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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >A comparative multidose pharmacokinetic study of buspirone extended-release tablets with a reference immediate-release product.
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A comparative multidose pharmacokinetic study of buspirone extended-release tablets with a reference immediate-release product.

机译：丁螺环酮缓释片与参考速释产品的比较多剂量药代动力学研究。

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Buspirone is disclosed in U.S. Patent No. 3,717,634 as a pharmaceutically active compound that has been found to be effective for the treatment of anxiety disorders and depression. In this randomized, two-treatment, two-period, multidose crossover study, the pharmacokinetics of a once-daily extended-release (ER)formulation of buspirone was compared with that of an immediate-release (IR) formulation of commercially available buspirone. A total of 30 mg of the ER formulation was administered to 36 healthy volunteers once daily for 7 days, and 15 mg of the IR formulation was administered twice daily for 7 days. Pharmacokinetic profiles of buspirone and its metabolite, 1-pyrimidinylpiperazine (1-PP), were obtained at steady state. The bioavailability of buspirone from the ER formulation was more than three times higher than that from the IR formulation at steady state, and that of 1-PP was about 25% less. The mean steady-state Cmax of buspirone from the ER formulation was 46% higher than that from the IR formulation (p < 0.05), and that for 1-PP was lower by 29% (p < 0.05). The mean apparent half-life of buspirone from the ER formulation (9.04 hours) was considerably longer than that observed for the IR formulation (3.06 hours). The median 1-PP/buspirone AUC ratio was much higher for the IR formulation at steady state (24.4) than for the ER formulation (6.44). There were no significant differences in average pharmacokinetic metrics observed in men and women. Based on these observations of the potential benefits of once-daily dosing with the ER product in terms of prolonged buspirone plasma concentrations, a significant increase in the ratio of buspirone to 1-PP concentration with a lower intersubject variation could be achieved that should provide an improvement in the desired therapeutic effects of buspirone.
机译：在美国专利号3,717,634中公开了丁螺环酮作为药物活性化合物，已发现其可有效治疗焦虑症和抑郁症。在这项随机，两次治疗，两个时期的多剂量交叉研究中，比较了丁螺环酮的每日一次缓释（ER）制剂与市售丁螺环酮的速释（IR）制剂的药代动力学。每天一次向36位健康志愿者给药30毫克的ER制剂，共7天，每天两次给药15毫克的IR制剂，共7天。在稳态下获得了丁螺环酮及其代谢产物1-嘧啶基哌嗪（1-PP）的药代动力学概况。稳态条件下，ER制剂中丁螺环酮的生物利用度比IR制剂高3倍以上，而1-PP的生物利用度低约25％。 ER制剂中丁螺环酮的平均稳态Cmax比IR制剂中的平均稳态Cmax高46％（p <0.05），而1-PP的丁苯吡酮的稳态Cmax降低29％（p <0.05）。 ER制剂中丁螺环酮的平均表观半衰期（9.04小时）比IR制剂（3.06小时）明显更长。在稳定状态下，IR制剂（24.4）的中位1-PP /丁螺环酮AUC比率要比ER制剂（6.44）高得多。男性和女性的平均药代动力学指标没有显着差异。基于这些观察结果，就长期使用丁螺环酮血浆浓度而言，每天服用ER产品的潜在好处是，可以显着增加丁螺环酮与1-PP浓度之比，且受试者间差异较小，从而应丁螺环酮所需治疗效果的改善。

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