5-fluorouracil oral forms

Folic acid is a nutritional supplement frequently used during periods of deficiency. Folic acid needs increase during chronic diseases, such as malabsorption liver disease, alcoholism, and anticonvulsant or oral contraceptive use. Folic acid supplementation during pregnancy is strongly recommended to prevent neural tube defects to the unborn child. The active form of folic acid, folinic acid, is used in the management of certain medical diseases (e.g., patients taking methotrexate, and 5-fluorouracil). 

Buur A and Bundgaard H, Prodrugs of 5-fluorouracil V. 1-Alkoxycarbonyl derivatives as potential prodrug forms for improved rectal or oral delivery of 5-fluorouracil,/. Pharm. Sci., 75, 522-527 (1986). 

ABSTRACT. Inclusion complexation of carmoful (1-hexylcarbamoyl-5-fluorouracil, HCFU) with three cyclodextrins (a-, 3 " and Y CyDs) were studied by solubility method and X-ray diffractometry. On the basis of the phase solubility diagrams, solid complexes of HCFU with a-5 3" and yCyDs were obtained in the molar ratios (host guest) of 2 1, 1 1 and 1 1, respectively. The dissolution rate of HCFU from the solid complexes was much greater than that of HCFU itself (a-CyD > complex > 3 CyD complex > y-CyJ) complex > HCFU alone). The hydrolysis of HCFU was suppressed by 3 CyD, while no appreciable inhibition was observed by a- and yCyDs. The rapid dissolving form of HCFU-CyD complexes was found to increase significantly the serum levels of the drug after oral administration to rabbits. 

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