氧化苦参碱在乙肝患者体内的药动学

Pharmacokinetics of oxymatrine injection in patients with chronic hepatitis B

目的:研究氧化苦参碱注射液在乙型肝炎患者体内的药动学。方法:8例乙型肝炎患者和10名健康志愿者分别予氧化苦参碱注射液400mg,im,用HPLC分析法测定人血浆中的氧化苦参碱浓度。结果:肌注氧化苦参碱后其体内过程符合药动学二室模型,乙型肝炎患者和健康受试者的主要药动学参数分别为:T_((1/2)(K_a))(7.2±4.0),(4.6±2.0)min;T_((1/2)(α))(24.9±13.3),(29.8±13.8)min; T_((1/2)(β))(141.8±22.5),(133.3±19.1)min;t_(max)(23.8±12.2).(19.0±5.4)min;c_(max)(6.80±1.48),(7.09±0.88)mg·L^(-1);F(c)(41.96±11.00),(43.64±12.40)L;AUC(847.18±137.89),(934.49±159.06)mg·L^(-1)·min;CL_((s))(0.48±0.07),(0.44±0.07)L·min^(-1)。经统计学处理,2组药动学参数均无显著差异(P均>0.05)。结论:氧化苦参碱在乙型肝炎患者和健康人体内的药动学过程无显著性差异。

AIM: To study the pharmacokinetics of oxymatrine injection in patients with chronic hepatitis B. METHODS: Intramuscular injection of a single dose of 400 mg oxymatrine was given to 8 patients with chronic hepatitis B and 10 healthy male volunteers, respectively. The plasma concentrations of oxymatrine were determined by HPLC. RESULTS: The concentration-time curves of oxymatrine after intramuscular injection accorded with two-compartment model. The main pharmacokinetic parameters were as follows: T1/2(Ka)(7.2±4.0) , (4.6±2.0) min; T1/2(a)(24.9±13.3), (29.8±13.8) min; T1/2(β)(141.8±22.5), (133.3± 19.1) min; tmax(23.8 ±12.2), (19.0 ±5.5) min; Cmax(6.80± 1.48), (7.09±0.88) mg·L-1; V/F(c) (41.96 ±11.00), (43.64 ± 12.40) L; AUC (847.18 ±137.89), (934.49±159.06) mg·L-1·min; CL(s)(0.48 ±0.07), (0.44±0.07) L·min-1. CONCLUSION: The difference of the chief pharmacokinetic parameters of oxymatrine between the 2 groups (the patients with hepatitis B and the healthy volunteers) are not significant respectively ( P > 0.05) .