Transporter enhanced corticosteroid activity

摘要

Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17alpha-alkoxycarbonyloxy-11beta-hydroxyandrost-4-en-3-one-17beta-carboxylate type and the corresponding Delta^1,4-compounds are described. The enhancing agents have the formula: wherein Z₁ is carbonyl, beta-hydroxymethylene or methylene; R₂ is H, -OH or -OCOR₃ wherein R₃ is C₁-C₅ alkyl; Y is -OH, -SH or -OCOR₄ wherein R₄ is C₁-C₅ alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated.