Simons K J, Briggs C J
J Pharm Pharmacol. 1985 May;37(5):367-9. doi: 10.1111/j.2042-7158.1985.tb05088.x.
The pharmacokinetics of HI-6, a cholinesterase-reactivating oxime, were studied in rats, following intravenous or intramuscular administration. A two-compartment model was used to analyse the intravenous data and a one-compartment open model with first-order absorption was used for intramuscular data. Drug concentration had no influence on rate and extent of absorption of intramuscular injections, and bioavailability was 100%. Peak plasma concentrations of HI-6 occurred 15 min after intramuscular injection. No significant differences were found between mean values for half-life, plasma clearance, volume of distribution and area under the plasma concentration versus time curve for the two intramuscular doses and the intravenous dose used. Mean HI-6 plasma concentrations were 140.5 +/- 4.2 micrograms ml-1 3 min after 20 mg ml-1 i.v., with a mean elimination half-life of 65.2 +/- 21 min. Plasma clearance rate was 3.95 +/- 0.93 ml min-1 kg and the apparent volume of distribution was 0.38 +/- 0.17 litre kg-1. The oxime is rapidly distributed in and eliminated by rats when administered intravenously or intramuscularly.
在大鼠体内静脉注射或肌肉注射后，对胆碱酯酶复活肟HI - 6的药代动力学进行了研究。采用二室模型分析静脉注射数据，采用一级吸收的一室开放模型分析肌肉注射数据。药物浓度对肌肉注射的吸收速率和程度没有影响，生物利用度为100%。HI - 6肌肉注射后15分钟出现血浆峰浓度。两种肌肉注射剂量和静脉注射剂量的半衰期、血浆清除率、分布容积和血浆浓度-时间曲线下面积的平均值之间未发现显著差异。静脉注射20mg/ml后3分钟，HI - 6的平均血浆浓度为140.5±4.2μg/ml，平均消除半衰期为65.2±21分钟。血浆清除率为3.95±0.93ml/min/kg，表观分布容积为0.38±0.17L/kg。静脉注射或肌肉注射时，该肟在大鼠体内迅速分布并消除。
