麦冬提取物中多种皂苷类成分的药代动力学

Pharmacokinetics Research on Ophiopogonins Components in Ophiopogon japonicus Extract

摘要:

目的：对多种麦冬皂苷类成分在大鼠体内的药代动力学行为进行系统研究。方法：通过静注给药麦冬皂苷提取物，于不同时间点取大鼠血样，检测血药质量浓度。根据稀释比标准曲线法，得到大鼠血浆中多种麦冬皂苷类成分的标准曲线和线性范围，并测定静注给药后血浆内麦冬皂苷含量的变化，描绘体内暴露量大的成分的药时曲线并计算了相关药代动力学参数。结果：在静注给药大鼠血浆中筛选了28种皂苷类成分，由于含量的差异和血浆暴露的程度，麦冬皂苷类成分表现出不同的代谢行为。一类皂苷成分的血浆暴露水平高，在大鼠体内的血浆药物浓度-时间曲线下面积（AUC）较大，而另一类呈现相反的特征，血浆暴露水平低，在大鼠体内的AUC较小。结论：麦冬皂苷类成分复杂，种类繁多，由于其母核结构的不同，在血浆内的代谢具有不同的特点。本研究对于表征复杂中药成分组群在体内的代谢特点具有重要意义。

Abstract:

Objective: To study the pharmacokinetics research on ophiopogonins components in rats. The acquisitions in this paper include the standard curve of ophiopogonins in rat plasma and linear range, the description of concentration-time curve of ophiopogonins and the calculation of pharmacokinetic parameters of ophiopogonins. Method: The pharmacokinetics research on phiopogonins in rat was conducted by means of intravenous injection and intragastric administration. Intravenous injection dose of ophiopogon japonicus extract at 200 mg·kg^-1 was applied to each rat through the tail vein. Serial blood samples were collected in heparinized tubes from the orbital sinus. Pharmacokinetic parameters in rat plasma were calculated by compartmental models using the WinNonlin 6.1 software. Result: 5 minutes after the intravenous injection, 50 types of ophiopogonins components were detected in the plasma of rat, and 28 of them were calculated to pharmacokinetic coefficients. Conclusion: According to the result of proportion and plasma exposure, the ophiopogonins components show differential pharmacokinetics characteristics. Based on the relative exposure approach, pharmacokinetic coefficients are e obtained. The results suggested that part of ophiopogonins components has high exposure level in rat plasma and possess high area under curve (AUC), while the other types of ophiopogonins has relative low exposure level and low AUC.