Composition containing vildagliptin and metformin and preparation method

A technology for metformin and a composition is applied in the field of a composition containing vildagliptin and metformin and the field of preparation thereof, which can solve the problems such as a large increase in related substances, a rapid increase in impurities, and the inability to improve the compressibility of metformin, and achieve process impurities. The effect of reducing and simplifying the production process and improving the flowability of raw materials

Inactive Publication Date: 2018-01-05
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the original research product mentioned above, due to the use of special equipment, the production process is responsible. If metformin and vildagliptin are mixed with wet granulation, the related substances will increase greatly due to the contact with water in the process; if metformin is dry granulated alone, and The compressibility of metformin cannot be improved. If fillers such as microcrystalline cellulose are added to improve its compressibility, since microcrystalline cellulose and other moisture are high and difficult to remove during drying, the growth of impurities during the storage stability process is relatively large. quick

Method used

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  • Composition containing vildagliptin and metformin and preparation method
  • Composition containing vildagliptin and metformin and preparation method
  • Composition containing vildagliptin and metformin and preparation method

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preparation example Construction

[0022] The invention provides a method for preparing a composition containing vildagliptin and metformin, comprising: S1) dissolving 1 to 10 parts by weight of a binder in water and / or an alcohol solvent to obtain a granulation liquid; S2 ) Fluidized granulation and drying of 5-95 parts by weight of metformin and / or its pharmaceutically acceptable salt with the granulation liquid, and then adding 1-5 parts by weight of vildagliptin and / or its pharmaceutically acceptable salt The above acceptable salt is uniformly mixed with 1-5 parts by weight of lubricant, and compressed into tablets to obtain a composition containing vildagliptin and metformin.

[0023] Among them, the present invention has no special limitation on the sources of all raw materials, which can be commercially available.

[0024] In the present invention, the content of the binder is preferably 2 to 10 parts by weight, more preferably 2 to 8 parts by weight, and more preferably 2 to 5 parts by weight; the binde...

Embodiment 1

[0040] 1.1 Dissolve 20g of hydroxypropyl cellulose in 300mL of purified aqueous solution to prepare a granulation solution.

[0041] 1.2 Put 400 g of metformin into a fluidized bed for fluidization at a fluidization temperature of 65° C. to obtain a suspension mixture material.

[0042] 1.3 Spray the granulation solution in 1.1 onto the suspension mixture in 1.2 to granulate, dry at 60°C, add 20 g of vildagliptin, mix evenly, add magnesium stearate, mix evenly, compress tablets, and prepare Opadry coating Liquid and carry out coating, obtain vildagliptin metformin tablet.

Embodiment 2

[0044] 2.1 Dissolve 20g of hydroxypropyl cellulose in 300mL of purified aqueous solution to prepare a granulation solution.

[0045] 2.2 Put 500 g of metformin into a fluidized bed for fluidization at a fluidization temperature of 65° C. to obtain a suspension mixture material.

[0046] 2.3 Spray the granulation solution onto the suspension mixture material to granulate, dry at 60°C, add 25 g of vildagliptin, mix evenly, add magnesium stearate, mix evenly, compress tablets, prepare Opadry coating solution and Carry out coating, obtain vildagliptin metformin tablet.

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Abstract

The invention provides a preparation method of a composition containing vildagliptin and metformin. The method includes: S1) dissolving 1-10 parts by weight of an adhesive in water and/or an alcohol solvent to obtain a granulation solution; S2) subjecting 5-95 parts by weight of metformin and/or pharmaceutically acceptable salt thereof and the granulation solution to fluidization granulation and drying, then adding 1-5 parts by weight of vildagliptin and/or pharmaceutically acceptable salt thereof and 1-5 parts by weight of a lubricant, mixing the substances uniformly, and conducting tabletting to obtain the composition containing vildagliptin and metformin. Compared with the prior art, the invention adopts fluidization granulation and simplifies the production procedure, at the same timefluidization granulation improves the raw material fluidity, and the obtained particles are loose, thus increasing compressibility. In addition, vildagliptin and pharmaceutically acceptable salts thereof are not added in the granulation process, thus lowering process impurities.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a composition containing vildagliptin and metformin and a preparation method thereof. Background technique [0002] Vildagliptin is a selective, competitive and reversible DPP-4 inhibitor. Vildagliptin inhibits the activity of this enzyme by combining with DPP-4 to form a DPP-4 complex. It increases the concentration of GLP-1 and promotes the production of insulin by pancreatic B cells, while reducing the concentration of glucagon, thereby reducing blood sugar. and had no significant effect on body weight. The vildagliptin metformin compound tablet combines the advantages of the classic hypoglycemic drug metformin and the new dipeptidyl peptidase 4 (DPP-4) inhibitor vildagliptin, which can synergistically increase the level of GLP-1 and regulate the function of islet cells , reduce weight, and contribute to safe and effective blood sugar manageme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/40A61K9/20A61P3/10A61K31/155
Inventor 张伟明龙伟龙文陶安进袁建成
Owner HYBIO PHARMA
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