普罗布考片单次口服给药的人体药物代谢动力学研究  

Pharmacokinetics of Single-dose Probucol Tablet in Healthy Volunteers

作　　者：向瑾[1] 徐楠[1] 余勤[1] 王颖[1] 梁茂植[1] 苗佳[1] 南峰[1] 沈奇[1] 秦永平[1] 

机构地区：[1]四川大学华西医院国家药物临床试验机构.GCP中心临床药理研究室,成都610041

出　　处：《华西医学》2012年第7期975-978,共4页West China Medical Journal

摘　　要：目的采用高效液相色谱-质谱联用法(HPLC-MS/MS)研究普罗布考片的人体药物代谢动力学变化规律。方法 2010年10月-11月,24例健康男性受试者单次口服普罗布考片0.5 g,采用HPLC-MS/MS法测定给药后不同时间点血浆中普罗布考的经时血药浓度,采用DAS 2.0软件进行药动学参数计算。结果受试者单次口服普罗布考片,达峰时间为(11.50±6.66)h,峰浓度为(2 894.72±1 320.53)ng/mL,药-时曲线下面积(AUC)0-t为(238 876.96±131 873.67)ng/mL.h,AUC0-∞为(259 989.08±146 112.88)ng/mL.h,半衰期为(278.52±164.72)h。结论普罗布考片体内过程符合二室模型,单次口服具有较好的安全性。Objective To study the pharmacokinetics of probucol tablet in healthy volunteers with high performance liquid chromatography-electrospray tandem mass spectrometry （HPLC-MS/MS）. Methods Twenty-four healthy male vohmteers were enrolled in the study during October and November in 2010. The subjects were orally administered a single dose of 0.5 g probucol tablet. The concentrations ofprobucol were assessed with I-IPLC-MS/MS method and data were analyzed automatically with DAS 2.0 Pharmacokinetic Program. Results The parameters of probucol tablet were as following： the time to peak plasma concentration was （ 11.50 ~ 6.66） hours, the peak plasma concentration was （2 894.72 ± 1 320.53） ng/mL, the area under the plasma concentration- time curve （AUC）t was （238 876.96±131 873.67） ng/mL h, AUC0 was （259 989.08 4± 146 112.88） ng/mL h and the half- time was （278.52 4± 164.72） hours. Conclusion Probucol conforms to a two-compartment open model and a single dose possesses a good safety in healthy volunteers.

关 键 词：普罗布考 高效液相色谱-质谱联用法 药物代谢动力学 

分 类 号：R96[医药卫生—药理学]