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Novel pharmaceutical tegafur co-crystal and preparation method thereof

A technology of tegafur and drugs, which is applied in the field of preparation of new co-crystals and new co-crystals to achieve the effects of improved bioavailability, improved stability and improved thermal stability

Inactive Publication Date: 2015-04-08
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At this stage, foreign research on drug co-crystals has gradually increased and deepened; while domestic research on it is still relatively small

Method used

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  • Novel pharmaceutical tegafur co-crystal and preparation method thereof
  • Novel pharmaceutical tegafur co-crystal and preparation method thereof
  • Novel pharmaceutical tegafur co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Take 0.40g of tegafur and 0.27g of 4-hydroxybenzamide, add 2ml of acetonitrile solution, heat to 60°C and reflux, stir to dissolve, continue to reflux for 20-30 minutes, quickly put it in an ice-water bath, and slowly precipitate white After 24 hours, the crystals were filtered to obtain a white tegafur organic drug co-crystal.

Embodiment 2

[0042] Take 0.40g of Tegafur and 0.27g of 4-hydroxybenzamide, add 4ml of acetonitrile solution, heat to reflux at 60°C, stir to dissolve, continue to reflux for 20-30 minutes, quickly put it in an ice-water bath, and slowly precipitate white After 24 hours, the crystals were filtered to obtain a white tegafur organic drug co-crystal.

Embodiment 3

[0044] Take 0.80g of Tegafur and 0.54g of 4-hydroxybenzamide, add 5ml of acetonitrile solution, heat to reflux at 60°C, stir to dissolve, continue to reflux for 20-30 minutes, quickly put it into an ice-water bath, and slowly precipitate white After 24 hours, the crystals were filtered to obtain a white tegafur organic drug co-crystal.

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystals, particularly relates to a novel pharmaceutical tegafur co-crystal and a preparation method thereof, and more particularly relates to a novel co-crystal consisting of tegafur and an organic matter of 4-phenol benzamide. The co-crystal takes the tegafur as a pharmaceutical effective component (API); the selected matter for forming the co-crystal is the 4-phenol benzamide; the tegafur is connected with the 4-phenol benzamide by hydrogen bonds and a pi-pi accumulation effect; and the stoichiometric ratio (mole ratio) of both the tegafur and the 4-phenol benzamide is 1:1. The method for preparing the co-crystal disclosed by the invention is a temperature reduction type crystallization method which is simple and convenient to operate and easy to implement; used solvents are organic solvents which are low in boiling point and low in cost, such as acetonitrile and ketone; and convenience is provided for realizing industrial production.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and in particular relates to a new co-crystal of tegafur and a preparation method of the new co-crystal. Background technique [0002] Tegafur is the second-generation fluorouracil drug for anti-metabolic tumor chemotherapy, which was successfully synthesized in 1968 by Dr. Hiller, a former Soviet scientist. Tegafur is an inactive precursor of 5-FU, which is degraded by liver drug-metabolizing enzymes and cytochrome P-450 system in vivo, and gradually transforms into 5-FU to work. Its anti-tumor mechanism is the same as that of 5-FU. Tegafur has the advantages of high fat solubility, oral administration, rapid gastrointestinal absorption, and long half-life. Its side effects are one-seventh of that of 5-FU, and its curative effect index is twice as high. [0003] Tegafur is widely used in the treatment of intestinal cancer and metastatic intestinal cancer, but because tegafur ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/04C07C235/46C07C231/24A61P35/00
CPCC07D405/04C07C231/24C07C235/46
Inventor 汤谷平吴敏胡秀荣沈洁赵蒙蒙
Owner ZHEJIANG UNIV
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