Pharmacokinetics of a newly identified active metabolite of buspirone after administration of buspirone over its therapeutic dose range
Pharmacokinetics of a newly identified active metabolite of buspirone after administration of buspirone over its therapeutic dose range
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DOI：
10.1177/0091270006292250
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发表时间：
2006-11-01
影响因子：
2.9
通讯作者：
Croop, Robert
中科院分区：
文献类型：
--
作者：
Dockens, Randy C.;Salazar, Daniel E.;Croop, Robert
本研究的目的是评估在丁螺环酮治疗剂量范围内，丁螺环酮新鉴别的活性代谢产物6-羟基丁螺环酮（6 OHB）的药代动力学。在正常健康志愿者中进行了一项为期26天、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，每次给药5天，从5 mg每日两次开始，增加至30 mg每日两次。6 OHB的血浆浓度约为丁螺环酮的40倍。丁螺环酮给药后，6 OHB迅速形成，暴露量随丁螺环酮剂量成比例增加。关于6 OHB本身的安全性和有效性的进一步研究是必要的。
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.