诺氟沙星-磺丁基醚-β-环糊精包合物的制备及人体药动学研究  

Preparation and in vivo Pharmacokinetic Study of Norfloxacin Sulfobutylether-β-cyclodextrin Complex

作　　者：谷福根[1] 李文妍[2] 孟根达来[1] 王毅[1] 张爱武[1] 吴春芝[1] 郭智[1] 

机构地区：[1]内蒙古医学院附属医院药剂部,呼和浩特010059 [2]内蒙古医学院药学院

出　　处：《中国药师》2011年第9期1256-1259,共4页China Pharmacist

基　　金：内蒙古自然科学基金资助课题(编号:2009MS1202)

摘　　要：目的:制备诺氟沙星(NFX)-磺丁基醚-β-环糊精(SBE-β-CD)包合物,并研究其溶解度、溶出度以及体内药动学行为。方法:采用冷冻干燥法制备NFX-SBE-β-CD包合物,以X-射线衍射法及差示热量扫描法(DSC)对其进行物相鉴定。同时,测定NFX包合物的溶解度、溶出度并研究其体内药动学。结果:NFX与SBE-β-CD已形成包合物;经包合后,NFX的溶解度、溶出速率显著增加;包合物的药动学参数t_(1/2),t_(max)与原药比较,无显著性差异(P>0.05),而其尿药排泄速率以及累积排泄量均显著高于原药(P<0.05)。结论:NFX制成SBE-β-CD包合物后,其溶解度、溶出度以及体内生物利用度显著改善。Objective： To prepare norfloxacin sulfobutylether-β-cyclodextrin （NFX-SBE-β-CD） complex and investigate the solubility, dissolution rate and in vivo pharmacokinetic behavior. Method： NFX-SBE-β-CD complex was prepared by lyophilization method and identified by X-ray diffraction and differential scanning calorimetry （DSC）. The solubility, dissolution rate and pharmacokinetic property of the complex in human beings were also studied. Result： The formation of the NFX-SBE-β-CD complex could be confirmed. The solubility and dissolution rate of NFX were obviously improved by SBE-β-CD. Pharmaeokinetic parameters of the complex, such as t1/2 and tmax ,were not significantly different from those of the intact drug （P 〉 0. 05 ） ,while the urine excretion rate and cumulative excretion amount were significantly greater than those of NFX （P 〈 0. 05 ）. Conclusion： SBE-β-CD could significantly improve the solubility, dissolution rate and bioavailability of NFX.

关 键 词：诺氟沙星 磺丁基醚-Β-环糊精 溶解度 包合物 生物利用度 

分 类 号：R945[医药卫生—微生物与生化药学]