Dockens Randy C, Salazar Daniel E, Fulmor I Edgar, Wehling Michele, Arnold Mark E, Croop Robert
Bristol-Myers Squibb Comapny, Princeton, NJ 08543, USA.
J Clin Pharmacol. 2006 Nov;46(11):1308-12. doi: 10.1177/0091270006292250.
The objective of this study was to assess the pharmacokinetics of a newly identified active metabolite of buspirone, 6-hydroxybuspirone (6OHB), over the therapeutic dose range of buspirone. A 26-day, open-label, nonrandomized, single-sequence, dose-escalation study in normal healthy volunteers was conducted (N = 13). Subjects received escalating doses of buspirone with each dose administered for 5 days starting at a dose of 5 mg twice daily and increasing up to 30 mg twice daily. Plasma concentrations of 6OHB were approximately 40-fold greater than those of buspirone. 6OHB was rapidly formed following buspirone administration, and exposure increased proportionally with buspirone dose. Further research regarding the safety and efficacy of 6OHB itself is warranted.
本研究的目的是评估丁螺环酮新鉴定的活性代谢物6-羟基丁螺环酮（6OHB）在丁螺环酮治疗剂量范围内的药代动力学。在正常健康志愿者中进行了一项为期26天的开放标签、非随机、单序列、剂量递增研究（N = 13）。受试者接受递增剂量的丁螺环酮，从每日两次5 mg的剂量开始，每次剂量给药5天，直至每日两次30 mg。6OHB的血浆浓度比丁螺环酮高约40倍。服用丁螺环酮后6OHB迅速形成，且暴露量随丁螺环酮剂量成比例增加。有必要对6OHB本身的安全性和有效性进行进一步研究。
