5-fluorouracil drug co-crystal with 2-aminopyridine as precursor and preparation method and application of 5-fluorouracil drug co-crystal

2015 
The invention relates to a preparation method and application of a novel 5-fluorouracil drug co-crystal. 5-fluorouracil is selected as a drug API, 2-aminopyridine is selected as a drug precursor, and the 5-fluorouracil drug co-crystal prepared through a solvent evaporation method and a liquid-phase assisted grinding method is a triclinic system, wherein the axial angle alpha is 104.152-104.452 degrees, the axial angle beta is 94.432-94.732 degrees, the axial angle gamma is 95.252-95.552 degrees, and other parameters of the triclinic system are shown in the specification. 5-fluorouracil-2-aminopyridine powder prepared through the two methods has very high purity and crystallinity, and the co-crystal compound has high solubility in an aqueous solution. The novel co-crystal structure prepared through the preparation method can effectively modify active ingredients of drugs, the situation that 5-fluorouracil and other external interferents form other bonds will not occur after 5-fluorouracil and 2-aminopyridine form the co-crystal through non-covalent bonds, and therefore the drugs are more stable.
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