伊维菌素长效透皮剂和普通注射剂在家兔体内的药代动力学比较研究

为比较研究制备的伊维菌素长效透皮制剂与普通伊维菌素注射剂药物代谢及药效时间，本研究制备伊维菌素含量分别为0.5%、1.0%和1.5%的长效透皮制剂，采用高效液相色谱法检测不同药量相同体积伊维菌素长效透皮制剂和普通伊维菌素注射剂（1.0%）在家兔体内的药代动力学，并通过PKSolver药代动力学处理软件对数据进行分析。结果显示，0.5%、1.0%、1.5%伊维菌素长效透皮剂和1.0%普通注射剂吸收半衰期分别为0.81、0.52、1.02和0.12 d；达峰时间为1.55、0.97、1.62和0.42 d；峰浓度为47.36、72.02、115.30和99.53 ng/mL；消除半衰期为3.61、5.92、5.59和1.79 d；平均滞留时间为5.27、7.37、5.13和2.16 d；药时曲线面积为1 488.70、3 081.98、3 161.20和480.00 ng·d/mL，伊维菌素长效透皮剂体内维持有效药物浓度的时间长达35 d，普通注射剂仅为9 d。结果表明，伊维菌素长效透皮剂效果稳定，可进行更深入的研究。

Comparative Study on Pharmacokinetics of Long-acting Transdermal Agents of Ivermectin and Common Injection in Rabbits

To compare the drug metabolism and efficacy time of ivermectin long-acting transdermal preparation and ordinary ivermectin injection,the study prepared the long-acting transdermal preparation with ivermectin content of 0.5%,1.0% and 1.5% respectively.The pharmacokinetics of ivermectin long-acting transdermal preparation and common ivermectin injection (1.0%) in rabbits with different dosage and the same volume were detected by HPLC,and the data were analyzed by PKSolver pharmacokinetic processing software.The results showed that the t_1/2ka of 0.5%,1.0%,1.5% ivermectin long-acting transdermal agent and 1.0% injection were 0.81,0.52,1.02 and 0.12 d,respectively;The T_max were 1.55,0.97,1.62 and 0.42 d,respectively;The C_max were 47.36,72.02,115.30,99.53 ng/mL,respectively;The t_1/2ke were 3.61,5.92,5.59 and 1.79 d;The MRT were 5.27,7.37,5.13 and 2.16 d,respectively;The AUC were 1 488.70,3 081.98,3 161.20 and 480.00 ng·d/mL,respectively.The effective concentration of long-acting transdermal agent of ivermectin was maintained for 35 d in vivo and 9 d in general injection.The effect of long-acting transdermal agents of ivermectin was confirmed,which could be further studied.