酮康唑栓剂的制备、溶出度和生物利用度研究

Preparation of ketoconazole suppository and study on its dissolution behaviour and bioavalability

设计和制备了酮康唑栓剂,并运用高效液相色谱法进行了家兔体内生物利用度研究,旨在探讨酮康唑直肠吸收程度及处方设计的合理性。实验测得,酮康唑栓剂的 T_(max)=2.64h;C_(max)=3.59μg/ml;AUC_(0-∞)=43.94μg·h/ml。与口服酮康唑混悬液相比,栓剂的相对生物利用度为53.15%,其结果可供临床研究时参考。

To avoid hepatoxity and gastrointestinalreactions after the oral administration of ke-toconazole,we prepared the suppositories andstudied dissolution behaviour in vitro and bio-availability in rabbits given rectally at thedose of 50mg/kg.Using N-(p-bromophenyl)-2-amino-4,5-di-hydrothiazole as the internal standard,thepharmacokinetics parameters and bioavailabilityof ketconazole suppositories obtained by thereverse phase high performance liquid chro-matography were found to be:Tmax=2.64h,Cmax=3.59μg/ml,AUC_(o→∞)=43.94μg.h/ml,Fr-el=53.15% respectivly.