Block W, Pingoud A, Khan M, Kjellerup P
Arzneimittelforschung. 1981;31(6):1041-5.
The pharmacokinetics of 4-amino-5-chloro-N-(2-diethylaminoethyl)-2-methoxybenzamide (metoclopramide, Paspertin) after a single dose of the drug in five different dosage forms: ampoules, tablets, drops, dragées and suppositories, were studied. The clinical investigations were carried out on 10 healthy subjects under carefully controlled conditions. The analysis of metoclopramide in plasma was carried out using reverse-phase high-pressure liquid chromatography. Bioavailabilities between 76 and 79% were determined for the oral application forms and 53% for the rectal application form. Significant differences between maximum plasma levels were found for different individuals. The initial distribution of the drug is very rapid, and the elimination half-lives are comparable for all formulations and ranged from 3.9 and 5.3 h. The apparent volume of distribution is 3.1 l/kg body weight and the total body clearance is 38.4 l/h.
研究了单剂量的4-氨基-5-氯-N-(2-二乙氨基乙基)-2-甲氧基苯甲酰胺（胃复安，灭吐灵）在五种不同剂型：安瓿剂、片剂、滴剂、糖衣丸剂和栓剂中的药代动力学。临床研究在10名健康受试者身上，在严格控制的条件下进行。采用反相高压液相色谱法对血浆中的胃复安进行分析。口服剂型的生物利用度在76%至79%之间，直肠剂型的生物利用度为53%。不同个体的最大血浆水平存在显著差异。药物的初始分布非常迅速，所有制剂的消除半衰期相当，范围为3.9至5.3小时。表观分布容积为3.1升/千克体重，全身清除率为38.4升/小时。
