TRANSPORTER-ENHANCED CORTICOSTEROID ACTIVITY

摘要

Combinations and compositions for use in enhancing the activity and/or du ration of action of loteprednol etabonate and other soft anti-inflammatory s teroids of the haloalkyl 17.alpha.-alkoxycarbonyloxy-11.beta.-hydroxyandrost -4-en-3-one-17.beta.-carboxylate type and the corresponding .DELTA.1,4-compo unds are described. The enhancing agents have the formula:(II) wherein Z1 is carbonyl, .beta.-hydroxymethylene or methylene; R2 is H, -OH or -OCOR3 wher ein R3 is C1-C5 alkyl; Y is -OH, -SH or -OCOR4 wherein R4 is C1-C5 alkyl, cy clopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Also use of the combinati ons and compositions in treating topical or other localized inflammation.