雷公藤总生物碱滴眼液在大鼠房水中药物浓度的测定

Determination the aqueous humor concentration of total alkaloid from tripterygium wilfordii eye drops in rats

目的测定雷公藤总生物碱滴眼液在大鼠房水中的浓度时间曲线。方法 SD大鼠48只随机分成实验组1(0.05%滴眼液组)、实验组2(0.025%滴眼液组)和对照组(口服组),每组16只大鼠32只眼,实验组1大鼠结膜囊内滴入0.05%的自制雷公藤总生物碱滴眼液,实验组2大鼠结膜囊内滴入0.025%的自制雷公藤总生物碱滴眼液,对照组饲服昆明山海棠粉(7.5g/kg),于给药后的0.5、1、2、4、8、12、24、48h各组分别处死2只大鼠,并抽取双眼房水20μl,应用高效液相色谱法测定房水中雷公藤次碱的药物浓度。结果实验组1与实验组2各时间点的药物浓度差异有统计学意义(P=0.041≤0.05),与对照组比较差异有统计学意义(P=0.04≤0.057)。实验组2和对照组比较差异无统计学意义(P=0.166≥0.05)。实验组1的药物峰值面积最大,其在0.2μg/ml的药物浓度可以维持约4 h。其次是实验组2,在0.2μg/ml的药物浓度可以维持约2 h,但对应峰值面积明显小于实验组1。对照组的药物浓度在0.2μg/ml以下,峰值面积小于实验组1和实验组2。结论 0.05%雷公藤总生物碱滴眼液与口服药物相比,可在房水中维持较高药物浓度,适合应用于临床。

Objective To determination the aqueous humor concentration of alkaloid from tripterygium wilfordii eye drops in rats. Methods 48 SD rats were divided randomly into 3 groups ： group 1 （ 16 rats, treated with 0. 05% total alkaloid from tripterygium wilfordii eye drops）, group 2 （16 rats, treated with 0. 025% total alkaloid from tripterygium wilfordii eye drops） and control group （16 rats, treated with Tripterygium Hypoglaucun Hutch） . Two rats each group were executed in the 0. 5, 1, 2, 4, 8, 12, 24, 48 hour. Aqueous humor （20 μl） of both eyes was sampled. Wilforine concentrations were deter- mined using validated high performance liquid chromatography. Results The difference between group 1 and group 2 was significant （P =0. 041 ≤0. 05）, the same as group 1 and control group （P =0. 046≤0. 05） . The difference between group 2 and control group was not significant （P = 0. 166 ≥0. 05） . Wilforine concentrations in aqueous humor of group 1 were elevated gradually. The peak concentration was 1 h. It contains 0. 2 μg/ml concentrations for about 4 hours, followed by group 1 and control group. Conclusion 0. 05% total alkaloids From Tripterygium Wilfordii eye drops was contain higher concentration than oral drugs and was good for clinical application.