Yacobi A, Stoll R G, Sum C Y, Lai C M, Gupta S D, Hulse J D
J Clin Pharmacol. 1982 Apr;22(4):206-12. doi: 10.1002/j.1552-4604.1982.tb02164.x.
To determine the elimination of high-molecular-weight hydroxyethyl starch (HES, Mw 450,000) in normal subjects, ten volunteers were given 500 ml 6% HES solution by intravenous infusion, and serial blood and urine samples were collected for nonglucose total carbohydrate determination. On the average, 46 and 64 per cent of the dose was excreted in the urine within two and eight days, respectively. The plasma concentration declined rapidly during the first week after infusion. The average terminal half-life was 17 days during the first 42 days, which accounted for elimination of about 90 per cent of the dose. The remainder was eliminated with a terminal half-life of 48 days determined between days 42 and 83 of the study. As expected, the infusion of HES resulted in plasma volume expansion over a 48-hour period during which time levels of nonglucose carbohydrates were above 3.5 mg/ml. HES is metabolized by alpha-amylase in the body. During the first 48 hours after infusion of HES, plasma alpha-amylase activity was significantly increased over control. Concomitantly, alpha-amylase activity in urine was also elevated but not significantly so.
为确定正常受试者体内高分子量羟乙基淀粉(HES,分子量450,000)的清除情况,对10名志愿者静脉输注500 ml 6% HES溶液,并采集系列血液和尿液样本用于测定非葡萄糖总碳水化合物。平均而言,分别在2天和8天内有46%和64%的剂量经尿液排出。输注后第一周血浆浓度迅速下降。在最初42天内平均终末半衰期为17天,这期间约90%的剂量被清除。在研究的第42天至83天期间测定的终末半衰期为48天,其余部分以此半衰期被清除。正如预期的那样,输注HES导致48小时内血浆容量增加,在此期间非葡萄糖碳水化合物水平高于3.5 mg/ml。HES在体内由α-淀粉酶代谢。输注HES后的最初48小时内,血浆α-淀粉酶活性显著高于对照组。与此同时,尿液中的α-淀粉酶活性也有所升高,但升高不显著。