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Pazopanib hydrochloride as well as preparation method and application thereof

A technology of pazopanib hydrochloride and pazopanib hydrochloride crystals, applied in the field of crystals of pazopanib hydrochloride and its preparation, can solve the problems of high impurity content, poor method reproducibility, content and crystal form cannot be reproduced, etc. problems, to achieve high-purity, good stability

Inactive Publication Date: 2018-02-06
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But no matter what method, the obtained pazopanib hydrochloride has low purity and high impurity content; the method has poor reproducibility, and it is difficult to scale up to the pilot scale, so that the content and crystal form cannot be reproduced

Method used

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  • Pazopanib hydrochloride as well as preparation method and application thereof
  • Pazopanib hydrochloride as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] In a 50L reactor, add 3kg of pazopanib hydrochloride (purity 97.3%, HPLC) and 30.3L of water-acetone-ammonia=9:0.8:1.1 mixture, heat to 60°C-72°C, add 150 grams of activated carbon were incubated and stirred for 30 minutes, filtered while hot, naturally cooled to room temperature under filtrate stirring, and then incubated for 5.5 hours, crystallized, filtered, and vacuum-dried at room temperature to obtain 2.81 kilograms of pazopanib hydrochloride crystals. Melting point: 290.5°C-300.6°C, purity 99.95%, single impurity 0.04%, MS: 349.13 (M+H) solvent residue detection meets the requirements.

Embodiment 2

[0033] Capsules Containing Pazopanib Hydrochloride Compound

[0034] Prescription: 85 grams of pazopanib hydrochloride, 3.5 ml of propylene glycol, 145 grams of starch, made into 1000 capsules.

[0035] Process: Wet pazopanib hydrochloride and starch with 20% propylene glycol aqueous solution, mix well, sieve and granulate, dry at 55°C, granulate, and fill capsules.

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Abstract

The invention belongs to the technical field of medicine, and specifically relates to a crystal form of pazopanib hydrochloride and a preparation method thereof. The new crystal form of pazopanib hydrochloride obtained in the present invention has the advantages of high purity, the largest impurity is less than 0.5‰, and stability Good performance; the method has good reproducibility, and the purity and crystal form can be well reproduced when it is scaled up to the pilot scale.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a crystal of pazopanib hydrochloride and a preparation method thereof. Background technique [0002] Pazopanib hydrochloride is a new oral angiogenesis inhibitor developed by GlaxoSmithKline that interferes with the formation of new blood vessels required for the survival and growth of recalcitrant tumors, targeting the vascular endothelial growth factor receptor (VEGFR) , acts by inhibiting neovascularization of blood supply to tumors. It is indicated for the treatment of advanced renal cell carcinoma (a type of kidney cancer in which cancer cells are found in the kidney tubules), soft tissue sarcoma (STS), epithelial ovarian cancer, and non-small cell lung cancer (NSCLC). [0003] The structural formula of pazopanib hydrochloride is as follows: [0004] [0005] Pazopanib hydrochloride is a polymorphic compound. Patent WO2011069053A1 discloses more than a dozen crystal fo...

Claims

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Application Information

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IPC IPC(8): C07D403/12A61K31/506A61P35/00
CPCC07D403/12C07B2200/13
Inventor 严洁
Owner TIANJIN HANRUI PHARMA
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