Yacobi A, Stampfli H F, Lai C M, Kamath B L
Drug Metab Dispos. 1981 May-Jun;9(3):193-5.
The purpose of this study was to determine the distribution of N-acetylprocainamide (NAPA) in heart, kidney, and liver tissues of rats and their relationship to the plasma concentration after intravenous administration of the drug (100 mg/kg) to 24 Charles River rats. A specific HPLC procedure was used. The plasma and tissue concentrations of NAPA declined biexponentially in parallel, with an elimination half-life of about 1.8 hr. The equilibrium between plasma and the organs tested in this study was attained within 5 min. The tissue/plasma concentration ratio remained constant throughout the study. The tissue/plasma ratios for heart, kidney, and liver were 2.1, 7.9, and 2.4, respectively. The data indicate that: a) these organs have greater affinity to NAPA than do plasma proteins, and b) plasma concentrations may be reliable measures of the therapeutically effective concentrations at the site of action, i.e., the heart tissues.
本研究的目的是确定在给24只查尔斯河大鼠静脉注射药物（100mg/kg）后，N-乙酰普鲁卡因胺（NAPA）在大鼠心脏、肾脏和肝脏组织中的分布及其与血浆浓度的关系。采用了一种特定的高效液相色谱法。NAPA的血浆和组织浓度呈双指数平行下降，消除半衰期约为1.8小时。本研究中血浆与受试器官之间的平衡在5分钟内达到。在整个研究过程中，组织/血浆浓度比保持恒定。心脏、肾脏和肝脏的组织/血浆比分别为2.1、7.9和2.4。数据表明：a）这些器官对NAPA的亲和力高于血浆蛋白，b）血浆浓度可能是作用部位（即心脏组织）治疗有效浓度的可靠指标。
