Strong J M, Dutcher J S, Lee W K, Atkinson A J
Clin Pharmacol Ther. 1975 Nov;18(5 Pt 1):613-22. doi: 10.1002/cpt1975185part1613.
Absorption of a single oral dose of N-acetylprocainamide (NAPA) was studied in 3 normal subjects. Approximately 85% of the oral dose was absorbed and peak plasma NAPA concentrations were reached in 45 to 90 min. In 2 subjects, NAPA was absorbed at a fast initial rate, then more slowly, prolonging the apparent elimination phase half-life. Absolute bioavailability was determined by a new stable isotope method that entailed intravenous injection of NAPA 13C at the same time that an unlabeled NAPA capsule was given orally. Plasma levels and urine excretion of both compounds were determined by mass fragmentography. Bioavailability was assessed by deconvoluting the plasma level vs time curves resulting from intravenous and oral drug administration, and also by comparing the relative percentage of NAPA and NAPA-13C excreted unchanged in the 24 hr after simultaneous administration.
在3名正常受试者中研究了单次口服N-乙酰普鲁卡因胺（NAPA）的吸收情况。口服剂量的约85%被吸收，血浆NAPA浓度在45至90分钟内达到峰值。在2名受试者中，NAPA最初以快速吸收，随后吸收变慢，延长了表观消除相半衰期。绝对生物利用度通过一种新的稳定同位素方法测定，该方法在口服未标记的NAPA胶囊的同时静脉注射13C标记的NAPA。两种化合物的血浆水平和尿排泄通过质谱分析法测定。生物利用度通过对静脉内和口服给药产生的血浆水平与时间曲线进行反卷积来评估，也通过比较同时给药后24小时内未改变排泄的NAPA和NAPA-13C的相对百分比来评估。
