比伐卢定序贯给药在中国健康受试者中的药代、药效及安全性研究

中国临床药理学与治疗学 ›› 2014, Vol. 19 ›› Issue (7): 785-788.

比伐卢定序贯给药在中国健康受试者中的药代、药效及安全性研究

柴栋¹, 王睿², 白楠², 梅和坤²

¹ 解放军总医院海南分院药剂科, 三亚 572013,海南;
² 解放军总医院药物临床研究中心,北京 100856

收稿日期:2013-09-07 修回日期:2014-06-20 发布日期:2014-07-21
通讯作者: 袁力勇,男,主任医师,主要研究方向:麻醉药理学。 Tel: 13967804761 　E?mail: ylysgl@hotmail.com
作者简介:柴栋,男,博士,副主任药师,主要从事临床药理学研究。 Tel: 010-66939670 E-mail: chaid@sohu.com

Pharmacokinetics, pharmacodynamics and safety of bivalirudin sequential regimen in Chinese healthy volunteers

CHAI Dong¹, WANG Rui², BAI Nan², MEI He-kun²

¹ Department of Pharmacy, Hainan Branch of PLA General Hospital, Sanya 572013, Hainan;
² Department of Drug Clinical Trial Center of PLA General Hospital, Beijing 100853,China

Received:2013-09-07 Revised:2014-06-20 Published:2014-07-21

摘要/Abstract

摘要： 目的探讨合理的比伐卢定临床序贯给药方案。方法筛选健康受试者12名,给予比伐卢定 0.75 mg/kg 静脉推注后,1.75 mg·kg^-1·h^-1的速度匀速静滴 4 h,不同时间点采集血样,测定血药浓度、活性凝血时间(ACT)及凝血功能,计算药代动力学、药效学参数,同时观察试验期间的不良事件。结果序贯给药期间药-时曲线与时-效曲线吻合良好,ACT稳定在220~240 s,药效动力学符合M-M equation模型。试验期间未出现严重不良事件,凝血功能于停药后24 h恢复至正常水平。结论比伐卢定序贯给药(0.75 mg/kg 静脉推注后,1.75 mg·kg^-1·h^-1 静滴)的药效及安全性能够满足临床要求。

关键词: 比伐卢定, 序贯给药, 活性凝血时间

Abstract: AIM: To investigate the reasonable sequential regimen of bivalirudin in clinic. METHODS: 12 Chinese healthy volunteers were selected. During bivalirudin administration (0.75 mg/kg bolus followed by a 1.75 mg·kg^-1·h^-1 infusion for 4 h), blood samples were collected in regular time, and blood concentration of bivalirudin, active coagulation time (ACT) and function were measured. Then the primary pharmacokinetic parameters were caculated using WinNonlin 5.2.1. The adverse events were observed during the clinical trial.RESULTS:The time-effect curves and time-concentration curve of bivalirudin in this clinical trial were paralleled. The ACT was 220-240 s steadily respectively. During the clinical trial, there were no serve adverse events, and the coagulation function recovered to normal after 24 h. CONCLUSION: Bivalirudin sequential regimen (0.75 mg/kg bolus followed by a 1.75 mg·kg^-1·h^-1 infusion for 4 h) is effective and safe for clinic.

Key words: bivalirudin, sequential regimen, active coagulation time (ACT)

中图分类号:

R969.1

柴栋, 王睿, 白楠, 梅和坤. 比伐卢定序贯给药在中国健康受试者中的药代、药效及安全性研究[J]. 中国临床药理学与治疗学, 2014, 19(7): 785-788.

CHAI Dong, WANG Rui, BAI Nan, MEI He-kun. Pharmacokinetics, pharmacodynamics and safety of bivalirudin sequential regimen in Chinese healthy volunteers[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2014, 19(7): 785-788.

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