Uematsu T, Itaya T, Nishimoto M, Takiguchi Y, Mizuno A, Nakashima M, Yoshinobu K, Hasebe T
Department of Pharmacology, Hamamatsu University School of Medicine, Japan.
Eur J Clin Pharmacol. 1988;34(2):213-6. doi: 10.1007/BF00614562.
The pharmacokinetics and safety of a brief i.v. infusion of l-carnitine 0, 20, 40 and 60 mg/kg have been investigated in 10 healthy subjects. The diurnal intraindividual variability of plasma carnitine was small (C. V. = 3.0, 3.9 and 3.9%, respectively), and the total 24 h excretion in urine was also small and relatively constant: 4.6, 21.5 and 13.0 mg/day in the controls vs 4.6, 20.2 and 6.0 mg/day during treatment in the three subjects to whom saline alone was administered according to a single-blind design. Therefore, the pre-dose level of carnitine was subtracted from the level after dosing for the pharmacokinetic analysis. Plasma carnitine fitted well to a three-compartment open model, with Vc of 0.11-0.20 l/kg and a t1/2 gamma of 10-23 h. The urine recovery in 24 h was 77.2-95.4%. There were no objective or subjective side-effects attributable to carnitine, so its i.v. infusion is considered to be safe.
在10名健康受试者中研究了静脉快速输注0、20、40和60mg/kg左旋肉碱的药代动力学和安全性。血浆肉碱的日内个体差异较小（变异系数分别为3.0%、3.9%和3.9%），24小时尿总排泄量也较少且相对恒定：单盲设计下，仅给予生理盐水的三名受试者中，对照组尿排泄量分别为4.6、21.5和13.0mg/天，治疗期间分别为4.6、20.2和6.0mg/天。因此，药代动力学分析时从给药后的水平中减去给药前的肉碱水平。血浆肉碱很好地符合三室开放模型，中央室容积（Vc）为0.11 - 0.20l/kg，消除相半衰期（t1/2γ）为10 - 23小时。24小时尿回收率为77.2% - 95.4%。没有可归因于肉碱的客观或主观副作用，因此其静脉输注被认为是安全的。
