摘要
目的:将非诺贝特制成自微乳制剂,并对其进行体内外评价。方法:测定乳化后乳剂的粒径大小及分布情况;考察非诺贝特自微乳制剂的体外溶出度以及比格犬体内药动学,并与市售制剂相比较。结果:制备的非诺贝特自微乳制剂可在5min内乳化完全,且乳化后形成的微乳平均粒径小于50nm。以0.1mol.L-1盐酸为溶出介质,20min可溶出90%以上。比格犬体内药动学结果表明,与市售制剂相比,自微乳制剂的AUC0-∞提高了约7倍。结论:自微乳制剂可显著提高非诺贝特的体外溶出和体内生物利用度。
OBJECTIVE To evaluate the dissolution behavior and the pharmacokinetics behavior of fenofibrate self-microemulsifying formulation in beagle dogs. METHODS The formulation was selected by drawing the ternary phase diagram and the particle sizes of resultant emulsions after self-emulsifying were determined. The plasma concentrations were determined by HPLC and the pharmacokinetics behavior of self-microemulsifying formulations was evaluated by comparison with the commercial product. RESULTS The dissolution of fenofibrate self-microemulsifying formulations at 20 min was much higher （more than 90%） than that of the commercial products（less than 10%）. The area under time-concentration curve （AUC） was significantly higher （about 7 times） in fenofibrate self-microemulsifying formulation group than that in the commercial products. CONCLUSION The self-microemulsifying delivery systems can significantly increase fenofibrate＇s dissolution in vitro and absorption in vivo.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2009年第14期1167-1170,共4页
Chinese Journal of Hospital Pharmacy
关键词
非诺贝特
自微乳
溶出
生物利用度
fenofibrate
self-microemulsifying
dissolution
bioavailability
