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首页> 外文期刊>British Journal of Clinical Pharmacology >Effect of single and multiple doses of elobixibat, an ileal bile acid transporter inhibitor, on chronic constipation: A randomized controlled trial
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Effect of single and multiple doses of elobixibat, an ileal bile acid transporter inhibitor, on chronic constipation: A randomized controlled trial

机译：单药和多剂量Elobixibat，髂骨胆汁酸转运蛋白抑制剂，慢性便秘：随机对照试验

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Aims Elobixibat is a minimally absorbed ileal bile acid transporter inhibitor. This study aimed to investigate the safety, tolerability, efficacy, pharmacokinetics and pharmacodynamics of elobixibat in Japanese patients with chronic constipation. Methods This study consisted of single‐dose and multiple‐dose tests with a dose‐escalating design. Sixty patients including females and males were randomized into five dose levels of elobixibat (2.5, 5, 10, 15 or 20?mg, n ?=?10 per level) and corresponding placebo ( n ?=?2 per group). A crossover design was used to examine food effect in single‐dose test. Patients received test tablets once daily for 14?days in multiple‐dose test. We assessed pharmacokinetic‐dose proportionality, levels of serum high‐ and low‐density lipoprotein cholesterol and plasma 7α‐hydroxy‐4‐cholesten‐3‐one (C4), food effect and sex‐specific effect. Adverse events and bowel functions such as bowel movements, stool consistency and straining were also evaluated. Results Food consumption reduced systemic exposure by around 80% [e.g. least squares mean (ratio of breakfast/no breakfast) maximum plasma concentration: 0.2085 (90% confidence interval, 0.1371–0.3172) at 15?mg] while increased plasma C4 level ( P ??0.001). In the multiple‐dose test, elobixibat reduced low‐density lipoprotein cholesterol and increased C4 whilst unaltering high‐density lipoprotein cholesterol level. The increased spontaneous bowel movement frequency was correlated with higher dosage and higher C4 level (R 2 ?=?0.5929 at Week 2). Adverse events were mainly gastrointestinal symptoms, most of which were mild. Conclusions Elobixibat should be taken before breakfast. Once‐daily administration of elobixibat was found to be safe and tolerated up to 20?mg in female and male patients with chronic constipation.
机译：AIMS Elobixibat是一种微量吸收的髂骨胆汁酸转运蛋白。本研究旨在探讨日本慢性便秘患者Elobixibat的安全性，耐受性，疗效，药代动力学和药物动力学。方法本研究由单剂量和多剂量试验组成，具有剂量升级的设计。 60例患者包括女性和男性，随机分为5剂量水平的Elobixibat（2.5,5,10,15或20？Mg，N？= 10％）和相应的安慰剂（每组N？=？2）。交叉设计用于检查单剂量测试中的食物效果。患者在多剂量测试中每天一次接受一次测试片剂。我们评估了药代动力学剂量比例，血清高和低密度脂蛋白胆固醇和血浆7α-羟基-4-胆固醇-3-一（C4），食物效应和性特异性效应。还评估了诸如肠道运动，粪便一致性和紧张的不良事件和肠功能。结果食品消耗减少了系统性暴露约80％[例如最小二乘意味着（早餐比/无早餐）最大等离子体浓度：在15μmg/ mg的血浆中的0.2085（90％置信区间，0.1371-0.3172），同时增加等离子体C4水平（p≤≤0.001）。在多剂量试验中，Elobixibat降低了低密度脂蛋白胆固醇，并且在膨胀高密度脂蛋白胆固醇水平上增加C4。增加的自发性肠道运动频率与较高剂量和更高的C4水平相关（R 2？=Δ= 0.5929）。不良事件主要是胃肠道症状，其中大部分是轻微的。结论Elobixibat应该在早餐前服用。发现Elobixibat的每日施用是安全的，并且在慢性便秘的女性和男性患者中可安全和耐受20μmg。

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