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抗酸剂和食物对人体中丙酰嗪(Biarison)吸收的影响。

The effect of antacid and food on the absorption of proquazone (Biarison) in man.

作者信息

Ohnhaus E E

出版信息

Int J Clin Pharmacol Ther Toxicol. 1980 Mar;18(3):136-9.

PMID:7380586
Abstract

The study was carried out on a group of twelve healthy volunteers in order to determine the effect of food and antacid on the absorption of proquazone when administered orally as a single dose. Each subject received, in a randomised cross-over sequence, 600 mg of proquazone after a 10 h overnight fast, 15 min. after 20 ml of an antacid (Maaloxan) and 15 min. after a standard breakfast. The interval between each administration was at least 7 days. Blood plasma samples were obtained up to 24 hours after administration. The samples were analysed using a modified fluorimetric method which determined the amount of unchanged drug. The only effect of antacid, compared to fasting, was to slow the rate of absorption without appreciably altering the extent of absorption. Food, on the other hand, markedly increased the maximal plasma concentration and also the area under the plasma concentration/time curve in a statistically significant and, most probably, clinically relevant manner. Possible explanations for this effect are discussed and it is concluded that the administration of proquazone with or after food should be doubly advantageous for the patient as it ought to offer protection from local gastrointestinal irritation and at the same time lead to an enhanced bioavailability.

摘要

该研究针对一组12名健康志愿者开展,目的是确定单剂量口服普罗喹宗时食物和抗酸剂对其吸收的影响。每位受试者在禁食10小时过夜后,分别在服用20毫升抗酸剂(胃得乐)15分钟后以及标准早餐后15分钟,以随机交叉顺序服用600毫克普罗喹宗。每次给药间隔至少7天。给药后24小时内采集血浆样本。使用改良荧光法分析样本,该方法可测定未变化药物的量。与禁食相比,抗酸剂唯一的作用是减缓吸收速率,而未明显改变吸收程度。另一方面,食物显著提高了最大血浆浓度,并且以具有统计学意义且极有可能具有临床相关性的方式增加了血浆浓度/时间曲线下面积。文中讨论了这种效应的可能解释,并得出结论:普罗喹宗与食物同服或在进食后服用对患者应该有双重益处,因为这样既能防止局部胃肠道刺激,同时又能提高生物利用度。

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