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

Author(s): Yusuke Tanaka, Mitsugi Inkyo, Ryoko Yumoto, Junya Nagai, Mikihisa Takano, Shunji Nagata.

Abstract:

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.

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

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Article Details

VOLUME: 6
ISSUE: 6
Year: 2010
Page: [571 - 576]
Pages: 6
DOI: 10.2174/157341310793348713
Price: $58