Mastrandrea V, Ripa S, La Rosa F, Tarsi R
Int J Clin Pharmacol Res. 1984;4(3):209-12.
Amoxicillin was administered at doses of 500 mg and 1000 mg, intravenously and intramuscularly to normal volunteers in a parallel study. Intramuscular amoxicillin was 100% bioavailable at both dose levels. Mean peak serum levels observed for the 500 mg and 1000 mg doses, respectively, were: i.v. (5 min after dosing) 46 and 74 micrograms/ml; i.m. (30 min after dosing) 14 and 21 micrograms/ml. Six hour trough levels ranged between 0.5 and 0.9 micrograms/ml. Between 50% and 60% of the doses were excreted in urine as intact amoxicillin in the 24 h after dosing. Almost 90% of this excretion occurred in the first 3 h after dosing. There was a statistically significant increase in mean clearance, after i.v. dosing, from the 500 mg level (14.8 l/h) to the 1000 mg level (20.7 l/h) implying that amoxicillin pharmacokinetics are non-linear over this range. Since there was very little difference between mean renal clearances at these dose levels (9.2 and 11.7 l/h, respectively) this clearance change might be due to enhancement of non-renal clearance. It would not be expected that this non-linearity would have any therapeutic influence.
在一项平行研究中，对正常志愿者静脉注射和肌肉注射剂量为500毫克和1000毫克的阿莫西林。两个剂量水平的肌肉注射阿莫西林生物利用度均为100%。500毫克和1000毫克剂量观察到的平均血清峰值水平分别为：静脉注射（给药后5分钟）46和74微克/毫升；肌肉注射（给药后30分钟）14和21微克/毫升。6小时谷浓度在0.5至0.9微克/毫升之间。给药后24小时内，50%至60%的剂量以完整阿莫西林形式经尿液排泄。几乎90%的排泄发生在给药后的前3小时。静脉给药后，平均清除率从500毫克水平（14.8升/小时）至1000毫克水平（20.7升/小时）有统计学显著增加，这意味着在此剂量范围内阿莫西林的药代动力学呈非线性。由于这些剂量水平下平均肾清除率之间差异很小（分别为9.2和11.7升/小时），这种清除率变化可能是由于非肾清除率增加所致。预计这种非线性不会产生任何治疗影响。
