Uekama K, Fujinaga T, Otagiri M, Seo H, Tsuruoka M
J Pharmacobiodyn. 1981 Sep;4(9):735-7. doi: 10.1248/bpb1978.4.735.
Inclusion complex of digoxin with gamma-cyclodextrin (gamma-CyD) in 1:4 molar ratio was prepared, and its dissolution and absorption behaviors were compared with those of digoxin alone. The dissolution rate of digoxin in water was found to be markedly increased by gamma-CyD complexation. Bioavailability of digoxin following the oral administration of gamma-CyD complex to dogs was 5.4 times as much as that of digoxin alone. The present data did indicate improvement of dissolution and absorption characteristics of digoxin by inclusion complexation, suggesting the decrease in dose in oral digoxin therapy.
制备了地高辛与γ-环糊精(γ-CyD)摩尔比为1:4的包合物,并将其溶解和吸收行为与单独的地高辛进行了比较。发现γ-环糊精包合显著提高了地高辛在水中的溶解速率。给犬口服γ-环糊精包合物后,地高辛的生物利用度是单独地高辛的5.4倍。目前的数据确实表明包合作用改善了地高辛的溶解和吸收特性,提示口服地高辛治疗时可降低剂量。