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

摘要

Objective; To prepare norfloxacin sulfobutylether-p-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. Resu The formation of the NFX-SBE-p-CD complex could be confirmed. The solubility and dissolution rate of NFX were obviously improved by SBE-β-CD. Pharmacokinetic 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-p-CD could significantly improve the solubility, dissolution rate and bioavailability of NFX.%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t1/2,tmax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.