【摘要】 目的制备格列齐特凝胶骨架缓释制剂,考察影响该制剂药物释放的因素以及体内的药动学特征。方法采用单因素考察确定影响药物释放的关键因素,以自制片与参比制剂体外释放数据的相似因子作为评价指标,采用正交设计法优化格列齐特缓释片的最佳处方。结果 HPMC K15M、HPMC K100LV、磷酸氢钙用量对药物释放影响最为显著,自制格列齐特缓释片在12 h内的释放符合零级释放模型。自制制剂与参比制剂在Beagle犬体内的血药浓度-时间曲线相似,相对生物利用度为102.64%,达到了生物等效。结论自制格列齐特缓释片具有平稳的体外药物释放行为和良好的体内药动学特征。更多还原

【Abstract】 Objective To prepare gliclazide sustained release tablets,and determine the influence factors for drug release and in vivo pharmacokinetic characteristics.Methods The single factor inspection test was used to determine the key factors affecting the drug release.Results of similar factors of the in vitro release of self-made and reference tablets were used as evaluation indicators.Orthogonal experiment was designed to optimize the best formulation of gliclazide sustained-release tablets.Results The amount of HPMC K15M,HPMC K100LV and calcium hydrogen phosphate had significant effect on the drug release.The release of self-made gliclazide sustained release tablets within 12 h conformed to the zero-order release model.The blood concentration-time curve of the self-made preparation and the reference preparation in Beagle dogs was similar,and the relative bioavailability was 102.64%,suggesting bioequivalence.Conclusion The self-made gliclazide sustained release tablets have stable in vitro release behaviors and good in vivo pharmacokinetic characteristics.更多还原