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目的 测定小儿抗痫胶囊中主要有效成分 α-细辛醚在大鼠体内的血药浓度 ,并根据血药浓度 -时间配对资料测算其体内药代动力学参数。方法 采用 HPL C测定 ig给药 1.2 5 ,2 .5 ,5 g/ kg不同剂量小儿抗痫胶囊后 ,大鼠体内 α-细辛醚的血药浓度。血药浓度数据采用 3P97药代动力学软件进行参数模拟。结果 小儿抗痫胶囊中有效成分α-细辛醚在大鼠体内的动力学过程可用一级动力学过程的一室开放型模型来描述。低、中、高 3个不同剂量组高峰血药浓度 (Cmax)分别为 0 .4 6 ,0 .83,1.33μg/ m L,达峰时间 (Tpeak)分别为 81.94 ,88.85和 96 .12 min,血药浓度时间曲线下面积 (AUC)分别为 15 2 .75 ,2 2 5 .16和 393.2 1μg· m in/ m L。结论 本研究建立的 HPL C测定大鼠ig不同剂量小儿抗痫胶囊后 α-细辛醚血药浓度的实验方法简便、快速、灵敏 ,血浆中内源性物质及复方各组分药物不干扰测定。该研究可为小儿抗痫胶囊在临床和量化研究提供可靠的依据
Objective To determine the blood concentration of α-asarone, the main active component of Pediatric Anti-seizure Capsules in rats, and to measure the in vivo pharmacokinetic parameters based on the plasma concentration-time pairing data. Methods HPL C was used to measure the plasma concentration of α-asarone in rats after ig administration of 1.2, 2.5, and 5 g/kg of different doses of anti-epileptic capsules. Blood drug concentration data was simulated using 3P97 pharmacokinetics software. Results The dynamic process of α-asarone in rat anti-seizure capsules in rats can be described by a one-compartment open model with first-order kinetics. The peak plasma concentrations (Cmax) of the low, medium, and high dose groups were 0.46, 0.83, and 1.33 μg/m L, respectively, and peak time (peak) was 81.94, 88.85, and 96.12 min, respectively. The area under the blood concentration time curve (AUC) was 15 2 .75, 2 2 5 .16 and 393.2 1 μg·m in/m L, respectively. Conclusion The experimental method for the determination of α-asarone in children with ig different doses of anti-epilepsy capsules established by HPL C in this study is simple, rapid, and sensitive. The plasma endogenous substances and compound components do not interfere with the assay. . The study can provide a reliable basis for the clinical and quantitative research of anti-epileptic capsules in children