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首页> 外文期刊>The Canadian journal of clinical pharmacology =: Journal canadien de pharmacologie clinique >Effect of moderate hepatic insufficiency on the pharmacokinetics of sitagliptin
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Effect of moderate hepatic insufficiency on the pharmacokinetics of sitagliptin

机译：中度肝功能不全对西他列汀药代动力学的影响

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Background Sitagliptin is a highly selective dipeptidyl peptidase-4 inhibitor for the treatment of patients with type 2 diabetes. Sitagliptin is primarily excreted by renal elimination as unchanged drug, with only a small percentage (～16%) undergoing hepatic metabolism. Objectives The primary purpose of this study was to evaluate the influence of moderate hepatic insufficiency on the pharmacokinetics of sitagliptin. Methods In an open-label study, a single 100-mg oral dose of sitagliptin was administered to 10 male or female patients with moderate hepatic insufficiency (Child-Pugh's scores ranged from 7 to 9) and 10 healthy control subjects matched to each patient for race, gender, age (± 5 yrs) and body mass index (BMI kg/m 2 ± 5%). After administration of each dose, blood and urine samples were collected to assess sitagliptin pharmacokinetics. Results The mean AUC 0-∞ and C max for sitagliptin were numerically, but not significantly (p0.050), higher in patients with moderate hepatic insufficiency compared with healthy matched control subjects by 21% and 13%, respectively. These slight differences were also not considered to be clinically meaningful. Moderate hepatic insufficiency had no statistically significant effect on the T max, apparent terminal t1/2, fraction of the oral dose excreted into urine (f e,0-∞) and renal clearance (C1r) (p0.100) of sitagliptin. Sitagliptin was generally well tolerated by both patients and subjects; all adverse experiences were transient and rated as mild in intensity. Conclusions Moderate hepatic insufficiency has no clinically meaningful effect on the pharmacokinetics ofsitagliptin.
机译：背景西格列汀是用于治疗2型糖尿病患者的高度选择性二肽基肽酶4抑制剂。西他列汀主要通过肾脏排泄作为不变药物排泄，只有一小部分（〜16％）进行肝代谢。目的这项研究的主要目的是评估中度肝功能不全对西他列汀药代动力学的影响。方法在一项开放标签研究中，对10例中度肝功能不全（Child-Pugh评分范围为7至9）的男性或女性患者单次口服100 mg西他列汀，并与10例健康对照者匹配，以种族，性别，年龄（±5岁）和体重指数（BMI kg / m 2±5％）。每次给药后，收集血液和尿液样本以评估西他列汀的药代动力学。结果中度肝功能不全患者的西他列汀平均AUC0-∞和C max数值，但不显着（p> 0.050），分别比健康对照者高21％和13％。这些细微的差异也不被认为具有临床意义。中度肝功能不全对西他列汀的T max，表观终末t1 / 2，排入尿液的口服剂量比例（f e，0-∞）和肾清除率（C1r）（p <0.100）均无统计学意义。西他列汀通常被患者和受试者耐受。所有不良经历都是短暂的，强度为轻度。结论中度肝功能不全对西他列汀的药代动力学没有临床意义。

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