期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 409, 期 1-2, 页码 260-268出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2011.02.051
关键词
Nanomilling; Nanosuspension; Poorly soluble compound; Vitamin E TPGS; Rod shape crystals
The purpose of this study was to develop a nanosuspension of a poorly soluble drug by nanomilling process using wet media milling to achieve superior in vitro dissolution and high in vivo exposure in pharmacokinetic studies. A promising nanosuspension was developed with Vitamin E TPGS based formulation with particle size in the nano range. Although the formulation showed significant improvement during in vitro dissolution and in vivo plasma level, probably due to the strong hydrophobic interaction between Vitamin TPGS and the drug molecule, crystal growth was observed during stability studies. A systematic study was done with different combinations of solubilizer/stabilizer system in order to obtain a more stable nanosuspension. Hydroxypropyl methylcellulose (HPMC 3 cps) was found to stabilize the nanosuspension by better surface coverage due to stronger interaction with the drug as compared to other stabilizers used in this study. (C) 2011 Elsevier B.V. All rights reserved.
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