二妙丸中3种生物碱成分在Beagle犬体内的药代动力学  

Pharmacokinetics of berberine,jatrorrhizine and palmatine in Beagle dogs after oral administration of Ermiao Wan

作　　者：房长进[1] 宋敏[1] 杭太俊[1] 张晓磊[1] 苏浩明[1] 姜翠翠[1] 

机构地区：[1]中国药科大学药物分析教研室,南京210009

出　　处：《中国药科大学学报》2012年第5期438-442,共5页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.81001619)~~

摘　　要：建立高灵敏的LC-MS/MS法测定血浆中小檗碱、巴马汀和药根碱的浓度,并用于研究Beagle犬灌服市售二妙丸后体内3种生物碱的药代动力学特征。6只健康Beagle犬,雌雄各半,单剂量灌服市售二妙丸制剂(相当于小檗碱25mg/kg)后,0～48 h间隔采集血样,采用电喷雾正离子化质谱法监测血浆中各成分的浓度。测得小檗碱、药根碱和巴马汀的cmax分别为(4.474±1.8),(0.508 3±0.2),(0.812 4±0.7)ng/mL,t1/2分别为(38.1±15.4),(23.8±9.9),(20.2±17.1)h,AUC0-48 h分别为(37.4±3.9),(3.75±1.2),(3.01±0.9)ng.h/mL。结果显示Beagle犬口服给药二妙丸后小檗碱、药根碱和巴马汀的血药浓度低,达峰时间快,消除半衰期长。This study developed an LC-MS/MS method for the simultaneous determination and plasma pharmacokinetic study of berberine,jatrorrhizine and palmatine in beagle dogs after oral administration of Ermiao Wan.Six dogs（3 males and 3 females） were orally administered with Ermiao wan（equal to berberine 25mg/kg）.Blood samples were collected into heparinized tubes from 0 to 48 h.The detection was performed by positive electrospray ionization（ESI） in the selected reaction monitoring mode.The main pharmacokinetic parameters of berberine,jatrorrhizine and palmatine were obtained as follows： cmax（4.474±1.8）,（0.508 3±0.2） and（0.812 4±0.7） ng/mL,t1/2（38.1±15.4）,（23.8±9.9） and（20.2±17.1） h,AUC0-48 h（37.4±3.9）,（3.75±1.2） and（3.01±0.9） ng ·h/mL.The results indicated that the oral bioavailability of berberine,jatrorrhizine and palmatine were very low.They were absorbed rapidly,and eliminated slowly in vivo.

关 键 词：二妙丸 小檗碱 药根碱 巴马汀 药代动力学 LC-MS/MS 

分 类 号：R969.1[医药卫生—药理学]