美斯地浓磷脂复合物大鼠体内药代动力学研究

【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 1.5 mg/kg)和美斯地浓原料药（含美斯地浓1.5 mg/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) 2 h,峰浓度(Cmax) 22.79 μg/mL, 药时曲线下面积(AUC0-∞) 7128.21 μg·min/mL，而美斯地浓原料药为：Tmax 2 h, Cmax 6.00 μg/mL, AUC0-∞ 1772.36 μg·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。

英文摘要:

【Abstract】 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 μg/mL and AUC0-∞ 1772.36 μg·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.

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