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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 To investigate in vitro dissolution characteristics of fenofibrate nanosuspensions, powdered raw materials and micronized powdered raw materials, the bioavailability of fenofibrate nanosuspensions in vivo and in vivo were compared and evaluated in vitro and in vivo. Methods The dissolution rate in vitro was determined by ultraviolet spectrophotometry. The plasma concentration of drug was measured by high performance liquid chromatography after intragastric administration. The in vivo absorption fraction was calculated by Wagner-Nelson method to investigate the correlation between in vivo absorption and in vitro dissolution. Results The AUC0-36h and Cmax of the nano-group were 10 times and 2 times that of the raw material group and the micro-powder group respectively. The relationship between the in vivo absorption fraction fa of the nano-suspension group and the in vitro dissolution rate ft was: fa = 4.407 9ft? 303.31, r = 0.983 8. Conclusion Compared with the raw materials and the micronized powder group, the dissolution rate and bioavailability of fenofibrate were significantly increased after the drug was made into nanosuspension. The dissolution in vitro and the correlation with the absorption in vivo were good.