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目的:建立Beagle犬血浆中栀子苷的高效液相色谱分析方法,研究醒脑静口服给药后栀子苷的药代动力学特征及生物利用度。方法:Beagle犬分别口服、注射给予醒脑静,采用HPLC测定Beagle犬血浆中栀子苷浓度,以Kinetica软件拟合,计算相关药动学参数。结果:Beagle犬血浆中栀子苷在1.24～158.88 mg.L-1线性关系良好,口服给药的主要药动学参数为Cmax(11.8±0.6)mg.L-1,Tmax(52.0±4.5)min,AUC(1 280.8±172.0)mg.min.L-1,MRT(118.7±25.4)min。注射给药的药动学参数为Cmax(107.4±6.3)mg.L-1,AUC(7 930.1±670.0)mg.min.L-1,MRT(92.4±5.1)min。生物利用度为(6.46±0.87)%。结论:该实验建立的Beagle犬血浆中栀子苷的HPLC分析方法,适用性良好,提取、方法回收率和日内、日间精密度均符合要求,室温及冻融条件下稳定性良好。醒脑静口服给药栀子苷的生物利用度较低。
OBJECTIVE: To establish a method for the determination of geniposide in plasma of Beagle dogs by HPLC and to study the pharmacokinetics and bioavailability of geniposide after Xingnaojing oral administration. Methods: Beagle dogs were orally administered with xingnaojing injection. The plasma concentration of geniposide in Beagle dogs was determined by HPLC. Kinetica software was used to calculate the pharmacokinetic parameters. Results: The geniposide in plasma of Beagle dogs had good linearity in the range of 1.24 ~ 158.88 mg.L-1. The main pharmacokinetic parameters of oral administration were Cmax (11.8 ± 0.6) mg.L-1, Tmax (52.0 ± 4.5) min, AUC (1280.8 ± 172.0) mg.min.L-1, MRT (118.7 ± 25.4) min. The pharmacokinetic parameters for injection were Cmax (107.4 ± 6.3) mg.L-1, AUC (7 930.1 ± 670.0) mg.min.L-1 and MRT (92.4 ± 5.1) min. Bioavailability was (6.46 ± 0.87)%. Conclusion: The HPLC method for determination of geniposide in plasma of Beagle dogs established in this experiment is of good applicability. The extraction, method recovery, intra-day and inter-day precision meet the requirements. The stability is good under room temperature and freeze-thaw conditions. Xingnaojing oral administration of lower bioavailability of geniposide.