氟比洛芬自乳化给药系统中释放的体内外分析

目的:研究氟比洛芬(furbiprofen,FB)自乳化释药系统的自乳化能力及在家犬体内的药动学。方法:评价系统自乳化速度,激光散射仪测定乳化后形成乳剂粒径的大小及分布情况,采用HPLC法测定家犬血浆药物浓度,与市售片比较,考察FB自乳化制剂体外溶出行为及体内药动学。结果:体系在1min内已基本乳化完全,乳化后乳剂粒子粒径大多数在70nm左右。与市售片剂相比,以水为溶出介质,氟比洛芬自乳化制剂120min可以溶出95%,而市售胶囊溶出约为50%。家犬体内药动学研究结果表明:与市售片剂相比,自乳化制剂达峰时间提前,tmax为0.75h,而市售胶囊tmax为1.5h;AUC0-∞提高了40%。结论:自乳化制剂可以显著提高FB的体外溶出及体内吸收。

Assessment of flurbiprofen with a self-emulsifying formulation in vitro and in vivo

OBJECTIVE To evaluate the self emulsifying ability and dissolution behavior of flurbiprofen in vitro and the pharmacokinetic behavior in dogs.METHODS The self emulsifying rate was evaluated by determining the particle size of resultant emulsions after self emulsifying by light scattering particle analysis.The plasma concentrations were determined by HPLC and dissolution and pharmacokinetic behavior of self emulsifying formulations were evaluated by comparison with commercial tablets.RESULTS Concentration under the curve(AUC) was significantly higher in the flurbiprofen self emulsifying formulation group than that in the commercial flurbiprofen group.Also,tmax was shortened in the self-emulsifying formulation group(0.75 h) compared with market products(1.5 h) and the dissolved amount from self emulsifying formulations in water at 120 min was much higher(about 95%) than that of the market products(about 50%).CONCLUSION The self emulsifying drug delivery systems can increase drug dissolution in vitro and absorption in vivo significantly.