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目的:建立HPLC-MS方法同时测定血浆中6种生物碱的浓度以评价2种给药载体中左金丸的主要成分药物动力学过程。方法:家兔经皮给予相同剂量的微乳凝胶和水凝胶后不同时间点采集血浆样本,LC-MS法测定血浆中6种生物碱的浓度,数据以WinNonLin软件拟合,并计算主要药动学参数。结果:以小檗碱、巴马汀、黄连碱、药根碱、吴茱萸碱和吴茱萸次碱为指标成分,与水凝胶比较微乳凝胶的相对生物利用度分别为131%,127%,108%,121%,92%,109%,吸收速率常数之比分别为10.5,5.1,3.7,0.8,1.8,1.5。结论:该方法可同时测定血浆中上述6种生物碱的含量,能快速、简便地进行生物样本分析;药代动力学参数显示,与水凝胶相比,微乳凝胶给药系统能加速药物的经皮吸收速度。
OBJECTIVE: To establish a HPLC-MS method for the simultaneous determination of six alkaloids in plasma to evaluate the pharmacokinetics of the main components of Zuojin pills in two kinds of drug delivery vehicles. Methods: Plasma samples were collected from rabbits at different time points after microemulsion gel and hydrogel were administered percutaneously. The concentrations of six alkaloids in plasma were determined by LC-MS. The data were fitted by WinNonLin software and the main Pharmacokinetic parameters. RESULTS: The relative bioavailability of microemulsion gel with hydrogels was 131%, 127%, respectively. The relative bioavailability of berberine, palmatine, coptisine, jatrorrhizine, evodiamine and rutaecarpine was the highest, The ratios of 108%, 121%, 92%, 109% and absorption rate constants were 10.5, 5.1, 3.7, 0.8, 1.8, 1.5. Conclusion: This method can simultaneously determine the contents of the above six kinds of alkaloids in plasma, and can quickly and easily analyze the biological samples. The pharmacokinetic parameters show that compared with the hydrogel, the microemulsion gel delivery system can accelerate Percutaneous absorption rate of the drug.