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Sorafenib tosylate-hydroxypropyl-beta-cyclodextrin clathrate compound and preparation method thereof

A sorafenib tosylate: hydroxypropyl, cyclodextrin inclusion compound technology, applied in the field of hydroxypropyl-β-cyclodextrin inclusion compound and its preparation, can solve the toxic and side effects of anticancer drugs, Lack of selectivity, limited application, etc.

Inactive Publication Date: 2011-08-10
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the cytotoxicity of anticancer drugs lacks selectivity to normal cells and cancer cells, which leads to serious side effects of anticancer drugs and limits their clinical application.

Method used

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  • Sorafenib tosylate-hydroxypropyl-beta-cyclodextrin clathrate compound and preparation method thereof
  • Sorafenib tosylate-hydroxypropyl-beta-cyclodextrin clathrate compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The weight ratio of sorafenib tosylate and hydroxypropyl-β-cyclodextrin is 1:1.

[0018] Put 1 part of sorafenib tosylate and 1 part of hydroxypropyl-β-cyclodextrin in an appropriate amount of absolute ethanol by weight ratio to form a clear solution. Stir at 10°C for 1 h, then evaporate the solvent on a rotary evaporator, collect the product, grind it through an 80-mesh sieve, and dry it in vacuum.

Embodiment 2

[0020] The weight ratio of sorafenib tosylate and hydroxypropyl-β-cyclodextrin is 1:2.

[0021] Put 1 part of sorafenib tosylate and 2 parts of hydroxypropyl-β-cyclodextrin in an appropriate amount of absolute ethanol by weight ratio to form a clear solution. Stir at 20° C. for 2 h, then evaporate the solvent on a rotary evaporator, collect the product, grind it through an 80-mesh sieve, and dry it in vacuum.

Embodiment 3

[0023] The weight ratio of sorafenib tosylate and hydroxypropyl-β-cyclodextrin is 1:3.

[0024] Put 1 part of sorafenib tosylate and 3 parts of hydroxypropyl-β-cyclodextrin in an appropriate amount of absolute ethanol by weight ratio to form a clear solution. Stir at 30° C. for 3 h, then evaporate the solvent on a rotary evaporator, collect the product, grind it through an 80-mesh sieve, and dry it in vacuum.

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Abstract

The invention relates to a sorafenib tosylate-hydroxypropyl-beta-cyclodextrin clathrate compound and a preparation method thereof. Sorafenib plays the role of anticancer by inhibiting RAS / RAF / MEK (methyl ethyl ketone) / ERK (extracellular signal-regulated kinase) signal conducting channels and inhibiting tumor angiogenesis, and is directed to cancer cells instead of normal cells. The sorafenib is almost insoluble in water, and the average relative bioavailability of oral administration is 38% to 49%. According to the preparation method of the invention, the sorafenib tosylate-hydroxypropyl-beta-cyclodextrin clathrate compound is prepared based on the clathrate compound-forming property of hydroxypropyl-beta-cyclodextrin, thereby increasing medicine dissolvability, improving medicine dissolution and raising medicine bioavailability.

Description

technical field [0001] The invention relates to a hydroxypropyl-beta-cyclodextrin inclusion compound of an antitumor drug and a preparation method thereof. Background technique [0002] Sorafenib chemical name 4-{4-[3(4-chloro-3-trifluoromethyl-phenyl)-ureide]-phenoxy}-pyridine-2-carboxylic acid methylamine, molecular weight 464.8g / mol. Clinical use is Sorafenib Tosylate (Sorafenib Tosylate), its molecular formula: C 21 h 16 CIF 3 N 4 o 3 .C 7 h 8 o 3 S, molecular weight 637.0g / mol, molecular structure formula is as follows: [0003] [0004] Sorafenib tosylate is an odorless, white to brown solid. Good thermal stability, non-absorbent. Insoluble in water, slightly soluble in ethanol, soluble in polyethylene glycol 400. [0005] Sorafenib inhibits the growth of tumor cells in two ways: ① Sorafenib inhibits the activity of Raf-1 and B-Raf serine and threonine kinases, thereby inhibiting the RAS / RAF / MEK / ERK signaling pathway, inhibiting Proliferation of tumor ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/44A61P35/00A61K47/69
Inventor 栾立标申小萍
Owner CHINA PHARM UNIV
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