罗红霉素氨溴索分散片在健康人体的药代动力学  

Evaluation of pharmacokinetics of the dispersible tablet of roxithromycin and ambroxol hydrochloride in healthy volunteers

作　　者：王楠[1] 张梦[2] 杭太俊[3] 张正行[3] 张银娣[4] 张劲松[4] 

机构地区：[1]南京军区南京总医院药品科,江苏南京210002 [2]上海市食品药品检验所,上海201203 [3]中国药科大学药物分析室,江苏南京210009 [4]南京医科大学临床药理研究所,江苏南京210029

出　　处：《南京医科大学学报（自然科学版）》2009年第10期1435-1439,共5页Journal of Nanjing Medical University(Natural Sciences)

摘　　要：目的:建立同时测定人血浆中罗红霉素和盐酸氨溴索的液相色谱-串联质谱联用法(LC-MS/MS),研究健康受试者口服罗红霉素盐酸氨溴索分散片(每片含罗红霉素150 mg、盐酸氨溴索30 mg)后的人体药代动力学。方法:12名健康受试者单剂量口服罗红霉素盐酸氨溴索分散片后72 h内间隔取血,用LC-MS/MS测定血浆样品药时过程,用DAS数据处理软件计算主要药代动力学参数。结果:罗红霉素的主要药动学参数Cmax,Tmax,t1/2z,MRT,AUC0-τ,CLz/F和Vz/F分别为(6.99±1.55)μg/ml,(2.04±0.94)h,(13.30±2.56)h,(14.31±2.51)h,(84.56±26.20)h.μg/ml,(1.88±0.51)L/h和(35.06±8.68)L;盐酸氨溴索的分别为(53.91±22.41)ng/ml,(1.96±0.66)h,(8.24±2.01)h,(7.96±0.47)h,(447.98.±138.95)h.ng/ml,(61.85±14.79)L/h和(724.42±214.86)L。结论:血浆样品中罗红霉素和盐酸氨溴索同时测定LC-MS/MS法专属性强,灵敏度适宜。适用于罗红霉素盐酸氨溴索分散片药代动力学研究。Objective：To establish a LC-MS/MS method for assessment of pharmacokinetics of dispersible tablet of roxithromycin and ambroxol hydrochloride （each containing roxithromycin 150 mg,ambroxol hydrochloride 30 mg）. Methods：Each of 12 healthy Chinese volunteers was given a single oral dose of one tablet. Plasma samples were collected at 72 h post-administration and the concentrations were determined by LC-MS/MS. The pharmacokinetic parameters were calculated by DAS software. Results：The main pharmacokinetic parameters of Cmax,Tmax,t1/2,MRT,A UC0-τ,CLz/F and Vz/F for roxithromycin were （6.99±1.55） ug/ml, （2.04±0.94） h, （13.30±2.56） h, （14.31±2.51） h, （84.56±26.20） h.txg/ml, （1.88± 0.51）L/h and （35.06±8.68）L,respectively;and those for ambroxol hydroehloride were （53.91±22.41） ng/ml, （1.96±0.66） h, （8.24±2.01） h, （7.96±0.47） h, （447.98±138.95） h.ng/ml, （61.85±14.79）I./h and （724.42±214.86）L,respectively. Conclusion：The established LC-MS/MS method is selective,sensitive and reliable for the pharmacokinetic study of the dispersible tablet of roxithromycin and ambroxol hydrochloride.

关 键 词：罗红霉素 盐酸氨溴索 药代动力学 LC—MS/MS 

分 类 号：R969.1[医药卫生—药理学]