Potential use of 2-hydroxypropyl-β-cyclodextrin for preparation of orally disintegrating tablets containing dl-α-tocopheryl acetate, an oily drug

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  • Potential Use of 2-Hydroxypropyl-.BETA.-cyclodextrin for Preparation of Orally Disintegrating Tablets Containing dl-.ALPHA.-Tocopheryl Acetate, an Oily Drug
  • Potential use of 2 hydroxypropyl v cyclodextrin for preparation of orally disintegrating tablets containing dl a tocopheryl acetate an oily drug

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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.

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