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5-fluorouracil-caffeic acid eutectic crystal and preparation method thereof

A technology of fluorouracil and caffeic acid, which is applied in the pharmaceutical co-crystal of 5-fluorouracil and caffeic acid and its preparation field, can solve the problems of low bioavailability, poor physical and chemical properties, complex process technology, etc., and achieve high yield and purity, The effect of mild reaction conditions and simple process

Active Publication Date: 2020-07-24
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the poor physicochemical properties of 5-fluorouracil lead to its low bioavailability, which hinders the clinical application of 5-fluorouracil to some extent.
For this reason, scholars at home and abroad have formulated a variety of strategies to improve the physical and chemical properties of 5-fluorouracil, including pharmaceutical methods, molecular structure modification, etc., although these strategies have achieved certain results in improving the water solubility and permeability of 5-fluorouracil. Research progress, but its practical application is limited due to complex process technology, high cost and uncontrollable by-products

Method used

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  • 5-fluorouracil-caffeic acid eutectic crystal and preparation method thereof
  • 5-fluorouracil-caffeic acid eutectic crystal and preparation method thereof
  • 5-fluorouracil-caffeic acid eutectic crystal and preparation method thereof

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specific Embodiment approach 1

[0021] Specific implementation mode one: the molecular formula of the 5-fluorouracil-caffeic acid co-crystal in this embodiment is [C 4 h 3 N 2 o 2 F·C 9 h 8 o 4 2H 2 O], a 5-fluorouracil molecule, a caffeic acid molecule and two water molecules constitute the basic structural unit, the 5-fluorouracil-caffeic acid cocrystal belongs to the triclinic system, and the space group is P -1, the unit cell parameters are: a = 6.9299 Å, b = 6.9584 Å, c = 15.946 Å, α = 99.753°, β = 96.384°, γ = 98.812°. Its PXRD characteristic diffraction peaks appear at 11.36°, 13.1°, 15.64°, 19.48°, 26.08°, 28.12°.

[0022] The 5-fluorouracil-caffeic acid co-crystal described in this embodiment consists of one 5-fluorouracil molecule, one caffeic acid molecule and two water molecules bonded together through supramolecular interactions such as hydrogen bonds. Such as figure 1 As shown, the co-crystal is a complex formed by 5-fluorouracil and caffeic acid at a molar ratio of 1:1, and contains t...

specific Embodiment approach 2

[0023] Specific embodiment two: the preparation method of the present embodiment 5-fluorouracil-caffeic acid co-crystal is implemented according to the following steps:

[0024] Put 5-fluorouracil raw material and caffeic acid in a round-bottomed flask at a molar ratio of 1:1, add methanol and water (1:2, v / v) to the mixed powder, stir for 4-6 h and then filter, the filtrate After standing for 2-5 days, the solid phase was collected and dried in vacuum to obtain 5-fluorouracil-caffeic acid co-crystal.

specific Embodiment approach 3

[0025]Embodiment 3: This embodiment differs from Embodiment 2 in that the solid-to-liquid ratio of the mixture powder to the solvent in the system is 100 mg: (18-24) mL. Other steps and parameters are the same as in the second embodiment.

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Abstract

The invention discloses a 5-fluorouracil-caffeic acid eutectic crystal and a preparation method of the co-crystal, and relates to the field of pharmaceutical co-crystals. The composition of the 5-fluorouracil-caffeic acid eutectic crystal is [C4H3N2O2F.C9H8O4.2H2O], and a basic structural unit is formed by a 5-fluorouracil molecule, a caffeic acid molecule and two water molecules. The pharmaceutical 5-fluorouracil-caffeic acid eutectic crystal belongs to a triclinic system, and the space group is P-1. 5-fluorouracil and caffeic acid are used as raw materials, and the eutectic crystal is prepared by adopting a solvent evaporation method and a cooling method. According to the pharmaceutical 5-fluorouracil-caffeic acid eutectic crystal, the solubility of the 5-fluorouracil is improved, and afoundation is laid for improving the bioavailability and the drug effect of the 5-fluorouracil. The preparation method of the pharmaceutical 5-fluorouracil-caffeic acid eutectic crystal is simple andeasy to implement, low in cost and convenient to popularize in industrial pharmacy on a large scale.

Description

technical field [0001] The invention relates to the field of drug co-crystals, in particular to a drug co-crystal of 5-fluorouracil and caffeic acid and a preparation method thereof. Background technique [0002] 5-Fluorouracil is a commonly used anti-metabolite drug, which has therapeutic effects on various solid tumors such as colon cancer, gastric cancer, breast cancer, and lung cancer. However, the poor physical and chemical properties of 5-fluorouracil lead to its low bioavailability, which hinders the clinical application of 5-fluorouracil to some extent. For this reason, scholars at home and abroad have formulated a variety of strategies to improve the physical and chemical properties of 5-fluorouracil, including pharmaceutical methods, molecular structure modification, etc., although these strategies have achieved certain results in improving the water solubility and permeability of 5-fluorouracil. However, due to complex process technology, high cost and uncontroll...

Claims

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Application Information

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IPC IPC(8): C07D239/553C07C59/52C07C51/42C07C51/43A61K31/513A61K31/192A61P35/00
CPCC07D239/553C07C59/52C07C51/42C07C51/43A61P35/00C07B2200/13
Inventor 李延团于月明刘方焉翠蔚吴智勇
Owner OCEAN UNIV OF CHINA
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