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[摘要]
目的 研究盐酸吡硫醇脂质体注射液在大鼠体内的药动学行为,并与盐酸吡硫醇注射液进行比较,评价盐酸吡硫醇脂质体药动学特征。方法 采用大鼠股静脉给药,眼眶取血,UPLC/MS/MS法测定大鼠血浆中盐酸吡硫醇的浓度,运用MasslynxTM NT4.1软件进行数据采集;运用QuanLynxTM program进行数据分析。结果 脂质体及溶液剂的AUC0-t分别为(1817.093±197.832)、(2592.349±303.194)μg/(L?h);Cmax分别为(6080.502±549.12)、(9525.987±531.813)μg/L;t1/2分别(1.512±0.387)、(0.732±0.388)h。两制剂的药时过程均符合三隔室模型,两者药动学行为相似。结论 运用DAS2.0进行生物等效性评价,脂质体组与溶液剂组药动学参数均在等效置信区间内,两制剂生物等效。
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[Abstract]
Objective To study on the pharmacokinetic behavior in vivo of pyritinol hydrochloride(Py-Hy)liposomes injection in rats and compare with the Py-Hy solution to evaluate pharmacokinetic characteristics of the Py-Hy liposomes. Methods Using femoral vein of rats, taking eyes blood, using UPLC/MS/MS to determinate plasma concentration of pyritinol hydrochloride in rat, using Masslynx TM NT4.1 software for data collection. Using Quan LynxTM program for data analysis. Results AUC0-t of liposomes and solution agent are (1817.093 ± 197.832) and (2592.349 ± 303.194) μg/(L?h), Cmax were (6 080.502 ± 549.12) and (9 525.987 ± 531.813) μg/L, t1/2 were (1.512 ± 0.387) and (0.732 ± 0.388) h, respectively. The medicine processes of the two preparations was in line with the three compartment model, and the pharmacokinetic behavior of the two preparations was similar. Conclusion The bioequivalence is evaluated by DAS2.0, the pharmacokinetic parameters of liposomes and solution agent group is in equivalent within the confidence interval, and the two preparations is biological equivalent.
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