盐酸吡硫醇脂质体在大鼠体内药动学研究.PDFVIP

• 700 • 现代药物与临床 Drugs Clinic 第 28 卷 第 5 期 2013 年 9 月 盐酸吡硫醇脂质体在大鼠体内药动学研究 1 2 2 2 1* 李金卓 ，潘 磊 ，冯 佳 ，唐 星 ，金向群 1. 吉林大学，吉林 长春 130021 2. 沈阳药科大学，辽宁 沈阳 110016 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。 关键词：盐酸吡硫醇；盐酸吡硫醇脂质体；药动学 中图分类号：R969.1 ：R971 文献标志码：A 文章编号：1674 - 5515(2013)05 - 0700 - 04 DOI: 10.7501/j.issn.1674-5515.2013.05.011 Pharmacokinetics of pyritinol hydrochloride liposomes in rats 1 2 2 2 1 LI Jin-zhuo , PAN Lei , FENG Jia , TANG Xing , JIN Xiang-qun 1. Jilin University, Changchun 130021, China 2. Shenyang Pharmaceutical University, Shenyang 110016, China 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