药理学
药代动力学
药效学
部分凝血活酶时间
医学
效力
分配量
尿
凝血酶原时间
生物利用度
交叉研究
化学
内科学
生物化学
血小板
替代医学
病理
体外
安慰剂
作者
Hongyun Wang,Ning Ou,Liwei Lang,Ruihua Shi,Pei Hu,Ji Jiang
出处
期刊:Xenobiotica
[Informa]
日期:2016-03-21
卷期号:46 (12): 1133-1141
被引量:10
标识
DOI:10.3109/00498254.2016.1156185
摘要
1. Ilaprazole is a novel proton pump inhibitor and this is the first study to investigate the pharmacokinetics, pharmacodynamics and safety of intravenous ilaprazole in healthy volunteers. 2. In this open-label, single-dose, randomized and four-period crossover study, 16 healthy Chinese subjects received ilaprazole 5, 10 or 20 mg intravenously, or 10 mg orally. Serial blood and urine samples were collected and intragastric pH was recorded within 24 h. The percentage time of intragastric pH > 6 was the major index. Safety was assessed throughout the study. 3. Plasma exposure of intravenous ilaprazole increased proportionally over the dose of 5-20 mg. Clearance and volume of distribution were independent of dose. Ilaprazole was not eliminated through urine and the absolute bioavailability was 55.2%. For the intravenous dose of 5, 10, 20 mg, and oral dose of 10 mg, the mean percentages time of intragastric pH > 6 were 47.3%, 52.8%, 68.2% and 47.5%, respectively. 4. Ilaprazole showed linear pharmacokinetics over the dose of 5-20 mg. Intravenous ilaprazole provided rapid onset of action and the potency of effect were exhibited in a dose-dependent manner. Intravenous ilaprazole was safe and well tolerated except for elevated activated partial thromboplastin time (APTT) and prothrombin time (PT).
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