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LC-MS/MS法同时测定大鼠血浆中茶多酚(tea polyphenols,TP)的4种儿茶素类抗氧化活性成分EGCG、ECG、EGC和EC。利用各成分血药浓度(C)-时间(T)曲线下面积占总面积百分率作为自定义权重系数Wj,计算TP的整合血药浓度(C′),并从logC′-T曲线估算TP多效应成分整合药代动力学(PK)参数。采用大鼠静脉注射TP后不同时间含药血清对小鼠体外肝匀浆脂质过氧化的抑制率(I)考察TP抗自由基效应(E),从E-T曲线计算TP的有关药效动力学(PD)参数;进而通过E-logC和E-logC′作图,线性回归,求出相关系数R2。结果表明,TP的E-logC′-T曲线符合静脉注射给药的三室模型药物消除规律,其整合PK参数显示TP在大鼠体内分布快速而广泛,自深室的消除缓慢;不同成分的PK参数相差较大,而其整合PK参数充分兼顾了酯型与非酯型儿茶素的PK特性。E-T曲线呈三相衰减,时程与logC′-T曲线时程一致。C′与I高度相关,且其吻合程度优于各成分,从而表明整合PK参数能够最大程度表征中草药的整体处置规律,反映整体效应物质在生物体内的存留特点。
Simultaneous Determination of 4 Catechins Antioxidant Active Ingredients EGCG, ECG, EGC and EC from Tea Polyphenols (TP) in Rat Plasma by LC-MS / MS. The integrated plasma concentrations of TP (C ’) were calculated using the area under the plasma concentration (C) -time (T) curve of each component as the custom weight coefficient Wj, and the TP was estimated from the logC’-T curve Effect Components Integrate Pharmacokinetic (PK) Parameters. Inhibition rate of lipid peroxidation in mice liver homogenate by using serum containing TP at different times after intravenous injection of TP (I) TP anti-free radical effect (E), TP pharmacokinetics (PD) parameters; and then through the E-logC and E-logC ’plot, linear regression, find the correlation coefficient R2. The results showed that the E-logC’-T curve of TP was in accordance with the elimination rule of intravenous injection of three-compartment model. The integration of PK parameters showed that TP was distributed rapidly and extensively in rats and was slowly eliminated from the deep compartment. PK of different components The parameters are quite different, and its integrated PK parameters take full account of the ester and non-ester type catechins PK characteristics. E-T curve was three-phase attenuation, time history and logC’-T curve consistent. C ’was highly correlated with I, and the degree of coincidence was better than that of each component, which indicated that the integration of PK parameters can fully characterize the overall disposal law of Chinese herbal medicine and reflect the characteristics of the whole effect substance in the living body.