患者静脉输注羟乙基淀粉130／0．4或羟乙基淀粉200／0．5的药代动力学

Pharmacokinetics of 6% HES 130/0.4 versus 6% HES 200/0.5

目的比较患者静脉输注6％羟乙基淀粉（HES）130／0．4和HES200／0．5的药代动力学。方法择期手术患者20例，ASAI级，随机分为2组，HES130／0．4组和HES200／0．5组，每组10例。分别在30min内静脉输注500ml HES 130／0，4或HES200／0．5，蒽酮比色法测定输注后各时点血清中胶体浓度，采用3P97软件计算其药代动力学参数。结果二室模型权重为1时计算药代动力学参数最符合HES130／0．4和HES200／0，5的体内特点，HES 130／0．4主要的药代动力学参数如下：t1/2α=1．7h、t1/2β=10h、K10=0．13h^-1、K12=0.133h^-1、K21=0．210h^-1、CL（s）=10．77L／h、AUC=46mg·h·ml^-1。HES200／0．5主要药代动力学参数如下：t1/2α=3，2h、t1/2β=164h、K10=0．09h^-1、K12=0．120h^-1、K21=0．010h^-1、CL（s）=0．19L／h、AUC=53mg·h·ml^-1。结论HES130／0．4和HES200／0．5在血管内停留时间均较长，HES130／0．4较HES200／0．5具有更好的药代动力学特点，其消除半衰期短、在血液内无蓄积。

Objective To investigate the pharmacokinetics of 6% hydroxyethyl starch （HES） 13010.4 and 6% HES 20010.5 after single-dose infusion in healthy patients. Methods Twenty ASA Ⅰ adult patients undergoing elective surgery were randomly divided into 2 groups （ n = 10 each） ： group Ⅰ HES 13010.4 and group Ⅱ HES 20010.5. 6% HES 13010.4 and 6% HES 20010.5 500 ml were infused iv over 30 min in group Ⅰ and Ⅱ respectively. Blood samples were taken immediatey before and after HES infusion and at 0.5, 1, 2, 4, 6, 8, 12, 24 and 48 h after HES infusion for determination of serum colloid concentration by anthrone chromatometry. The pharmacokinetic parameters were calculated using software 3P97. Results When weight is 1, the blood colloid concentration vs time curve for HES 130/0.4 and HES 200/0.5 was fitted to a two-compartment model. The main pharmacokinetic parameters for HES 130/0.4：t1/2α = 1.7 h, t1/2β = 10 h, Kl0 = 0.13 h^-1 , K12 = 0.133 h^-1 , K21 = 0.210 h^-1, CL（s） = 10.77 L/h, AUC = 46 mg·h· ml^-1. The main pharmacokinetic parameters for HES 20010.5 ：t1/2α = 3.2 h, t1/2β = 164 h, K10 = 0.09 h^-1, K12 = 0. 120 h^-1 , K21 = 0.010 h^-1, CL（s） = 0.19 L/h, AUC = 53 mg·h· ml^-1 . Conclusion Both HES 130/0.4 and HES 200/0.5 stay in the circulation fairly long. The pharmacokinetic profile of HES 130/0.4 is better than that of HES 200/0.5 after single-dose administration in terms of elimination half time and accumulation in blood. The elimination half time is shorter and there is no intravascular accumulation.