit quantity and can be applied to industrial mass production.

Description

technical field [0001] The invention mainly relates to a composition containing repaglinide and metformin hydrochloride and a preparation method thereof, belonging to the technical field of medicine. [0002] Background technique [0003] Repaglinide hypoglycemic agents are insulin secretagogues, which have a good effect on regulating postprandial blood glucose, so they are also called "postprandial blood glucose regulators". The probability of hypoglycemia is less than that of sulfonylureas. It is characterized by fast drug metabolism, so diabetic patients with mild liver damage and kidney damage can also take it. Metformin hydrochloride is an oral antihyperglycemic drug that is still commonly used in developed countries in the world. It is also the drug of choice for patients with type 2 diabetes, especially obese patients. Metformin inhibits the liver from producing glucose and increases the sensitivity of peripheral tissues to insulin. , Increase insulin-mediated gluco...

Claims

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Application Information

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IPC IPC(8): A61K31/451A61K31/155A61K9/20A61K9/48A61P3/10A61P3/04
Inventor 卢良华
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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