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目的 首次研制出雷公藤多甙（TⅡ）滴眼液,并用高效液相色谱仪法对该滴眼液的药代动力学参数进行研究。方法 将0.03％TⅡ滴眼液50μl滴入兔眼下睑结膜囊内,在4h中定时采取房水做为测试样本,经处理后,用高效液相色谱仪测定样本中的雷公藤内酯醇质量浓度。结果TⅡ滴眼液在新西兰白兔眼内为一室模型,主要药代动力学参数为:A=2.703 μg/Ml;Ke=2.047h-1;Ka=2.708h-1;Lagtime=0.456h;t1/2（ka）=0.256h;t1/2（ke）=0.339h;T（max）=0.880h;C（max）=0.278μg/ml;AUC=0.323μg/（h·ml）。其拟合的动力学方程为C（t）=178.123×Dose× （e-2.047×（t-0.456）-e-2.708×（t-0.456））。结论TⅡ滴眼液眼内有效峰浓度出现在点药后0.88h,4h基本被代谢消除。
AIM: To study the pharmacokinetics of tripterygium wilfordii (TII) eye drops for the first time and to study the pharmacokinetics of this eye drop by high performance liquid chromatography (HPLC). Methods 50μl of 0.03% TⅡ eye drops were dripped into the conjunctiva of the lower eyelid of rabbits. Atrial fibrillation was taken periodically as the test sample in 4 hours. After treatment, the HPLC method was used to determine the concentration of triptolide in the samples . Results The TⅡ eye drops in the New Zealand white rabbits were a one-compartment model with the main pharmacokinetic parameters as follows: A = 2.703 μg / Ml; Ke = 2.047h-1; Ka = 2.708h-1; Lagtime = 0.456h; t1 / 2 (ka) = 0.256 h; t1 / 2 (ke) = 0.339 h; T (max) = 0.880 h; C (max) = 0.278 μg / ml; AUC = 0.323 μg / (h · ml). The fitted kinetic equation was C (t) = 178.123 × Dose × (e-2.047 × (t-0.456) -e-2.708 × (t-0.456)). Conclusions The intraocular effective peak concentration of TⅡ eye drops appeared at 0.88h after 4h, and was basically eliminated by 4h.