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健康志愿者体内S-腺苷-L-甲硫氨酸的药代动力学

Pharmacokinetics of S-adenosyl-L-methionine in healthy volunteers.

作者信息

Giulidori P, Cortellaro M, Moreo G, Stramentinoli G

出版信息

Eur J Clin Pharmacol. 1984;27(1):119-21.

PMID:6489422
Abstract

S-Adenosyl-L-methionine (AdoMet) kinetics was studied in 6 male subjects given 100 and 500 mg i.v. Drug concentrations in plasma and urine were assayed using a radioenzymatic method. Pharmacokinetic parameters were estimated according to an open two-compartment model. The apparent volumes of distribution after the 100 and 500 mg doses were 407 +/- 27 and 443 +/- 36 ml/kg (mean +/- SEM), terminal half-lives 81 +/- 8 and 101 +/- 7 min and body clearances 3.7 +/- 0.5 and 3.1 +/- 0.2 ml/min per kg. Urinary excretion was 34 +/- 3 and 40 +/- 2% of the administered dose. The results demonstrate that drug disposition occurs more via metabolism than via renal excretion, and it is not dependent on the administered dose. Binding of AdoMet to serum proteins is negligible.

摘要

对6名男性受试者静脉注射100毫克和500毫克的S-腺苷-L-甲硫氨酸(AdoMet)后,研究了其动力学。采用放射酶法测定血浆和尿液中的药物浓度。根据开放二室模型估算药代动力学参数。100毫克和500毫克剂量后的表观分布容积分别为407±27和443±36毫升/千克(平均值±标准误),末端半衰期分别为81±8和101±7分钟,机体清除率分别为3.7±0.5和3.1±0.2毫升/分钟/千克。尿排泄量分别为给药剂量的34±3%和40±2%。结果表明,药物处置更多地通过代谢而非肾排泄发生,且不依赖于给药剂量。AdoMet与血清蛋白的结合可忽略不计。

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