Gulaid A A, James I M, Kaye C M, Lewellen O R, Roberts E, Sankey M, Smith J, Templeton R, Thomas R J
Biopharm Drug Dispos. 1981 Apr-Jun;2(2):103-14. doi: 10.1002/bdd.2510020202.
The pharmacokinetics of acebutolol have been studied in eight healthy male volunteers following the oral administration of acebutolol hydrochloride ('Sectral', May & Baker) as a single dose (400 mg), and during and after repeated oral dosing (400 mg, b.d. for 56 days). Following single dose administration, considerable inter-subject variation in plasma levels of parent drug and the major metabolite, diacetolol, was evident. Acebutolol appeared to be eliminated from plasma in a bi-phasic manner, and this was confirmed from urinary excretion rate data. Mean initial and terminal half-lives of about 2 and 11 h, respectively, were determined. Plasma levels of diacetolol were greater than those of parent drug from 3 to 4 h following dose administration. Total urinary excretion of diacetolol was generally greater than that of acebutolol. During repeated dosing, steady-state plasma levels of acebutolol and diacetolol were achieved in 6 volunteers. Acebutolol did not appear to stimulate or inhibit its metabolism.
在八名健康男性志愿者中研究了醋丁洛尔的药代动力学。单次口服盐酸醋丁洛尔（“Sectral”，May & Baker公司生产）400毫克后，以及在重复口服给药期间（400毫克，每日两次，共56天）和给药后，均进行了相关研究。单次给药后，母体药物和主要代谢物双醋洛尔的血浆水平在受试者之间存在明显差异。醋丁洛尔似乎以双相方式从血浆中消除，这一点从尿排泄率数据得到了证实。分别测定出平均初始半衰期和终末半衰期约为2小时和11小时。给药后3至4小时，双醋洛尔的血浆水平高于母体药物。双醋洛尔的总尿排泄量通常高于醋丁洛尔。在重复给药期间，6名志愿者达到了醋丁洛尔和双醋洛尔的稳态血浆水平。醋丁洛尔似乎并未刺激或抑制其自身代谢。
