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Stable vildagliptin compound

A compound and composition technology, applied in the field of medicine, can solve the problems of high total amount of impurities, large number of vildagliptin impurities, difficult to repeat the crystal form, etc.

Inactive Publication Date: 2016-07-20
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] During the research process, by repeating the method of the prior art, the obtained vildagliptin has a large number of impurities and a high total amount of impurities, and it is difficult to repeat the crystal form after amplification

Method used

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  • Stable vildagliptin compound
  • Stable vildagliptin compound
  • Stable vildagliptin compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] In a 100L reaction kettle, add 6 kg of vildagliptin (purity 98.06%, HPLC) and 36L of acetone-acetonitrile-ammonia water = 3:1:0.5 mixture, heat to 60°C, keep warm for 30 minutes, while hot filter. The filtrate was kept at 30°C for 1.5 hours; then naturally cooled to room temperature and kept for 2.5 hours, the precipitated crystals were filtered and dried naturally at room temperature to obtain 5.71 kg of white crystals with a purity of 99.91%, and the solvent residue test met the requirements.

Embodiment 2

[0037] In a 100L reaction kettle, add 6 kg of vildagliptin (purity 98.06%, HPLC) and 48L of acetone-acetonitrile-ammonia = 3:2:1 mixture, heat to 70°C, keep warm for 30 minutes, while hot filter. The filtrate was kept at 35°C for 1 hour; then naturally cooled to room temperature and kept for 2 hours, the precipitated crystals were filtered and dried naturally at room temperature to obtain 5.56 kg of white crystals with a purity of 99.92%, and the solvent residue test met the requirements.

[0038] Microparticles or microspheres are prepared by combining the compounds of the present invention with a pharmaceutically acceptable solid or liquid carrier, and optionally with pharmaceutically acceptable adjuvants and vehicles, using standard and conventional techniques. The composition is used for the preparation of oral preparations. It is given by way of example only and in no way is it intended to limit the scope of the invention in any way.

Embodiment 3

[0040] Tablets containing vildagliptin

[0041] Prescription: 20 grams of vildagliptin, 10 grams of N-methylglucosamine, 21 grams of polyvinylpyrrolidone, 200 grams of microcrystalline cellulose, 150 grams of sodium carboxymethyl starch, 15 grams of magnesium stearate, appropriate amount of distilled water, Made in 10000 pieces.

[0042] Process: Dissolve vildagliptin and excipients in distilled water at 80°C, add 5% of microcrystalline cellulose, mix well, dry in vacuum, pulverize, pass through a 100-mesh sieve, mix well with other materials and press piece.

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Abstract

The invention specifically relates to a vildagliptin compound and a preparation method thereof, belonging to the technical field of medicine. The vildagliptin compound with a novel crystal form obtained in the invention has the advantages of high purity and good stability, wherein maximal impurity content is less than 0.05%. The preparation method for the vildagliptin compound has good reproducibility and enables the purity and the crystal form of the vildagliptin compound to be perfectly reproduced when carried out in pilot scale. The invention also relates to application of the vildagliptin compound with the novel crystal form is preparation of a drug used for treating diabetes type 2.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a vildagliptin compound crystal and a preparation method thereof, and also relates to the application of the crystal in the manufacture of medicine for treating type 2 diabetes. Background technique [0002] Vildagliptin is a selective, competitive and reversible DPP-4 inhibitor. Novartis was approved by the European Commission in 2007. Vildagliptin will be listed in 27 EU countries, Norway and Ireland , for improving blood sugar control in patients with type 2 diabetes. [0003] Chemical name: (2 S )-1-[2-[(3-Hydroxytricyclo[3.3.1.1 3,7 ]dec-1-yl)amino]acetyl]-2-pyrrolidinecarbonitrile (also known as 1-[2-(3-hydroxy-adamantane-1-amino)-acetyl]pyrrolidine-2(S) - nitrile); [0004] Molecular formula: C 17 h 25 N 3 o 2 [0005] Molecular weight: 303.40g / mol [0006] Its structural formula is as follows: [0007] [0008] During the research process, by re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/16A61K31/40A61P3/10
Inventor 严洁
Owner TIANJIN HANRUI PHARMA
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