Abstract
Bioreversible derivatization of mebendazole to improve its poor water solubility, which is attributed to its low peroral bioavailability, was performed by N-acylation of the benzimidazole moiety with various chloroformates. The N-alkoxycarbonyl derivatives were readily hydrolyzed to mebendazole in rabbit liver homogenate and in human and rabbit plasma. The pH-rate profiles for the hydrolysis of the derivatives were derived at 37°C, and the lipophilicity of the compounds was assessed by partition experiments in octanol-aqueous buffer systems. The water solubility of the N-alkoxycarbonyl derivatives was up to 16-times higher than that of the parent drug. The results obtained suggest that N-alkoxycarbonyl derivatives of benzimidazole anthelmintics may be useful to improve the peroral bioavailability.
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