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Evaluation of In Vitro Dissolution and In Vivo Oral Absorption of Drug Nanopowders Prepared by Novel Wet-Milling Equipment

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In vitro dissolution and in vivo oral absorption studies were carried out in order to evaluate the effects of nanoparticulation. Omeprazole, albendazole and danazol nanopowders were prepared using novel wet-milling equipment, an ULTRA APEX MILL, with Pluronic F-68 or F-108 as dispersing agents, followed by lyophilization. An in vitro dissolution study showed that the dissolution rates of all nanopowders were drastically improved compared to the corresponding bulk powders, and their apparent saturated solubilities also increased compared to mixed powders consisting of bulk powders and dispersing agents. The AUCs after oral administration to rats of omeprazole nanopowders with Pluronic F-68 and F-108, and albendazole nanopowder with Pluronic F-68, were 1.93, 2.90 and 10.3 times higher, respectively than those for the corresponding bulk powders. The ULTRA APEX MILL can be a very useful tool for pharmaceutical techniques to enhance the dissolution and oral bioavailability of poorly water-soluble drugs.

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Keywords: BCS; CMC; Cmax value; Dissolution rate; FaSSIF solution; HPLC; Hixson-Crowell equation; JP 2nd solution; Omeprazole; albendazole; Pharmacokinetic; Plasma; Pluronic F-108; Tmax; danazol; nanoparticles; nanopowder; oral absorption; pharmacogenomics; poloxamer; poorly water-soluble drug; wet-milling

Document Type: Research Article

Publication date: 2010-12-01

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