摘要 |
Combinations and compositions for use in enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17a-alkoxycarbonyloxy-11ß-hydroxyandrost-4-en-3-one-17ß-carboxylate type and the corresponding ?<SUP>1,4</SUP>-compounds are described. The enhancing agents have the formula:(II) wherein Z<SUB>1</SUB> is carbonyl, ß-hydroxymethylene or methylene; R<SUB>2</SUB> is H, -OH or -OCOR<SUB>3</SUB> wherein R<SUB>3</SUB> is C<SUB>1</SUB>-C<SUB>5</SUB> alkyl; Y is -OH, -SH or -OCOR<SUB>4</SUB> wherein R<SUB>4</SUB> is C<SUB>1</SUB>-C<SUB>5</SUB> alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Also use of the combinations and compositions in treating topical or other localized inflammation. |