NEW ADDITION SALTS OF RALOXIFENE, PROCESS FOR THE PREPARATION THEREOF AND USE THEREOF IN THERAPY

摘要

The present invention describes new raloxifene salts, namely raloxifene sulfamate in amorphous and crystal forms and hydrates thereof as well as processes for the preparation thereof. The compounds have a better solubility in water and in 0.1 molar hydrochloric acid than the hitherto used salt raloxifene hydrochloride, therefore they are very suitable for the preparation of pharmaceutical preparations for preventing and treating osteoporosis, bone degradation and breast cancer in postmenopausal women. The present invention also enables the preparation of a new pharmaceutical form suitable for exterior transdermal use. The present invention also relates to a process for improving the stability of amorphous raloxifene sulfamate by adding sugars, preferably mannitol, which also enables the manufacture of dry injections and solid forms of the preparations with increased stability.