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
CN110790712AActive Publication Date: 2020-02-14OCEAN UNIV OF CHINA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
OCEAN UNIV OF CHINA
Publication Date
2020-02-14

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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.
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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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