| 摘要 |
The present invention to provide methods, pharmaceutical formulations, and devices for the transdermal delivery of 5-substituted-6-cyclic-5,6,7,8,- tetrahydronaphthalene2-o1 compounds ("lasofoxifene" or "CP-336,156") and pharmaceutically acceptable salts thereof. The invention also provides transdermal compositions of CP-336,156 or its salts dissolved or dispersed i n a suitable carrier vehicle, optionally containing permeation enhancers and other excipients. The carrier vehicle may be a pressure sensitive adhesive, polymeric reservoir, or a fluid of controlled viscosity. The carrier vehicle may be contained in a device for purposes of holding the composition against the skin surface. Such devices may be in the form of matrix patches (drug in adhesive) or reservoir patches (drug in a liquid or polymeric reservoir with peripheral, in-line, or over-layed pressure sensitive adhesive). Further provided by this invention are methods for treating pathologies associated with the binding of lasofoxifene with the human estrogen receptor-alpha. For example, the invention formulations and devices are useful to treat or preve nt bone loss, obesity, breast cancer, endometriosis, cardiovascular disease and prostatic disease. |
