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• W2066483886 abstract "The transdermal absorption of 5-fluorouracil and its alkylcarbamoyl derivatives containing various lipophilic pro-moieties, including butylcarbamoyl, hexylcarbamoyl and octylcarbamoyl groups, was investigated in the rat. All compounds showed various degrees of lipophilicity and instability at physiological pH. Transdermal permeation of these drugs was examined by employing an in vitro technique using a diffusion device which was mounted with a full-thickness rat skin as the diffusion membrane. On application of the alkylcarbamoyl derivatives to the rat skin, 5-fluorouracil appeared in the receptor phase. 1-Butylcarbamoyl and 1-hexylcar-bamoyl derivatives showed 3–4-fold greater penetration than that of 5-fluorouracil. A lag time was observed before steady-state diffusion of the drug was established which was prolonged with increasing alkyl chain length. The increase in lipophilicity of the derivatives was found to enhance their binding with keratin, a component of the skin. The accumulation of both derivatives and 5-fluorouracil in the skin was noted. Drugs accumulated rapidly in the skin within 2 h after topical application and reached a constant level thereafter. In particular, the 1-butylcarbamoyl derivative, which permeated rapidly through the skin, showed a high level of accumulation in the skin. Co-application of 5-fluorouracil and the 1-octylcarbamoyl derivative resulted in an additive effect of skin absorption of 5-fluorouracil." @default.
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• W2066483886 date "1990-04-01" @default.
• W2066483886 modified "2023-09-23" @default.
• W2066483886 title "Transdermal delivery of 5-fluorouracil and its alkylcarbamoyl derivatives" @default.
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• W2066483886 doi "https://doi.org/10.1016/0378-5173(90)90184-6" @default.
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