Process of thermodynamical activation of water-insoluble...

Details Process of thermodynamical activation of water-insoluble... Process of thermodynamical activation of water-insoluble...

A - Human Necessities

61

K

A61K 9/16 (2006.01) A61K 9/14 (2006.01)

Patent

CA 2452575

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 polymer 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 drug in the easily soluble amorphous form, reduced amounts of drug in the nanocrystalline form, and is substantially free from practically insoluble drug crystals.

L'invention concerne un procédé permettant de préparer un composite hautement activé d'un ou de plusieurs médicaments insolubles dans l'eau. Ce procédé consiste : (a) à soumettre ce médicament insoluble dans l'eau et un polymère réticulé à un co-meulage ; (b) à exposer le produit meulé de l'étape (a) à un contact avec de l'eau ou des vapeurs d'eau. Le composite ainsi obtenu contient de grandes quantités de médicaments sous forme amorphe facilement soluble, de faibles quantités de médicaments sous forme nanocristalline et, de plus, ce composite est sensiblement dépourvu de médicaments sous forme de cristal pratiquement insolubles.

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