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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 make fenofibrate self-microemulsion and to evaluate it in vitro and in vivo. Methods: The particle size and distribution of emulsified emulsion were determined. The dissolution rate of fenofibrate self-microemulsion in vitro and the pharmacokinetics of beagle dog were compared with the commercial preparations. Results: The prepared fenofibrate self-microemulsion emulsified completely within 5min, and the average particle size of microemulsion formed after emulsification was less than 50nm. With 0.1mol.L-1 hydrochloric acid as dissolution medium, 20min can dissolve more than 90%. The in vivo pharmacokinetic results of beagle dogs showed that the AUC0-∞ of self-microemulsion formulations increased about 7-fold compared to the commercial formulations. CONCLUSIONS: Self-microemulsions significantly increase fenofibrate dissolution and in vivo bioavailability.