Marzo A, Arrigoni Martelli E, Urso R, Rocchetti M, Rizza V, Kelly J G
Real srl, Drug Metabolism and Pharmacokinetics Laboratory, Villaguardia, Como, Italy.
Eur J Clin Pharmacol. 1989;37(1):59-63. doi: 10.1007/BF00609426.
The pharmacokinetics of acetyl-L-carnitine hydrochloride were investigated in 6 healthy volunteers of both sexes after i.v. injection of 500 mg of the drug, expressed as inner salt. Plasma concentrations and urinary excretion of acetyl-L-carnitine (A), L-carnitine (B) and total acid soluble L-carnitine fraction were evaluated over a period lasting from 24 h before to 48 h after the administration. Plasma concentrations of A increased quickly after administration and then declined reaching base values within 12 h. Conversely, plasma concentrations of B rose more slowly, reaching a peak in 30-60 min, and then declined to base values within 24 h. Most of the injected dose of acetyl-L-carnitine was recovered in the urine during the first 24 h after administration as B and A. Mean renal clearance of both A and B during the first 12 h after injection was higher than the base values, suggesting the presence of a saturable tubular reabsorption process which may counterbalance major changes occurring in plasma concentrations of L-carnitine pattern.
对6名男女健康志愿者静脉注射500mg以内盐形式存在的盐酸乙酰左旋肉碱后，研究了其药代动力学。在给药前24小时至给药后48小时期间，评估了乙酰左旋肉碱（A）、左旋肉碱（B）和总酸溶性左旋肉碱组分的血浆浓度及尿排泄情况。给药后，A的血浆浓度迅速升高，然后下降，在12小时内达到基线值。相反，B的血浆浓度上升较慢，在30 - 60分钟内达到峰值，然后在24小时内降至基线值。给药后24小时内，大部分注射剂量的乙酰左旋肉碱以B和A的形式在尿液中回收。注射后前12小时内，A和B的平均肾清除率均高于基线值，表明存在可饱和的肾小管重吸收过程，该过程可能抵消左旋肉碱模式血浆浓度发生的主要变化。
