| 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-cn-3-one-17beta-carboxylate type and the corresponding Delta<SUP>1,4</SUP>-compounds are described. The enhancing agents have the formula: wherein Z<SUB>1 </SUB>is carbonyl, beta-hydroxymethylene or methylene; R<SUB>2 </SUB>is H, -OH or -OCOR<SUB>3 </SUB>wherein R<SUB>3 </SUB>is C<SUB>1-5 </SUB>alkyl; Y is -OH, -SH or -OCOR<SUB>4 </SUB>wherein R<SUB>4 </SUB>is C<SUB>1-5 </SUB>alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Ophthalmic administration in the treatment of dry eye is specifically targeted.
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