Preparing process for vildagliptin/metformin hydrochloride compound preparation

A kind of technology of metformin hydrochloride and compound preparation, applied in the field of medicine

Active Publication Date: 2014-04-23
NANJING HUAWE MEDICINE TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The inventors have found that the conventional wet granulation and compressed block methods are difficult to solve the above problems by studying the compound preparation of vildagliptin and metformin hydrochloride
And there is no literature report on the specific process of using spray drying to granulate the vildagliptin / metformin hydrochloride compound preparation

Method used

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  • Preparing process for vildagliptin/metformin hydrochloride compound preparation
  • Preparing process for vildagliptin/metformin hydrochloride compound preparation
  • Preparing process for vildagliptin/metformin hydrochloride compound preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Prescription:

[0019] Element Quantity / piece Vildagliptin 50mg Metformin Hydrochloride 1000mg Hydroxypropyl Cellulose 130mg Magnesium Aluminum Silicate 6mg Magnesium stearate 12mg

[0020] production method:

[0021] Add 50.0g of vildagliptin and 1.0kg of metformin hydrochloride to ethanol with 3 times the mass of the active substance and stir, then add 6g of magnesium aluminum silicate and 130g of hydroxypropyl cellulose to form a uniform dispersion. The prepared liquid is passed through a fluidized bed for spray drying, and the moisture content of the material is 1%. The dried material is passed through a vibrating sieve, sieved to select the powder containing the active substance with a particle size between 75 μm and 150 μm, and the powder containing the active substance is obtained by adding 1% magnesium stearate, and directly used for pressing into a tablet. The production process parameters are as follows:

...

Embodiment 2～6

[0024]

[0025] production method:

[0026] Referring to the method of Example 1, vildagliptin and metformin hydrochloride were added to the solvent, and magnesium aluminum silicate and hydroxypropyl cellulose were added according to the prescription of Examples 2-6 to form a uniform dispersion. Referring to the process parameters of the following examples 2 to 6, spray drying is carried out through a fluidized bed, the moisture content of the material is 1%, and the powder containing the active substance is selected by sieving with a particle size between 75 μm and 150 μm. Magnesium steatate is then used directly for compression into tablets.

[0027]

Embodiment 11

[0032] Comparative example 1.1 production method:

[0033] Referring to the prescription of Comparative Example 1.1, vildagliptin, metformin hydrochloride and hydroxypropyl cellulose were added to ethanol to form a dispersion. Then, spray drying was carried out with reference to the process parameters in the preparation method of Example 1, and the moisture content of the material was 1%. Sieve to select the powder containing the active substance with a particle size between 75 μm and 150 μm obtained by the above method, add 1% magnesium stearate, and directly press it into a tablet.

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Abstract

The invention provides a preparing process for a vildagliptin / metformin hydrochloride compound preparation. The preparing process comprises the following steps: (1) adding vildagliptin, metformin hydrochloride, magnesium aluminosilicate and hydroxy propyl cellulose into ethanol or isopropanol to form a dispersion liquid; (2) spraying and drying the dispersion liquid obtained in the step (1) to obtain spherical active matter-containing powder; (3) sieving and selecting the active matter-containing powder with particle size of 75 to 150 microns, which is obtained through the method, adding 1% of magnesium stearate, and directly pressing to form a tablet. The preparing process has the advantage that the unexpected satisfaction effects of uniform fluidity of integral materials and storage stability of the preparation are realized.

Description

technical field [0001] This field belongs to the technical field of medicine, and in particular relates to a preparation method of a pharmaceutical composition containing vildagliptin and metformin hydrochloride. Background technique [0002] Vildagliptin (vildagliptin) is a dipeptidyl peptidase IV (DPP-IV) inhibitor, also known as incretin enhancer, by inhibiting the activity of DPP-IV, to reduce glucagon-like peptide I GLP- 1, and then stimulate the secretion of insulin under high blood glucose concentration, and play an anti-type 2 role by delaying gastric emptying, inhibiting the release of glucagon, promoting the proliferation and differentiation of islet β cells, and enhancing satiety. Diabetes function. [0003] Metformin hydrochloride does not promote insulin secretion. Its hypoglycemic effect is mainly to promote the uptake of glucose by adipose tissue, increase the anaerobic glycolysis of muscle tissue, increase the utilization of glucose, and reduce the absorptio...

Claims

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Application Information

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IPC IPC(8): A61K31/40A61K47/10A61K47/02A61P3/10A61K31/155
Inventor 包金远许瑞蒋玉伟张孝清
Owner NANJING HUAWE MEDICINE TECH DEV
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