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目的:研究健康志愿者单次静脉滴注注射用胡黄连总苷(保肝降酶中药)后的药动学。方法:10例健康志愿者双周期、随机交叉静脉滴注注射用胡黄连总苷120,240 mg,用高效液相色谱-串联质谱测定血浆和尿液中胡黄连苷-Ⅰ、苷-Ⅱ的浓度,用Winnon Lin软件计算主要药动学参数。结果:健康人体单次静脉滴注注射用胡黄连总苷120,240 mg后,胡黄连总苷中胡黄连苷-Ⅰ、苷-Ⅱ组分的主要药动学参数:胡黄连苷-Ⅰ的Cmax分别为(462.51±102.54)和(885.42±149.40)ng·m L-1,t1/2分别为(1.16±0.30)和(1.44±0.41)h,AUC0~t分别为(598.61±138.18)和(1 263.57±226.40)h·ng·m L-1,AUC0~∞分别为(602.26±138.45)和(1 269.21±226.81)h·ng·m L-1;尿累积排泄百分率分别为(32.02±5.28)%和(31.23±7.14)%;胡黄连苷-Ⅱ的Cmax分别为(3 036.20±697.19)和(6 115.56±1 303.27)ng·m L-1;t1/2分别为(1.33±0.19)和(1.49±0.34)h,AUC0~t分别为(4 310.41±999.98)和(9 908.02±1 827.40)h·ng·m L-1,AUC0~∞分别为(4 337.38±1 003.38)和(9 936.52±1 827.40)h·ng·m L-1,尿累积排泄百分率分别为(49.42±7.28)%和(45.65±4.09)%。结论:健康人体单次静脉滴注120,240 mg注射用胡黄连总苷后,胡黄连苷-Ⅰ和Ⅱ在体内的处置过程大致相同,半衰期均较短,消除迅速。
OBJECTIVE: To study the pharmacokinetics of a single intravenous drip injection of Huhuanglian (a traditional Chinese herbal medicine for protection of the liver) in healthy volunteers. METHODS: Two-cycle, random cross-infusion of 10,240 mg total glucosides of Huhuanglian was injected into 10 healthy volunteers. Plasma and urinary concentrations of berberine-I and glucoside-II were determined by high performance liquid chromatography-tandem mass spectrometry. Winnon Lin software was used to calculate the main pharmacokinetic parameters. RESULTS: The main pharmacokinetic parameters of berberine-I and glycoside-II components in total glucosides of Huhuanglian were determined after single intravenous infusion of total glucosides of Huhuanglian 120 and 240 mg in healthy individuals: the Cmax of berberine-I was determined. It is (462.51±102.54) and (885.42±149.40) ng·m L-1, t1/2 is (1.16±0.30) and (1.44±0.41)h, and AUC0~t is (598.61±138.18) and (1) respectively. 263.57±226.40) h·ng·m L-1, AUC0~∞ were (602.26±138.45) and (1 269.21±226.81) h·ng·m L-1, respectively; the cumulative urinary excretion rate was (32.02±5.28). % and (31.23±7.14)%; Cmax of berberine-II was (3 036.20±697.19) and (6 115.56±1 303.27) ng·m L-1, respectively; t 1/2 was (1.33±0.19) and (1.49±0.34)h, AUC0~t were (4 310.41±999.98) and (9 908.02±1 827.40) h·ng·m L-1, and AUC0~∞ were (4 337.38±1 003.38) and (9) respectively. 936.52±1 827.40) h·ng·m L-1, the cumulative urinary excretion rate was (49.42±7.28)% and (45.65±4.09)%, respectively. CONCLUSION: After a single intravenous infusion of 120,240 mg of total glucosides of peponine for healthy individuals, the treatment of berberine-I and II in healthy individuals was approximately the same, with short half-lives and rapid elimination.