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Tegafur-L-proline eutectic and preparation method thereof

A technology of proline and tegafur, which is applied in the field of tegafur-L-proline co-crystal, can solve the problems of co-crystal stability and unsatisfactory dissolution rate, and achieve good chemical stability and good solubility , the effect of easy operation

Active Publication Date: 2020-09-22
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability and dissolution rate of these co-crystals are still unsatisfactory and need to be improved.

Method used

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  • Tegafur-L-proline eutectic and preparation method thereof
  • Tegafur-L-proline eutectic and preparation method thereof
  • Tegafur-L-proline eutectic and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0058] Dissolve 200mg of tegafur in 10ml of acetone solvent, 150mg of L-proline in 10ml of ethanol solvent, then mix the two solvents and heat to 50°C. After the solution is clarified, stir and react for 8 hours, then slowly cool down to 10~ After 15°C, stand for crystallization under temperature control for 58 hours, filter, wash the filter cake with propanol, and vacuum-dry Tegafur-L-proline cocrystal at 55°C for 10 hours. The yield is 93.23%, and the purity is 99.94%.

Embodiment 2

[0060] Dissolve 200mg of tegafur in 2.5ml of acetonitrile solvent, 138mg of L-proline in 3ml of ethanol solvent, then mix the two solvents and heat to 40°C. After the solution is clarified, stir and react for 10 hours, then slowly cool down to 5 After ~10°C, stand for crystallization under temperature control for 48 hours, filter, wash the filter cake with ethanol, and vacuum-dry Tegafur-L-proline cocrystal at 45°C for 12 hours. The yield is 92.22%, and the purity is 99.92%.

Embodiment 3

[0062] Dissolve 200mg of Tegafur in 3ml of acetone and 3ml of methanol mixed solvent, and 161mg of L-proline in 8ml of ethanol solvent, then mix the two solvents and heat to 60°C, stir the solution for 5 hours after clarification, then cool down slowly After reaching 15-20°C, set the temperature to stand and crystallize for 65 hours, filter, wash the filter cake with methanol, and vacuum-dry Tegafur-L-proline cocrystal at 60°C for 8 hours. The yield is 92.29%, and the purity is 99.93%. .

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Abstract

The invention discloses a tegafur-L-proline eutectic and a preparation method thereof, and belongs to the technical field of organic medicine eutectic. The molar ratio of tegafur to L-proline in the eutectic is 1:1. Under Cu-K[alpha] radiation, the an X-ray diffraction pattern has characteristic peaks, expressed by 2theta, at 7.0 + / - 0.2 degrees, 7.6 + / - 0.2 degrees, 8.6 + / - 0.2 degrees, 12.1 + / -0.2 degrees, 15.0 + / - 0.2 degrees and 18.0 + / - 0.2 degrees; wherein the eutectic is a monoclinic system, and the chiral space group is P21. The tegafur-L-proline eutectic crystal prepared by the preparation method disclosed by the invention is high in purity, relatively good in chemical stability and solubility and good in bioavailability.

Description

technical field [0001] The invention relates to the technical field of organic drug co-crystals, in particular to a tegafur-L-proline co-crystal. Background technique [0002] Tegafur (Tegafur, TG), whose chemical name is 1-(tetrahydro-2-furyl)-5-fluoro-2,4(1H,3H)-pyrimidinedione, is white or off-white crystalline powder , the molecular formula is C 8 h 9 FN 2 o 3 , the molecular weight is 200, and its structural formula is as follows: [0003] [0004] Tegafur is a derivative of fluorouracil. In 1968, Dr. Hiller, a former Soviet scientist, successfully synthesized TG. TG works by being degraded into fluorouracil by liver drug metabolizing enzymes and cytochrome P-450 system in vivo, and its function is the same as that of fluorouracil. Compared with 5-FU, TG has the advantages of high chemotherapeutic activity and low toxicity, and is widely used in the treatment of breast cancer and gastrointestinal cancer. [0005] Although tegafur is widely used in anti-tumor t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/04C07D207/16A61P35/00A61K31/513A61K47/18
CPCC07D405/04C07D207/16A61P35/00C07B2200/13
Inventor 张贵民翟立海李玲郭立红
Owner LUNAN PHARMA GROUP CORPORATION
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