Mesoporous material excipients for poorly aqueous soluble ingredients

摘要

The present invention encompasses formulations and methods for producing solid dispersions comprising mesoporous materials with poorly aqueous soluble active ingredients. The active ingredient is formed in the amorphous state and entrapped in the nanosized pores of the mesoporous excipients using a co-spray drying process. The pore walls of mesoporous channels stabilize the amorphous form of active ingredient against re-crystallization. The amorphous active ingredient entrapped in mesoporous channels exhibits good stability during extended storage under stress test conditions and possesses significantly enhanced dissolution rates.

主权项

1. An orally administrable pharmaceutical composition, said pharmaceutical composition comprising:
a substantially water-insoluble pharmaceutical active ingredient selected from the group consisting of ibuprofen, fenofibrate, indomethacin, carbamazepine, and ursodeoxycholic acid in a stable amorphous form which is present at about 50% w/w to about 75% w/w; and a mesoporous composition having a plurality of nanopores and selected from the group consisting of MCM-41, MCM-48, SBA-15, MCF, MSU and CMK-3, wherein said substantially water-insoluble pharmaceutical active ingredient is spray-dried together with said mesoporous composition to entrap said pharmaceutical active ingredient within said nanopores, wherein there is no crystal growth detected after 12 months storage at 40° C. and 75% relative humidity of said stable amorphous form.