Medicaments with a high degree of solubility and method for...

A - Human Necessities – 61 – K

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A61K 47/00 (2006.01) A61K 9/14 (2006.01)

Patent

CA 1225029

ABSTRACT OF THE DISCLOSURE A novel process is provided for the preparation of a stable pharma- ceutical composition with a high dissolution rate in the gastrointestinal tract, in which the active principle is an amorphous form. The process includes the first step of dissolving, in a pharmaceutically-acceptable solvent, an active principle and a stabilizing and crystal-formation-inhibiting amount of a poly- mer selected from the group consisting of polyvinylpyrrolidone and polyalkylene- glycol-polyvinylpyrrolidone to provide a solution. The next step involves atomizing that solution in a sprayer such that the input temperature is between 110 to 150°C and the output temperature is between 80 and 120°C, thereby to obtain a stable, amorphous drug-polymer composition. The invention also embraces the stable, amorphous, drug-polymer composition so formed. Such medicaments are stable over a considerable period of time and are much more soluble than the previously known similar medicaments.

415001

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