| 摘要 |
<p>Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17a-alkoxycarbonyloxy- 11 b-hydroxyandrost -4-en-3 -one-17 b-carboxylate type and the corresponding ?1,4-compounds are described. The enhancing agents have the formula: (II) wherein R is H or C1-C4 alkyl; Z1 is carbonyl or b -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.</p> |
