摘要
本文报道了11名健康志愿者一次口服60mg/kg吡喹酮普通片及吡喹酮缓释片的药代动力学分析。血浆吡喹酮浓度测定用HPLC荧光检测法。吡喹酮体内动力学分析符合一室口服模型。普通片峰浓度Cmax2.232±0.579mg/l较缓释片0.779±0.329mg/l高,p<0.01,普通片吸收半衰期t1/2k1.627±0.403较缓释片4.007±0.889短,p<0.01。缓释片的药时曲线平稳而延长。其相对生物利用度为普通片的68.32±8.51%。缓释片的体内外数据具有显著相关性p<0.01。此外并对两种剂型的临床意义进行了讨论。
60mg/kg of praziquantel tablets and praziquantel sustained release tublets weregiven orally to 11 normal male volunteers. HPLC method was used to measure plasma praziquantelconcentration. The C×t data of praziquantel tablets were fit to one compertment open model. TheC_(max) in the healthy volunteers who received the normal release tablet was higher and was attained morerapidly than that in subjects who received the sustained release tablet (p<0.01). The elimination half life (t1/2k)of normal release tablet was shorter than that of sustained release tablet (p<0.01). The re-sults showed that the sustained release formulation would produce more constant plasma levels. Morev-er, the fraction of the dose absorbed form sustained release tablets in vivo correlated with dissolutionrate in vitro. The relative bioavailability for the praziquantel was thus estimated as about 68.32±8.51%. The practical significance and clinical triplications of the above results were discussed.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1992年第2期87-91,共5页
The Chinese Journal of Clinical Pharmacology
关键词
吡喹酮
缓释片
药代动力学
praziquantel
Ptaziquante sustuined release tablets
relative bioavailability
Pharmndinetics
