雷诺嗪在健康人体的药代动力学  

Pharmacokinetics of ranolazine in healthy volunteers

作　　者：侯文静[1,2] 李扬[2] 胡欣[2] 史爱欣[2] 

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]卫生部北京医院药学部,北京100730

出　　处：《中国临床药理学杂志》2013年第5期342-344,349,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家科技部“重大新药创制”科技重大专项基金资助项目(2012ZX09303-008-002)

摘　　要：目的评价中国健康人单剂量口服雷诺嗪缓释片后体内的药代动力学。方法随机双盲单中心Ⅰ期临床研究,2名受试者口服安慰剂,8名受试者单次口服雷诺嗪缓释片1500 mg后,用LC-MS-MS法测定血浆中雷诺嗪浓度,用WinNonlin6.3软件对血药浓度数据进行处理,计算药代动力学参数。结果血浆中雷诺嗪浓度线性范围为5～4000 ng.mL-1,定量下限为5 ng.mL-1,日内、日间精密度均小于15%。主要的药代动力学参数:Cmax为(1.27±0.50)mg.mL-1,tmax为(3.13±1.55)h,t1/2为(5.02±1.47)h,V为(0.74±0.35)L,CL为(0.10±0.05)L.h-1,AUC0-48为(17.50±8.31)mg.h.mL-1。结论本方法操作简便、快捷、灵敏度高,可用于雷诺嗪缓释片在中国健康受试者体内药代动力学的研究。Objective To establish study pharmacokinetics after admin- istration of ranolazine sustained release tablets at a single dose to healthy Chinese volunteers. Methods The concentration of ranolazine in plasma was determined by LC - MS - MS method after administration of ranolazine sustained release tablets at a single doses via oral to 8 healthy vol- unteers. The concentration -time curves were simulated and the pharma- eokinetic parameters were calculated by WinNonlin 6. 3. Results The calibration curve was linear within the range of 5 -4000 ng·mL^- 1 The LLOQ was 5 ng·mL^-1 and RSDs of intra and inter day were less than 15%. The pharmacokinetic parameters after administration of 1500 mg ranolazine sustained release tablets at a single doses were as follow： Cmax was （1.27±0.50） mg ·mL^-1, tmax was （3. 13 ±1.55） h, t1/2 was （5.02± 1.47） h, Vwas （0. 74 ±0. 35） L, EL was （0. 10±0. 05）L·h^-1, AUC0-48 was （ 17.50 ± 8.31 ） mg·h· mL^-1. Conclusion The method is sensitive, selective and suitable for the pharmacokinetie study of ranolazine.

关 键 词：雷诺嗪 液相色谱-串联质朴法 药代动力学 

分 类 号：R972.3[医药卫生—药品] R969.1[医药卫生—药学]