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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。
This article reports the pharmacokinetics of 11 healthy volunteers orally once a day oral praziquantel tablets and praziquantel sustained-release tablets 60mg / kg. Determination of plasma praziquantel concentration by HPLC fluorescence detection method. Praziquantel in vivo kinetic analysis is consistent with a one-compartment oral model. Common peak peak concentration Cmax2.232 ± 0.579mg / l slower release tablets 0.779 ± 0.329mg / l high, p <0.01, ordinary tablet absorption half-life t1 / 2k1.627 ± 0.403 slower release tablets 4.007 ± 0.889 short, p < 0.01. Sustained-release tablets when the drug curve smooth and extended. The relative bioavailability of 68.32 ± 8.51% of ordinary tablets. In vitro and in vivo data for sustained release tablets had a significant correlation of p <0.01. In addition, the clinical significance of the two dosage forms was discussed.