Topical 5-fluorouracil prodrug composition and method

A - Human Necessities – 61 – K

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A61K 31/505 (2006.01)

Patent

CA 2065083

"TOPICAL 5-FLUOROURACIL PRODRUG COMPOSITION AND METHOD" ABSTRACT OF THE DISCLOSURE A pharmaceutical composition in unit dosage form adapted for topical administration to a human or non-human animal in need thereof comprising a pharmacologically affec- tive amount of a prodrug of 5-fluorouracil having the formula: Image wherein: R1 and R2 may be the same or different and are selected from the group consisting of H, R3CO- and R4-O-CO with the proviso that both R1 and R2 may not be H; or a non-toxic pharmaceutically acceptable salt, adduct, oxide or other derivative thereof; a pharmaceutically acceptable, topically administrable carrier therefor; and a method for topically applying the composition. R3 and R4 comprise groups such that the prodrug (1) has an enhanced delivery across topical membranes and (2) hydrolyzes after delivery to 5-fluorouracil.

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