Potential Use of 2-Hydroxypropyl-β-cyclodextrin for Preparation of Orally Disintegrating Tablets Containing dl-α-Tocopheryl Acetate, an Oily Drug

• Published in: Chemical & Pharmaceutical Bulletin Vol. 57; no. 11; pp. 1206 - 1212
• Main Authors: Keiichi MOTOYAMAa, Kiyoshi NAGATOMOa, Soliman Osama Abd ELAZIMa, Fumitoshi HIRAYAMAb, Kaneto UEKAMAb, Hidetoshi ARIMAa
• Format: Journal Article
• Language: Japanese
• Published: Pharmaceutical Society of Japan 01-11-2009
• ISSN: 0009-2363

To expand the application of a drug in orally disintegrating tablets, the potential use of β-cyclodextrin (β-CyD) and 2-hydroxypropyl-β-cyclodextrin (HP-β-CyD) as excipients for the tablets containing dl-α-tocopheryl acetate (VE), an oily drug, was evaluated. HP-β-CyD, not β-CyD, solubilized VE in water through the formation of higher order of complexes at the molar ratio of 1:2 (VE:HP-β-CyD). When prepared under the optimal preparation conditions, the VE tablets containing lactose and 5% (w/w) of HP-β-CyD, not β-CyD, had high hardness more than 4 kg and rapid disintegration within 100 s both in vitro and in vivo. In addition, VE tablets containing lactose and 5% (w/w) of HP-β-CyD, not β-CyD, maintained the high hardness and rapid disintegration under the accelerated stability test using different conditions for 4 weeks. Therefore, these results suggest the potential use of HP-β-CyD, not β-CyD, as an excipient for orally disintegrating tablets containing VE, an oily drug, in the molding method.