目的:制备盐酸奈必洛尔-羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)包合物,同时考察HP-β-CD提高盐酸奈必洛尔溶解度的效果。方法:应用溶液搅拌-冷冻干燥法制备包合物,采用L9(34)正交设计,以盐酸奈必洛尔与羟丙基-β-...目的:制备盐酸奈必洛尔-羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)包合物,同时考察HP-β-CD提高盐酸奈必洛尔溶解度的效果。方法:应用溶液搅拌-冷冻干燥法制备包合物,采用L9(34)正交设计,以盐酸奈必洛尔与羟丙基-β-环糊精投料比(摩尔比)、包合温度、包合时间、乙醇浓度为因素,以包封率为指标筛选最佳工艺;通过相溶解度法、红外分光光度法和X-射线粉末衍射法对包合物进行验证;以高效液相色谱法(HPLC)测定包合物的包封率和溶解度。结果:最佳包合工艺为盐酸奈必洛尔与羟丙基-β-环糊精投料比(摩尔比)为1∶1,包合温度40℃,包合时间4 h,乙醇浓度80%(V/V);验证实验表明,盐酸奈必洛尔-羟丙基-β-环糊精包合物形成,相溶解度图呈AL型,物理混合物图谱与包合物图谱存在显著差别;以最佳工艺制备包合物,HPLC法测定其包封率达(73.69±0.10)%,药物经包合后在纯化水和p H 6.8磷酸盐缓冲液中的溶解度分别增大了3.18和11.10倍。结论:溶液搅拌-冷冻干燥法制备包合物方法合理可行,改善了药物的溶解性能。展开更多
To enhance the efficiency of a pathogen forecasting model in the beach areas of southern Lake Michigan and to reduce the computation time, the near-shore current is approximated as a channelized flow parallel to the s...To enhance the efficiency of a pathogen forecasting model in the beach areas of southern Lake Michigan and to reduce the computation time, the near-shore current is approximated as a channelized flow parallel to the shorelines in clockwise or anti-clock- wise direction within the accuracy tolerance range. A channelized model with a curvilinear boundary can significantly reduce the computation effort, and at the same time achieve a good agreement between the predicted and measured water surface elevations, currents, and water temperatures. The sensitivity analysis results show that the suitable channel width for the near-shore region of southern Lake Michigan should be no less than 10 kin. The modeling results of the water temperature are much less sensitive to the channel width than those of the current velocity and the water surface elevation. The modeling results also show a close correlation between the speeds of the wind and the near-shore current. The current may fully respond the wind stress with a time lag of several hours. The correlation may provide an approximate estimation of the lake circulation under some wind conditions for a practical fore- casting purpose. More complex wind-current relationships need to be described with a more sophisticated hydrodynamic model. This verified model can be used for the pathogen forecasting in the near-shore regions of southern Lake Michigan in the future.展开更多
文摘目的:制备盐酸奈必洛尔-羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)包合物,同时考察HP-β-CD提高盐酸奈必洛尔溶解度的效果。方法:应用溶液搅拌-冷冻干燥法制备包合物,采用L9(34)正交设计,以盐酸奈必洛尔与羟丙基-β-环糊精投料比(摩尔比)、包合温度、包合时间、乙醇浓度为因素,以包封率为指标筛选最佳工艺;通过相溶解度法、红外分光光度法和X-射线粉末衍射法对包合物进行验证;以高效液相色谱法(HPLC)测定包合物的包封率和溶解度。结果:最佳包合工艺为盐酸奈必洛尔与羟丙基-β-环糊精投料比(摩尔比)为1∶1,包合温度40℃,包合时间4 h,乙醇浓度80%(V/V);验证实验表明,盐酸奈必洛尔-羟丙基-β-环糊精包合物形成,相溶解度图呈AL型,物理混合物图谱与包合物图谱存在显著差别;以最佳工艺制备包合物,HPLC法测定其包封率达(73.69±0.10)%,药物经包合后在纯化水和p H 6.8磷酸盐缓冲液中的溶解度分别增大了3.18和11.10倍。结论:溶液搅拌-冷冻干燥法制备包合物方法合理可行,改善了药物的溶解性能。
基金supported by the State key Laboratory of Hydroscience and Engineering of Tsinghua University(Grant Nos.Sklhse-2007-B-03,2011-KY-4)
文摘To enhance the efficiency of a pathogen forecasting model in the beach areas of southern Lake Michigan and to reduce the computation time, the near-shore current is approximated as a channelized flow parallel to the shorelines in clockwise or anti-clock- wise direction within the accuracy tolerance range. A channelized model with a curvilinear boundary can significantly reduce the computation effort, and at the same time achieve a good agreement between the predicted and measured water surface elevations, currents, and water temperatures. The sensitivity analysis results show that the suitable channel width for the near-shore region of southern Lake Michigan should be no less than 10 kin. The modeling results of the water temperature are much less sensitive to the channel width than those of the current velocity and the water surface elevation. The modeling results also show a close correlation between the speeds of the wind and the near-shore current. The current may fully respond the wind stress with a time lag of several hours. The correlation may provide an approximate estimation of the lake circulation under some wind conditions for a practical fore- casting purpose. More complex wind-current relationships need to be described with a more sophisticated hydrodynamic model. This verified model can be used for the pathogen forecasting in the near-shore regions of southern Lake Michigan in the future.
