Abstract
The soft corticosteroid, loteprednol etabonate (chloromethyl 17α-ethoxycarbonyloxy-11β-hydroxy-3-oxoandrosta-1,4-diene-17β-carboxylate), I, was designed based on the “inactive metabolite approach.” Accordingly, I should be metabolized by hydrolysis to the corresponding inactive cortienic acid derivative, II. The in vitro and in vivo metabolism of I indeed yielded mainly this inactive metabolite, which is more hydrophilic and thus readily eliminated from the body. Relatively high levels of I were found in tissues after intravenous administration of the drug in rats. The permeability of I through hairless mouse skin was comparable to what has been found for related “hard” steroids, without significant metabolism taking place in the skin.
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Bodor, N., Loftsson, T. & Wu, Wm. Metabolism, Distribution, and Transdermal Permeation of a Soft Corticosteroid, Loteprednol Etabonate. Pharm Res 9, 1275–1278 (1992). https://doi.org/10.1023/A:1015849132396
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DOI: https://doi.org/10.1023/A:1015849132396