二妙丸中3种生物碱成分在Beagle犬体内的药代动力学

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。

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

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:c_max(4.474±1.8),(0.508 3±0.2) and (0.812 4±0.7) ng/mL,t_1/2(38.1±15.4),(23.8±9.9) and (20.2±17.1) h,AUC_{0-48 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.