阿苯达唑纳米微粉平衡溶解度和表观脂水分配系数的测定.docVIP

阿苯达唑纳米微粉平衡溶解度和表观脂水分配系数的测定 　　[摘要] 目的 测定阿苯达唑纳米微粉在不同介质中的平衡溶解度以及表观脂水分配系数。 方法 采用高效液相色谱法测定阿苯达唑的浓度，采用摇瓶法测定阿苯达唑纳米微粉在不同极性溶剂和不同pH缓冲液中的平衡溶解度及表观脂水分配系数。 结果 不同极性溶剂中，阿苯达唑纳米微粉在甲醇中溶解度最大[（2564.28±38.73）μg/mL]，在水中的溶解度最小[（125.25±1.45）μg/mL]。在pH=1.2～6.8?冲液中，阿苯达唑纳米微粉溶解度从（551.33±19.00）μg/mL下降到（155.84±5.52）μg/mL；在pH=7.0～7.8缓冲液中，溶解度从（137.53±4.87）μg/mL上升到（168.94±5.63）μg/mL。纳米微粉的表观脂水分配系数在pH=1.2～2.0条件下lgP在0～2之间，pH=5.0～7.8条件下lgP在3～4之间。 结论 本研究测定了阿苯达唑纳米微粉在不同介质中的平衡溶解度以及表观脂水分配系数，为预测该纳米微粉体内外吸收的改善奠定了基础。 　　[关键词] 阿苯达唑纳米微粉；平衡溶解度；表观脂水分配系数；高效液相色谱法 　　[中图分类号] R927 [文献标识码] A [文章编号] 1673-7210（2016）11（c）-0119-06 　　Determination of the equilibrium solubility and apparent lipid-water partition coefficient of Albendazole Nano-meter Powder 　　ZHANG Yuxin1，2 CHEN Bei2 WANG Jianhua2 ZHAO Jun2 　　1.Institute of Pharmacy of Xinjiang Medical University， the Xinjiang Uygur Autonomous Region， Urumqi 830011， China； 2.Department of Pharmacy， the First Affiliated Hospital of Xinjiang Medical University， the Xinjiang Uygur Autonomous Region， Urumqi 830011， China 　　[Abstract] Objective To determine the equilibrium solubilities and apparent oil-water partition coefficients for Albendazole Nano-meter Powder in different medium. Methods HPLC was used to determine the concentration of Albendazole. Shake flask method was employed to determine the equilibrium solubility and oil-water partition coefficient of Albendazole Nano-meter Powder in the different polar solvents and different pH buffer. Results Among the different polar solvents， the solubility of Albendazole Nano-meter Powder in methanol was the largest [（2564.28±38.73）μg/mL]， and the solubility in water was the smallest [（125.25±1.45）μg/mL]. The solubilities of Albendazole Nano-meter Powder in the buffer solution of pH=1.2-6.8 decreased from （551.33±19.00） μg/mL to （155.84±5.52）μg/mL， and the solubilities in the buffer solution of pH=7.0-7.8 increased from （137.53±4.87） μg/mL to （168.94±5.63）μg/mL. The apparent oil-water partition coefficients of nano-meter powde wer