羟丙基-β-环糊精对地高辛透过大鼠小肠黏膜的影响

Effect of hydroxypropyl-β-cyclodextrin on permeability of digoxin through rat intestinal membrane

目的考察在不同质量浓度羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HPCD)溶液中地高辛透过大鼠小肠黏膜的能力。方法用大鼠离体外翻肠囊法进行小肠透过量试验;用HPLC法检查肠液中药物质量浓度。结果当HPCD质量浓度为0、1、2、5、10 mg.L-1时,地高辛2 h内在小肠中的累积吸收百分率依次降低,分别为51.3%、42.8%、33.1%、32.6%、11.7%。结论HPCD包合物降低了地高辛的小肠透过量,并减慢其吸收速度;游离药物与被包合药物存在着快速平衡,仍有部分药物透过小肠黏膜吸收。

Objective To test the permeability of digoxin through rat intestinal membrane in different concentrations of hydroxypropyl-β-cyclodextrin （HPCD）. Methods The rat everted gut sac was used to study the absorption of digoxin. The concentration of digoxin in the intestinal medium was determined by HPLC method. Results The concentrations of HPCD were 0,1,2,5 and 10 mg. L^-1, the accumulated absorption extent of digoxin decreased in turn with 51.3% 、42.8% 、33.1% 、32.6% and 11.7% ,respectively. Conclusions HPCD inclusion decreases the absorption extent and the rate of the absorption of the drug, however, a quick equilibrium is existed between the free drug and inclusion complexes, therefore, the absorption is only partially inhibited.