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Metformin compound pharmaceutical composition and preparation method thereof

A technology of metformin hydrochloride and a composition, applied in the field of pharmacy, can solve the problems of increased difficulty in industrialization of three-layer tablets, many control points, poor patient compliance, etc., achieves stable and controllable product quality, and solves poor compressibility and production costs. low effect

Inactive Publication Date: 2013-08-14
2Y CHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, there are major technical challenges in this compound preparation
[0006] First, due to the low solubility of repaglinide, the solubility in water is only 0.005mg / mL, and metformin hydrochloride is a water-soluble drug, it is difficult to ensure the synchronization of the drug release rate of the two by conventional technology, so it is difficult to Application in industrial production, solving the problem of synchronous and controlled release of insoluble drug repaglinide and water-soluble drug metformin hydrochloride has also become a hot spot in the industry
Second, in the marketed compound preparations, the content of repaglinide is only a few tenths of a milligram to a few milligrams, while metformin is usually several hundred milligrams. The weight ratio of the two active ingredients is very different, and it is easy to have uneven mixing.
Third, the crystal form of metformin hydrochloride is obvious, and its compressibility and plasticity are poor
The patent process is complex, with many control points, the difficulty of quality controllability increases, and the difficulty of industrialization of three-layer tablets increases
[0014] Therefore, there is an urgent need to find a method for the preparation of a compound preparation (pharmaceutical composition) that is simple in technology, does not require special auxiliary materials and special equipment, and solves the poor compressibility problem of metformin hydrochloride, so as to be suitable for industrial production under domestic conditions
And the compound preparation (pharmaceutical composition) prepared by this method can solve the problem of synchronous release and uniform content of the two active ingredients, and solve the problem of poor patient compliance caused by the large volume of the single-dose compound preparation

Method used

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  • Metformin compound pharmaceutical composition and preparation method thereof
  • Metformin compound pharmaceutical composition and preparation method thereof
  • Metformin compound pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Preparation of single-dose pharmaceutical composition of repaglinide 1.0 mg and metformin hydrochloride 500 mg

[0049] Prepare according to the ingredients and dosage of each step in the table below:

[0050]

[0051] Step 1: mix repaglinide, crospovidone, microcrystalline cellulose, sodium bicarbonate, povidone K29 / 32 and part of metformin hydrochloride (50.0 mg); add poloxa with a concentration of 12.5% Poloxamer solution (prepared by dissolving 0.5mg of poloxamer 188 in 3.5g of purified water), granulated, dried, and pulverized to obtain premixed powder I, wherein the drying temperature should not be higher than 60°C, and the moisture content of premixed powder I Content ≤ 5wt%.

[0052] Step 2: Mix the premixed powder Ⅰ with mannitol, crospovidone, povidone K29 / 32, and the remaining metformin hydrochloride (450.0 mg), add a wetting agent, purified water, granulate, and dry to obtain dry granules A, the moisture content of the dried particles A is ≤3wt%.

[00...

Embodiment 2

[0057] Preparation of single-dose pharmaceutical composition of repaglinide 2.0 mg and metformin hydrochloride 500 mg

[0058] Prepare according to the ingredients and dosage of each step in the table below:

[0059]

[0060]

[0061] Preparation method 1:

[0062] Step 1, mix repaglinide and meglumine evenly, then mix evenly with microcrystalline cellulose, crospovidone, povidone K29 / 32 and part of metformin hydrochloride (40.0 mg); use concentration of 8.9% The poloxamer solution (prepared by adding 0.5g of poloxamer 188 to 5.1g of 50% ethanol solution) was granulated, dried at 60°C until the moisture content was ≤3wt%, and pulverized to obtain premixed powder I.

[0063] Step 2. Mix the premixed powder I with the remaining metformin hydrochloride (460.0 mg), mannitol, crospovidone, and povidone K29 / 32 evenly, add purified water, granulate, dry, and granulate to obtain dry granules A (moisture content ≤ 3wt%).

[0064] Step 3. Add microcrystalline cellulose, crospov...

Embodiment 3

[0072] Preparation of single-dose pharmaceutical composition of repaglinide 2.0 mg and metformin hydrochloride 500 mg

[0073] Prepare according to the ingredients and dosage of each step in the table below:

[0074]

[0075]

[0076] Preparation:

[0077] Step 1, mix repaglinide and sodium bicarbonate evenly, then mix evenly with crospovidone, microcrystalline cellulose, povidone K25 and part of metformin hydrochloride (50.0mg); Dialkyl sodium sulfate solution (prepared by adding 0.5 mg sodium lauryl sulfate to 5.0 mg purified water) was granulated, dried at 60°C until the moisture content was ≤3%, and pulverized to obtain premix powder I.

[0078] Step 2. Mix the premixed powder I with mannitol, povidone K25, remaining metformin hydrochloride (450.0 mg) and cross-linked povidone evenly, add purified water, granulate, and obtain wet granules; take out the wet granules and dry until The moisture content of the granule is 1wt%-4wt%, and the dry granule A is obtained.

...

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Abstract

The invention provides a metformin compound pharmaceutical composition for treating type II diabetes and a preparation method thereof. The pharmaceutical composition contains a small dose of anti-diabetic medicine and a relatively large dose of metformin hydrochloride as active ingredients. The preparation method has a simple process, does not need special auxiliary materials, and is suitable for industrial production. Two active ingredients in the prepared pharmaceutical composition have the advantages of uniform content and good dissolubility.

Description

technical field [0001] The present invention relates to the field of pharmacy, specifically, the present invention relates to a metformin compound pharmaceutical composition for treating type II diabetes and a preparation method thereof, the pharmaceutical composition contains a small dose of antidiabetic drug and metformin hydrochloride, two The content of the active ingredient is uniform and the dissolution rate is good, and the preparation method has simple process and is suitable for industrialized production. Background technique [0002] Type II diabetes is non-insulin-dependent diabetes, which is a disease that seriously threatens human health. The complications of type II diabetes are diverse and complex, and the course of the disease often involves the kidneys and even life-threatening. [0003] Repaglinide (Repaglinide, ) is a benzoic acid derivative, which is a non-sulfonylurea short-acting insulin secretagogue. Metformin (Metformin, ) and salts thereof (for...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/28A61K9/48A61K31/155A61K31/451A61K31/4985A61P3/10
Inventor 何训贵徐丽霞葛双奇王元
Owner 2Y CHEM
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