PROCESS OF THERMODYNAMICAL ACTIVATION OF WATER-INSOLUBLE DRUGS LOADED INTO CROSS-LINKED POLYMERS

摘要

The present invention refers to a process to prepare a highly activated composite of one or more water-insoluble drugs, said process comprising the steps of: (a) subjecting said water-insoluble drug and a cross-linked polyme r to co-grinding; (b) exposing the ground product of step a. to contact with water or water vapours. The resulting composite contains large amounts of dr ug in the easily soluble amorphous form, reduced amounts of drug in the nanocrystalline form, and is substantially free from practically insoluble drug crystals.