非诺贝特纳米混悬剂溶出度测定与体内吸收的相关性评价  

Study on the Correlation between Dissolution in Vitro and Absorption in Vivo of Fenofibrate Nanosuspension

作　　者：王悦[1] 王永禄[1] 李学明[1] 毛利娟[1] 徐元龙[1] 

机构地区：[1]南京工业大学药学院,南京211816

出　　处：《中国现代应用药学》2010年第11期1013-1018,共6页Chinese Journal of Modern Applied Pharmacy

基　　金：江苏省高校自然科学基金资助项目(09KJB350001);南京工业大学学科基金资助项目(39728007)

摘　　要：目的考察非诺贝特纳米混悬剂、原料药粉、微粉化原料药粉的体外溶出特性,研究比较三者在大鼠体内的生物利用度,并对其体内外相关性作出评价。方法以紫外分光法测定体外溶出度;以高效液相色谱法测定大鼠灌胃给药后的血药浓度;以Wagner-Nelson法计算体内吸收分数,考察体内吸收与体外溶出的相关性。结果纳米组AUC0-36h和Cmax分别为原料组、微粉组的10倍和2倍,纳米混悬剂组体内吸收分数fa与体外溶出速率ft的关系为:fa=4.407 9ft?303.31,r=0.983 8。结论与原料和微粉组相比,非诺贝特制成纳米混悬剂后,药物的溶出速度和生物利用度均有显著提高,体外溶出与体内吸收相关性良好。OBJECTIVE The dissolution rate in vivo and bioavailability in rats of fenofibrate nanosuspension,coarse and microsize suspension were investigated.The correlations of the drugs in vitro-in vivo were also evaluated.METHODS The drug dissolutions in vitro were measured by UV spectrophotometer,and the plasma concentrations in rats were measured by HPLC.The correlations were studied by the test of dissolution in vitro and bioavailability in vivo through Wagnner-Nelson method.RESULTS The AUC0-36h and Cmax of the nanosuspensions were about 10-fold of the coarse and 2-fold of the microsize suspension.The relationship between the dissolution fraction and the absorption fraction was： fa=4.407 9ft？303.31,r=0.983 8.CONCLUSION The dissolution and bioavailability of nanosuspensions enhanced greatly compared with the coarse and microsize suspension.There were good correlationships between dissolution rate in vitro and absorption rate in vivo.

关 键 词：非诺贝特 纳米混悬剂 溶出度 Wagner-Nelson法 体内外相关性 

分 类 号：R943[医药卫生—药剂学]