γ-シクロデキストリン複合体化によるジゴキシンのバイオアベイラビリティの向上 : ヒトにおける舌下及び経口投与時の評価

概要

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The inclusion complex of digoxin with γ-cyclodextrin was prepared in a molar ratio of 1 : 4,and evaluated for sublingual and oral administrations in humans. In the dissolution tests of digoxin tablets, the increase in dissolution rate and decrease in acid hydrolysis were attained by γ-cyclodextrin complexation. The serum levels of digoxin after sublingual and oral administrations to human healthy volunteers in the form of complex tablets were higher than the digoxin alone, particularly in the case of the sublingual form of γ-cyclodextrin complex. The present data suggested that the sublingual administration of the rapid dissolving form of γ-cyclodextrin complex may be useful for improving the bioavailability of digoxin due to the prevention of acid hydrolysis in stomach and the enhancement of drug absorption rate.
1989-10-25