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Regorafenib and wogonin eutectic and application thereof

A technology of wogonin and regorafenib, applied in the field of medicine, can solve the problems of low oral bioavailability, influence of absorption and treatment effect, etc., and achieve the effects of improving bioavailability, increasing solubility, and reducing tumor volume

Pending Publication Date: 2020-05-08
QINGDAO CENT HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its poor solubility, the oral bioavailability is low, which affects the absorption and therapeutic effect of the drug. Improving the dissolution rate of poorly soluble drugs is an effective way to improve their bioavailability and enhance the therapeutic effect.

Method used

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  • Regorafenib and wogonin eutectic and application thereof
  • Regorafenib and wogonin eutectic and application thereof
  • Regorafenib and wogonin eutectic and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Dissolve about 173 mg of regorafenib and about 96 mg of wogonin (molar ratio 1:1) in 2-3 mL of acetonitrile:methanol 2:1 (V / V) solvent system, heat to 50°C, and use pore size Filter through a 0.22 μm microporous membrane, then mix the two solutions, let stand at room temperature to volatilize for 24 hours, then wash and filter, and vacuum dry at room temperature for 24 hours to obtain 167 mg of white crystalline solid with a yield of about 62.1%.

Embodiment 2

[0035] Dissolve about 346 mg of regorafenib and about 96 mg of wogonin (molar ratio 2:1) in 2-3 mL of acetonitrile:ethanol 2:1 (V / V) solvent system, heat to 50°C, and use pore size Filter through a 0.22 μm microporous membrane, then mix the two solutions, let stand at room temperature to volatilize for 24 hours, then wash and filter, and vacuum dry at room temperature for 24 hours to obtain 223 mg of white crystalline solid with a yield of about 50.4%.

Embodiment 3

[0037] Dissolve about 173 mg of regorafenib and about 190 mg of wogonin (molar ratio 1:2) in 2-3 mL of acetonitrile:ethyl acetate (2:1) solvent system, heat to 50°C, and use Filter through a 0.22 μm microporous membrane, then mix the two solutions, let stand at room temperature to volatilize for 24 hours, then wash and filter, and vacuum dry at room temperature for 24 hours to obtain 186 mg of white crystalline solid with a yield of about 51.2%.

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Abstract

The invention relates to a pharmaceutical composition for preventing and / or treating cancer and application thereof. The pharmaceutical composition takes regorafenib and wogonin as active ingredients,and the regorafenib and the wogonin exist in the form of eutectic. The compound disclosed by the invention has a good anti-cancer effect, particularly improves the solubility and bioavailability of an insoluble drug regorafenib for cocrystals of colon cancer, regorafenib and wogonin, and has a more remarkable anti-cancer effect compared with a physical mixture of the colon cancer, the regorafeniband wogonin.

Description

technical field [0001] The present invention relates to the field of medical technology, in particular to a drug compound for treating cancer, especially colon cancer, the drug compound contains regorafenib and wogonin as active ingredients, both in the form of co-crystals exist. Background technique [0002] Colon cancer is a common malignant tumor of the digestive tract that occurs in the colon, and it is more likely to occur at the junction of the rectum and the sigmoid colon. Tumor ranks third, and the incidence rate in my country is increasing year by year. [0003] Regorafenib is an oral multikinase inhibitor that targets tumorigenesis, tumor angiogenesis and maintenance of the tumor microenvironment by inhibiting multiple protein kinases. In September 2012, the US Food and Drug Administration (FDA) approved it for the treatment of colorectal cancer, and it is an important targeted drug for the treatment of colon cancer. Regorafenib belongs to class II in the Biophar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/81C07D311/30A61K31/352A61K31/44A61P35/00
CPCC07D213/81C07D311/30A61K31/352A61K31/44A61P35/00
Inventor 万海涛王睿孙晶王伟梁华韩淑红
Owner QINGDAO CENT HOSPITAL
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