美斯地浓磷脂复合物大鼠体内药代动力学研究  

Pharmacokinetics of Mestinon-phospholipid Complex in Rats

作　　者：胡霓霓[1] 谭群友[2] 张梨[1] 尹华峰[1] 张景勍[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室,重庆400016 [2]第三军医大学大坪医院野战外科研究所胸外科,重庆400042

出　　处：《四川大学学报（医学版）》2012年第6期873-876,共4页Journal of Sichuan University(Medical Sciences)

基　　金：教育部博士点基金资助项目(No.20095503120008);重庆市教育委员会资助项目(首批高等学校优秀人才资助;No.KJ090308)资助

摘　　要：目的研究美斯地浓磷脂复合物在大鼠体内药代动力学特征。方法健康SD雄性大鼠12只,分为2组,采用双周期交叉随机实验,分别灌胃给予美斯地浓磷脂复合物混悬液(含美斯地浓1.5mg/kg)和美斯地浓原料药(含美斯地浓1.5mg/kg),于不同时间点眼底静脉丛取血,采用高效液相色谱法测定各时间点血药浓度。采用DAS 2.1.1药动学程序对有关参数进行分析。结果美斯地浓磷脂复合物的药代动力学参数为:达峰时间(Tmax)2h,峰浓度(Cmax)22.79μg/mL,药时曲线下面积(AUC0-∞)7128.21μg.min/mL,而美斯地浓原料药为:Tmax2h,Cmax6.00μg/mL,AUC0-∞1772.36μg.min/mL,美斯地浓磷脂复合物相对生物利用度是原料药的410.98%。结论美斯地浓磷脂化后能明显提高其口服生物利用度。Objective To determine the pharmacokinetics characteristics of mestinon-phospholipid complex （PBPLC） in rats. Methods This study adopted a single-dose, randomized, open-label, two-period crossover trial design. Twelve healthy rats were randomly divided into two groups. One group was orally administered with mestinon-phospholipid complex, and the other group was orally administered with reference mestinon solution （1.5 mg/kg of mestinon）. The plasma concentrations of the drugs in ophthalmic vein bloods were determined using HPLC. The pharmacokinetic parameters were calculated with the aid of DAS2. 1. 1 software. Results Pharmacokinetic parameters of mestinon-phospholipid complex were Tmax 2 h, Cmax 22. 79 μg·min/mL and AUC0-∞ 7128.21 μg·min/mL, which were different from those of free mestinon Tmax 2 h, Cmax 6. 00 btg/mL and AUC0-∞ 1772.36μg·min/mL. The relative bioavailability of mestinon-phospholipid complex was 410.98 % of free mestinon. Conclusion The oral bioavailability of mestinon increases remarkably when administered as mestinon- phospholipid complex.

关 键 词：美斯地浓 磷脂复合物 药代动力学 

分 类 号：R96[医药卫生—药理学]