IMPROVEMENT OF THE ACTIVITY AND/OR EFFECTIVENESS OF WEIGHT STEROIDS WITH ANTI-DISPOSAL EFFECT FOR TOPICAL OR LOCAL DISPOSAL

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 17-alkoxycarbonyloxy-11-hydroxyandrost-4-en-3-one-17-carboxylate type and the corresponding 1,4-compounds are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or -hydroxymethylene; X1 is O or S; R5 is OH, OR6, OCOOR6 or OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is OH.