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首页> 外文期刊>Pulmonary pharmacology & therapeutics >MK-0873, a PDE4 inhibitor, does not influence the pharmacokinetics of theophylline in healthy male volunteers.
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MK-0873, a PDE4 inhibitor, does not influence the pharmacokinetics of theophylline in healthy male volunteers.

机译：MK-0873，一种PDE4抑制剂，不会影响健康男性志愿者中茶碱的药代动力学。

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BACKGROUND: MK-0873 is a novel selective phosphodiesterase-4 inhibitor, which has been in development for the treatment of chronic obstructive pulmonary disease (COPD). In this indication, theophylline is still an important treatment, despite its relatively small therapeutic window. In view of this, it is important to investigate whether MK-0873 could affect the pharmacokinetics, safety and tolerability of theophylline, when both drugs are given concomitantly. AIM: The objective of this study was to investigate the effect of multiple doses of oral MK-0873, a selective phosphodiesterase-4 inhibitor, on the pharmacokinetics, safety and tolerability profile of orally administered theophylline in healthy volunteers. METHODS: Eight healthy, non-smoking male subjects participated in this randomized, open-label, 2-period, cross-over study. In one period subjects received an oral dose of 2.5mg MK-0873 for 6 days co-administered with a single oral dose of 250mg theophylline on day 5. The other period consisted of a single dose of 250mg theophylline on day 1. In each period, blood samples were collected at predefined time points to evaluate theophylline pharmacokinetics. RESULTS: All subjects completed the study. The study medications were generally well tolerated and no clinically relevant changes were observed in either treatment periods. No significant difference was found in the AUC 0-infinity (77.7 vs. 83.8h ng/ml; p=0.280) and C(max) (6.70 vs. 7.77ng/ml; p=0.125) of theophylline between the MK-0873+theophylline and theophylline only treatment, and bioequivalence was demonstrated for AUC0-infinity (geometric mean ratio with 90% confidence interval: 0.930 (0.826, 1.047)). CONCLUSION: In this study, in a limited number of subjects, co-administration of oral MK-0873 did not affect the pharmacokinetics, safety, and tolerability of oral theophylline in non-smoking healthy male subjects.
机译：背景：MK-0873是一种新型的选择性磷酸二酯酶-4抑制剂，已被开发用于治疗慢性阻塞性肺疾病（COPD）。在这种适应症中，尽管茶碱的治疗窗口相对较小，但茶碱仍然是一种重要的治疗方法。有鉴于此，当同时使用两种药物时，研究MK-0873是否会影响茶碱的药代动力学，安全性和耐受性非常重要。目的：本研究的目的是研究多剂量口服MK-0873（一种选择性磷酸二酯酶4抑制剂）对健康志愿者口服茶碱的药代动力学，安全性和耐受性的影响。方法：八名健康，不吸烟的男性受试者参加了这项随机，开放标签，二期，交叉研究。在一个时期中，受试者在第5天接受了2.5毫克MK-0873的口服剂量，并在第5天与250毫克茶碱的单次口服剂量合用。另一时期在第1天接受了250毫克茶碱的单次剂量。在预定的时间点采集血样以评估茶碱的药代动力学。结果：所有受试者均完成研究。研究药物通常耐受良好，在两个治疗期间均未观察到临床相关变化。在MK-0873之间，茶碱的AUC 0-无穷大（77.7对83.8h ng / ml; p = 0.280）和茶碱的C（max）（6.70对7.77ng / ml; p = 0.125）没有显着差异。 +茶碱和仅茶碱治疗，并证明了AUC0-无穷大的生物等效性（90％置信区间的几何平均比：0.930（0.826，1.047））。结论：在本研究中，在少数受试者中，口服MK-0873的共同给药不会影响非吸烟健康男性受试者口服茶碱的药代动力学，安全性和耐受性。

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