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目的探讨口服中药熊胆粉透过血-眼屏障到达相应靶组织的机制及其作用。方法56只家兔按照随机数字表法分成对照组8只和给药组48只。给药组再随机分成6个亚组,每个亚组8只,空腹12h给予兔中药熊胆粉100mg/kg体重灌胃,分别在灌胃后0.5、1.0、2.0、4.0、6.0、8.0h于家兔耳缘静脉采血2ml,均左眼取房水、右眼取玻璃体。对照组的实验方法同给药组,处理时间记为0h。利用高效液相色谱仪法(HPLC)测定熊胆粉中标记物牛磺熊脱氧胆酸(TUDCA)在血液、房水、玻璃体内的浓度。结果利用HPLC可准确测血液、房水、玻璃体内TUDCA浓度,其中血液中浓度为(999.1±17.2)~(1300.6±78.2)μg/ml;房水中浓度为(12.7±1.4)~(47.8±4.7)μg/ml;玻璃体中浓度为(10.8±2.9)~(57.9±7.9)μg/ml。给药组各时间点血液、房水、玻璃体中TUDCA的浓度分别与对照组相比,差异有统计学意义(P<0.01);不同时间点房水和玻璃体内TUDCA浓度之间的比较,差异无统计学意义(P>0.05)。结论口服中药熊胆粉能透过血-眼屏障到达相应靶组织,于房水和玻璃体中的浓度明显小于血液中浓度,进入房水和玻璃体的能力相近。(中华眼科杂志,2006,421023-1025)
Objective To explore the mechanism and effect of oral administration of Chinese medicine bear bile powder through the blood-ocular barrier to reach the target tissue. Methods Fifty-six rabbits were divided into 8 groups in the control group and 48 in the administration group according to the random number table method. The dosing group was randomly divided into 6 subgroups, 8 in each subgroup, and rabbits were given 100 mg/kg body weight of bear bile powder 12 h after fasting, and 0.5, 1.0, 2.0, 4.0, 6.0, and 8.0 h after gavage, respectively. Rabbit blood was collected from the marginal veins of rabbits and 2 ml were taken from the left eye and the right eye. The experimental method of the control group was the same as that of the drug administration group, and the treatment time was recorded as 0 h. The concentration of TUDCA in blood, aqueous humor, and vitreous was determined by high performance liquid chromatography (HPLC). Results The concentration of TUDCA in blood, aqueous humor, and vitreous humor could be accurately measured by HPLC. The concentration in blood was (999.1±17.2)~(1300.6±78.2)μg/ml; the concentration in aqueous humor was (12.7±1.4)~(47.8±4.7). )μg/ml; vitreous concentration was (10.8±2.9)~(57.9±7.9)μg/ml. The concentrations of TUDCA in blood, aqueous humor, and vitreous in the administration group at each time point were significantly different from those in the control group (P<0.01); the differences between aqueous and intravitreal TUDCA concentrations at different time points were different. No statistical significance (P>0.05). Conclusion Oral Chinese herbal bear bile powder can reach the corresponding target tissue through the blood-eye barrier. The concentration in aqueous humor and vitreous is significantly lower than that in blood, and the ability to enter the aqueous humor and vitreous is similar. (Chinese Journal of Ophthalmology, 2006, 421023-1025)