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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist.
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Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist.

机译：食物摄入量和配方对双重内皮素受体拮抗剂波生坦的药代动力学和代谢的影响。

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摘要

The purpose of the study was to investigate the effect of food intake on the pharmacokinetics and metabolism as well as the relative bioavailability of bosentan. Sixteen healthy male subjects were treated in a randomized, four-way, crossover design with single oral doses of 125 mg bosentan, given as one tablet (with or without food), two tablets of 62.5 mg (with food), and a suspension (without food). The pharmacokinetic parameters of bosentan (and also three of its metabolites) were very similar after the four treatments: geometric means for Cmax and AUC0-infinity, ranged from 1.3 to 1.6 microg/ml and from 7.8 to 8.9 microg x h/ml, respectively, and median t(max) from 3.0 to 4.0 hours. The bioavailability of the 125 mg tablet relative to that of the suspension, both given fasted, was 102%. In the presence of food, Cmax and AUC0-max increased by 22% and 10%, respectively, whereas the two 62.5 mg tablets were bioequivalent to the 125mg tablet, both under fed conditions. The pharmacokinetics of the metabolites was independent of the treatment administered. In conclusion, bosentan bioavailability from the newly developed 125 mg tablet formulation is similar to that of the suspension, and food intake does not influence its pharmacokinetics to a clinically relevant extent.
机译：该研究的目的是研究食物摄入对波生坦的药代动力学和代谢以及相对生物利用度的影响。 16名健康男性受试者采用随机，四向，交叉设计治疗，单次口服剂量为125 mg波生坦，分别为一片（含或不含食物），两片62.5 mg（含食物）和混悬液（没有食物）。在四种处理之后，波生坦（及其三种代谢物）的药代动力学参数非常相似：Cmax和AUC0-无穷大的几何平均值分别为1.3至1.6 microg / ml和7.8至8.9 microg xh / ml，且t（max）中值从3.0到4.0小时不等。禁食的125毫克片剂相对于悬浮液的生物利用度均为102％。在有食物的情况下，在进食条件下，Cmax和AUC0-max分别增加了22％和10％，而两个62.5 mg的片剂与125mg的片剂具有生物等效性。代谢物的药代动力学与所给予的治疗无关。总之，新开发的125 mg片剂的波生坦生物利用度与混悬液相似，食物摄入不会在临床上影响药物动力学。

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