The pyrrolizidine alkaloids(PAs) in leaf of Gynura divaricata(L.) DC.was analyzed by LC-MSn technique.The result shows that two hepatotoxic pyrrolizidine alkaloids(HPAs) are detected from the methanol extract of G.div...The pyrrolizidine alkaloids(PAs) in leaf of Gynura divaricata(L.) DC.was analyzed by LC-MSn technique.The result shows that two hepatotoxic pyrrolizidine alkaloids(HPAs) are detected from the methanol extract of G.divaricata leaf,with relative molecular weight of 335 and 365,respectively and lower content.The constituent with relative molecular weight 335 is a retronecine-type alkaloid,and identified as integerrimine;another constituent with relative molecular weight 365 is an otonecine-type alkaloid,speculated to be isomer of usaramine or 18-hydroxyinterrimine.展开更多
目的研究健康受试者口服0.125mg和0.25mg普拉克索片的药动学过程,并评价该制剂的安全性,为注册治疗不宁腿综合征(restless leg syndrome,RLS)提供药动学依据。方法采用随机、开放、双向交叉试验设计,12名健康受试者(男女各半)分两个阶...目的研究健康受试者口服0.125mg和0.25mg普拉克索片的药动学过程,并评价该制剂的安全性,为注册治疗不宁腿综合征(restless leg syndrome,RLS)提供药动学依据。方法采用随机、开放、双向交叉试验设计,12名健康受试者(男女各半)分两个阶段分别进行单次口服普拉克索片0.125mg和0.25mg的药动学试验,两次给药间隔13天,每次给药前及给药后采集血样,采用液相色谱-串联质谱联用法(LC-MS/MS)测定健康受试者给药后血浆中普拉克索的浓度。采用WinNonlin(R)6.0版软件计算普拉克索片的药动学参数(AUC0-t、AUC0-∞﹑ρmax﹑tmax﹑t1/2﹑CL/F等)。整个试验过程进行全面安全性评估。结果单次口服普拉克索片0.125mg和0.25mg后,ρmax分别为(237±83)μg/L和(493±155)μg/L,tmax分别为(1.71±1.64)h和(1.21±1.01)h,t1/2分别为(6.12±2.21)h和(7.27±2.17)h,AUC0-∞分别为(1 791±765)μg·h·L-1和(4 419±1 932)μg·h·L-1,不同性别的药动学参数差异无统计学意义(P>0.05).试验过程无严重不良事件发生。结论单次口服0.125mg或0.25mg普拉克索吸收很快,吸收程度随剂量增加而增加,药动学过程不受性别影响.本研究制剂安全性较好,可按试验剂量给药治疗RLS。展开更多
文摘The pyrrolizidine alkaloids(PAs) in leaf of Gynura divaricata(L.) DC.was analyzed by LC-MSn technique.The result shows that two hepatotoxic pyrrolizidine alkaloids(HPAs) are detected from the methanol extract of G.divaricata leaf,with relative molecular weight of 335 and 365,respectively and lower content.The constituent with relative molecular weight 335 is a retronecine-type alkaloid,and identified as integerrimine;another constituent with relative molecular weight 365 is an otonecine-type alkaloid,speculated to be isomer of usaramine or 18-hydroxyinterrimine.
