难溶性药物T-OA微乳的制备和体内外性质

In vivo and in vitro studies of insoluble drugs T-OA microemulsion

目的制备难溶性药物T-OA口服微乳,并考察其体内外性质。方法采用伪三元相图绘制法筛选微乳处方;采用HPLC法测定T-OA的含量;给大鼠分别灌胃T-OA混悬液和T-OA微乳,比较药物在大鼠体内的生物利用度。结果筛选出的微乳载药体系处方为V[V(吐温80)∶V(乙醇)=3∶7]∶V(油酸)∶V(水)=0.54∶0.20∶0.26,微乳体系的载药量质量浓度为20 g·L-1;药物动力学研究结果表明所制备的T-OA微乳在大鼠体内的相对生物利用度达到5 654%。结论微乳载药系统提高了难溶性药物T-OA的生物利用度。

Objective To prepare insoluble drug T-OA microemulsion and to evaluate of in vivo and in vitro properties. Method Pseudo-ternary phase diagram was adopted to optimize the formula of T-OA microemulsion; T-OA content was measured by HPLC; T-OA suspension and T-OA microemulsion were adminitstered to compare drug bioavailability in rats. Results Screened microemulsion system formulation was drug premixed emulsifier V[V(Tween 80)∶V(ethanol)= 3∶7]∶V(oleic acid)∶V(water) = 0.54∶0.20∶0.26, drug loading of microemulsion was 20 g·L-1; pharmacokinetic study indicated that the relative bioavailability of T-OA microemulsion reached 5 654% in rats. Conclusion The microemulsion system had improved drugs bioavailability of poorly soluble drug T-OA.