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Co-crystal of 5-fluorouracil and L-phenylalanine and preparation method thereof

A technology of phenylalanine and fluorouracil, which is applied in the field of pharmaceutical cocrystal of 5-fluorouracil and L-phenylalanine and its preparation, can solve the problems of high cost, complicated process, and limitation of practical application, and achieve simple process , high yield and purity, and low cost

Active Publication Date: 2020-02-14
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although these methods have made some progress in improving the physical and chemical properties of 5-fluorouracil, their practical application is limited by the complex process and high cost.

Method used

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  • Co-crystal of 5-fluorouracil and L-phenylalanine and preparation method thereof
  • Co-crystal of 5-fluorouracil and L-phenylalanine and preparation method thereof
  • Co-crystal of 5-fluorouracil and L-phenylalanine and preparation method thereof

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specific Embodiment approach 1

[0021] Specific embodiment 1: The molecular formula of the 5-fluorouracil-phenylalanine co-crystal of this embodiment is [C 4 H 3 N 2 O 2 F·C 9 H 11 NO 2 ], a 5-fluorouracil molecule and a L-phenylalanine molecule form the basic structural unit, the 5-fluorouracil-phenylalanine co-crystal belongs to the orthorhombic crystal system, and the space group is P 2 1 2 1 2 1 , The unit cell parameters are: a = 7.0087 Å, b = 12.3981 Å, c = 15.1304 Å, α = 90.00°, β = 90.00°, γ = 90.00°. The PXRD characteristic diffraction peaks appear at 13.918°, 15.438°, 18.663°, 19.098°, 19.982°, 25.398°, 27.063°.

[0022] The 5-fluorouracil-phenylalanine co-crystal described in this embodiment is composed of a 5-fluorouracil molecule and an L-phenylalanine molecule that are joined together through supramolecular effects such as hydrogen bonds. Such as figure 1 As shown, the co-crystal is a simple 1:1 complex of 5-fluorouracil and L-phenylalanine, and the proton of phenylalanine is located on the amino g...

specific Embodiment approach 2

[0023] Specific embodiment 2: The preparation method of the 5-fluorouracil-phenylalanine co-crystal of this embodiment is implemented in the following steps:

[0024] Put 5-fluorouracil crude drug and L-phenylalanine in a round-bottom flask at a molar ratio of 1:1, add 95% ethanol to the mixed powder, stir for 4-6 hours and filter, and place the filtrate for 2-5 days The solid phase was collected and dried in vacuum to obtain 5-fluorouracil-phenylalanine co-crystal.

specific Embodiment approach 3

[0025] Specific embodiment three: This embodiment is different from the specific embodiment two in that the solid-to-liquid ratio of the mixture powder and the solvent in the system is 100 mg: (20-27) mL. The other steps and parameters are the same as in the second embodiment.

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Abstract

The invention discloses a pharmaceutical co-crystal of 5-fluorouracil and L-phenylalanine and a preparation method of the pharmaceutical co-crystal, and relates to the field of pharmaceutical co-crystals. The 5-fluorouracil-phenylalanine co-crystal is [C4H3FN2O2*C9H11NO2], and a basic structural unit is formed from a 5-fluorouracil molecule and an L-phenylalanine molecule. The co-crystal belongs to the orthorhombic system, and the space group is P212121. 5-fluorouracil and L-phenylalanine are used as raw materials, and the pharmaceutical co-crystal is prepared by adopting solvent evaporation method and cooling method. According to the pharmaceutical co-crystal disclosed by the invention, the solubility of 5-fluorouracil is improved, and a foundation is laid for improving the bioavailability and the drug effect of 5-fluorouracil. The preparation method of the pharmaceutical co-crystal is simple and easy 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 L-phenylalanine and a preparation method thereof. Background technique [0002] 5-Fluorouracil is a commonly used anti-tumor drug in clinical practice. It is mainly used for the treatment of skin cancer, gastrointestinal tumors, liver cancer, breast cancer and other cancers. It is the preferred chemotherapy drug for colon cancer. However, the permeability and water solubility of 5-fluorouracil are poor, resulting in low bioavailability, which limits the application of 5-fluorouracil in the field of medicine. Therefore, improving the physical and chemical properties of 5-fluorouracil has become an important issue. At present, domestic and foreign researchers have tried many methods, including pharmaceutics and chemical structure modification. Although these methods have made some progress in improving the physical and chemical properties of 5-fl...

Claims

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Application Information

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IPC IPC(8): C07D239/553C07C229/36C07C227/42
CPCC07D239/553C07C229/36C07C227/42C07B2200/13
Inventor 李延团王琳琳王凌阳焉翠蔚吴智勇
Owner OCEAN UNIV OF CHINA
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