格尔德霉素滴眼液在离体兔眼角膜的吸收与扩散

Absorption and permeability experiments of in vitro rabbit cornea of geldanamycin eye drops

目的制备格尔德霉素 ( geldanamycin)滴眼液 ,进行离体兔眼角膜实验 ,检测角膜及人工房水中药物量。方法采用二室渗透池法 ,在不同时间点取人工房水及角膜 ,分别测定药物在角膜吸收量及角膜中药物扩散进入人工房水量 ,对累积数据进行方程模拟。结果药物易被角膜吸收 ,但不易渗透进入房水 ,药物在角膜中不同时间的吸收累积曲线符合Higuchi方程 ,吸收速率常数为10 2 1 9ng/h。角膜中的药物扩散进入人工房水符合零级方程 ,药物在角膜和人工房水中达到平衡的时间分别为 2h和 4h ,药物从角膜扩散进入人工房水有 2h时滞。结论格尔德霉素滴眼液易被兔眼角膜吸收 ,且在角膜中达到较高浓度 。

Objective To prepare geldanamycin eye drops,doing experiments with in vitro rabbit cornea and detecting the release quantity of drug in cornea and man made aqueous humor.Methods By using two osmotic cells,man made aqueous humor and cornea were taken and the release amount of drug was determined at different time,developed the non lines fits of release from geldanamycin eye drops in cornea and man made aqueous humor individually.Results It is easy for geldanamycin to be absorbed in the cornea,but is difficult to penetrate into man made aqueous humor.The absorption of geldanamycin in the cornea is fit for the Higuchi equation with the velocity constant of absorption being 1 021 9 ng/h .Release of geldanamycin in man made aqueous humor from the cornea is fit for the Zero order equation,The equilibrate time in the cornea and aqueous humor is 4 h and 2 h individually.There is a time lag in man made aqueous humor which is 2 h .Conclusions Geldanamycin eye drops is easy to be absorbed by the cornea,relative high drug concentration can be detected in the cornea,there is a satisfactory prospect for geldanamycin in the treatment of herpes simplex keratitis(HSK).