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目的:建立高效液相色谱法测定血中葛根素的浓度,研究葛根素前体脂质体的药动学和生物利用度。方法:以愈风宁心片为对照品,3P37药动学软件处理数据,进行了药动学和生物利用度实验。结果:葛根素前体脂质体口服tmax,Cmax,CL(s),AUC分别为(2.18±0.27)h,(1.12±0.21)mg·L-1,(10.1±2.2)L·h-1,(7.8±1.7)mg·h·L-1,愈风宁心片口服tmax,Cmax,CL(s),AUC分别为(1.52±0.35)h,(0.98±0.17)mg·L-1,(16.5±4.6)L·h-1,(4.8±1.4)mg·h·L-1。葛根素前体脂质体的相对生物利用度为145.6%。结论:葛根素前体脂质体血药浓度达峰时间相对滞后,达峰浓度提高,清除速率降低,葛根素前体脂质体生物利用度显著高于对照品。
Objective: To establish a HPLC method for determination of puerarin in blood and study the pharmacokinetics and bioavailability of puerarin proliposome. Methods: The data was processed with 3P37 pharmacokinetic software and the pharmacokinetics and bioavailability experiments were performed with Yufeng Ningxin Tablet as the reference substance. RESULTS: Oral tmax, Cmax, CL(s) and AUC of puerarin precursor liposomes were (2.18±0.27) h, (1.12±0.21) mg·L-1, (10.1±2.2) L·h-1, respectively. (7.8±1.7) mg·h·L-1, oral tmax, Cmax, CL(s), and AUC were (1.52±0.35) h and (0.98±0.17) mg·L-1, respectively. (16.5±4.6) L·h-1, (4.8±1.4) mg·h·L-1. The relative bioavailability of puerarin precursor liposomes was 145.6%. Conclusion: The plasma peak plasma concentration of puerarin pro-liposomal lags behind. The peak concentration increases, the clearance rate decreases, and the bioavailability of puerarin proliposome is significantly higher than that of the control.