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目的:考察良肤乳膏中丹皮酚、白鲜碱、梣酮及甘草次酸等主要有效成分在小鼠皮肤中滞留量与时间的关系,研究良肤乳膏小鼠皮肤药物动力学特征。方法:采用HPLC测定皮肤生物样品中各成分的浓度,计算不同时间给药,皮肤中丹皮酚、白鲜碱、梣酮、甘草次酸的滞留量,采用DAS软件拟合药物动力学参数。结果:良肤乳膏中丹皮酚、甘草次酸在小鼠皮肤中滞留量的动力学过程符合二室模型,白鲜碱、梣酮符合一室模型,4种成分皮肤给药t1/2Ka分别为0.307,0.112,0.146,0.216 h,Tlag分别为0.006,0.123,0.136,0.109 h,Tmax均0.5 h,Cmax分别为40.163,1.607,6.725,100.553μg.cm-3,t1/2β分别为14.719,1.262,0.838,234.807 h,AUC0-∞分别为116.987,2.713,9.345,697.000μg.cm-3.h-1,MRT0-∞分别为3.662,1.67,1.585,10.897。结论:4种主要有效成分能迅速渗透进入皮肤,并在皮肤局部较长时间蓄积,有利于药物在皮肤局部长时间发挥药理作用。
OBJECTIVE: To investigate the relationship between the amount of main active ingredients such as paeonol, diterpenoside, anthrone, and glycyrrhetinic acid in Liangfu cream in mouse skin and the time, and to study the skin pharmacokinetics of Liangfu cream in mice. . Methods: The concentration of each component in skin biological samples was determined by HPLC. The retention of paeonol, diterpenoside, anthrone, and glycyrrhetinic acid in skin was calculated at different times. DAS software was used to fit the pharmacokinetic parameters. RESULTS: The kinetics of paeonol and glycyrrhetinic acid retention in mouse skin in Liangfu cream was in accordance with the two-compartment model. Dibasic alkaloids and anthrone were consistent with a one-compartment model. Four constituents were administered at t1/2Ka. They were 0.307, 0.112, 0.146, and 0.216 h, Tlag was 0.006, 0.123, 0.136, and 0.109 h, Tmax was 0.5 h, and Cmax was 40.163, 1.607, 6.725, 100.553 μg.cm-3, respectively, and t1/2β was 14.719. , 1.262, 0.838, 234.807 h, AUC0-∞ were 116.987, 2.713, 9.345, 697.000 μg.cm-3.h-1, and MRT0-∞ were 3.662, 1.67, 1.585, 10.897, respectively. Conclusion: The four main active ingredients can penetrate into the skin quickly and accumulate in the skin for a long time, which is beneficial to the long-term pharmacological action of the drug in the skin.