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Co-crystal of 5-fluorouracil and kaempferol and preparation method thereof

A technology of fluorouracil and kaempferol, which is applied in the field of medicinal chemistry, can solve the problems of poor solubility of kaempferol, low oral bioavailability, and limited potential of active anti-tumor drugs, and achieve good reproducibility, easy control of the crystallization process, and improved preparations compatibility effect

Active Publication Date: 2021-01-12
TIANJIN UNIVERSITY OF TECHNOLOGY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite its outstanding antitumor activity, kaempferol has low oral bioavailability due to its very poor solubility, limiting its potential as an active antitumor drug

Method used

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  • Co-crystal of 5-fluorouracil and kaempferol and preparation method thereof
  • Co-crystal of 5-fluorouracil and kaempferol and preparation method thereof
  • Co-crystal of 5-fluorouracil and kaempferol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Weigh 1.30 g of 5-fluorouracil and 2.86 g of kaempferol, add 30 ml of absolute ethanol to obtain a suspension, stir the suspension at room temperature for 5 hours, filter, and dry the resulting white solid at 40°C to obtain 5- A solid sample of co-crystal of fluorouracil and kaempferol, the yield is 83.3%.

Embodiment 2

[0048] Weigh 32.5 mg of 5-fluorouracil and 71.6 mg of kaempferol, add 1 ml of methyl acetate to obtain a suspension, stir the suspension at room temperature for 12 hours, filter, and dry the obtained white solid at 40°C to obtain 5- Solid sample of co-crystal of fluorouracil and kaempferol.

Embodiment 3

[0050] Weigh 13.0 mg of 5-fluorouracil and 28.6 mg of kaempferol, add them to a ball mill jar, then add 20 microliters of ethyl acetate, grind at a frequency of 20 Hz for 60 minutes, and dry the resulting white solid at 40°C to obtain 5-fluorouracil and kaempferol Eutectic solid samples.

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Abstract

The invention discloses a co-crystal of 5-fluorouracil and kaempferol and a preparation method of the co-crystal. The molar ratio of 5-fluorouracil to kaempferol in the co-crystal is 1: 1, and an X-ray powder diffraction pattern of the co-crystal has characteristic peaks when the value of an angle 2theta is equal to 12.2 + / -0.2 degrees, 13.9 + / -0.2 degrees, 14.8 + / -0.2 degrees, 16.5 + / -0.2 degrees, 17.5 + / -0.2 degrees or 26.7 + / -0.2 degrees. The co-crystal preparation method provided by the invention is simple in process, easy to control the crystallization process, good in reproducibility andsuitable for industrial production. The co-crystal can effectively reduce the hygroscopicity of kaempferol, optimize the dissolution properties of 5-fluorouracil and kaempferol, reduce a solubility difference between 5-fluorouracil and kaempferol, improve the preparation compatibility of 5-fluorouracil and kaempferol, and provide a research basis for better playing an anti-tumor synergistic effect of 5-fluorouracil and kaempferol.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a co-crystal of 5-fluorouracil and kaempferol and a preparation method thereof. Background technique [0002] Pharmaceutical active ingredients usually exist in crystalline forms, such as polymorphs, hydrates, solvates, salts, and co-crystals. Pharmaceutical co-crystals refer to crystalline substances in which active pharmaceutical ingredients and co-crystal formers are combined in the same crystal lattice in a fixed stoichiometric ratio through non-covalent interactions. The formation of co-crystals can adjust the physicochemical properties of drugs, including solubility, dissolution rate, bioavailability, stability, tabletability, etc., without changing the chemical structure. The co-crystal formed by the active ingredients of two drugs is also called drug-drug co-crystal, which can not only improve the physical and chemical properties of the two drugs at the same ...

Claims

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Application Information

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IPC IPC(8): C07D239/553C07D311/30A61P35/00A61K31/513A61K31/352
CPCA61P35/00C07B2200/13C07D239/553C07D311/30
Inventor 陈嘉媚吕文婷庄晓梅
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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