摘要
伊曲康唑难溶于水,使其用药方式受到限制.以多聚物5k PEGCA8作为包裹物,采用薄膜分散法制备伊曲康唑纳米粒,静脉注射小鼠体内,采用荧光-HPLC测定血液和体内组织中伊曲康唑药物浓度,并通过药代动力学软件Win Nonlin测定纳米粒型伊曲康唑在小鼠体内的药代动力学特性.结果表明:小鼠血液最大浓度Cmax为(2.850±0.075)μg/L,血药浓度-时间曲线下面积AUC(0-∞)为(25 490.84±720.416)(μg·h)/L,半衰期t1/2z为(6.526±1.386)h,达锋时间Tmax为1h.研究结果表明,纳米型伊曲康唑可以有效解决伊曲康唑难溶于水的问题,为伊曲康唑注射针剂的开发提供了参考.
Clinical uses of itraconazole were limited due to its poor solubility. In order to widen its range of application, nanoparticles encapsulating itraconazole were prepared by film-dispersion method using polymer 5kPEGCA8 as covering components. After intravenous injection of itraconazole-loaded nanoparticles into mice, itraconazole concentrations in plasma and organs were detected by Fluorescence-HPLC and its pharmacokinetic properties were analyzed by software WinNonLin. The results showed that maximum concentration of itraconazole （C max） in plasma was （2.850± 0.075） μg/L and the maximum time （Tmax） to reach this peak value was lh; the result also indicated that half-life （t 1/2） of itraconazole was （6.526± 1.386 ） h and the C-t curve showed that the area AUC （0-∞） was （25 490.84 ± 720.416） （μg·h）/L. These results indicated that itraconazole-loaded nanoparticles could effectively solve the problem of its low solubility in water, and provided references for the development of itraconazole powder-injection formulation in the future.
出处
《河南工业大学学报（自然科学版）》
CAS
北大核心
2015年第3期96-100,共5页
Journal of Henan University of Technology：Natural Science Edition
基金
国家自然科学基金项目(31071922)
