【摘要】 目的将姜黄素(Cur)制成自微乳化给药系统,并对其进行体内外评价。方法测定乳化后乳剂的pH值、自乳化时间、粒径、形态特征、稳定性和体外释放度,考察Cur自微乳化给药系统在小鼠体内的药物动力学过程,并与其混悬剂相比较。结果 Cur自微乳化给药系统可在4 min内乳化完全,乳化后的微乳pH值接近中性,平均粒径为31.98 nm。以0.25%SDS的纯净水为释放介质,10 min内药物可释放完全。8 h内微乳溶液中Cur的含量保持>94%。小鼠灌胃给药后的药动学过程表明,与Cur混悬液相比,微乳的AUC提高了12倍。结论自微乳化给药系统可显著提高Cur的体外溶出度和体内生物利用度。更多还原

【Abstract】 Objective To prepare the curcumin self-microemulsifying delivery system and to evaluate the quality in vivo and in vitro.Methods The pH,self-emulsification time,particle size,morphology,stability and dissolution of the resultant emulsion after self-emulsifying were determined.The plasma concentrations were determined by HPLC and the pharmacokinetics behavior of curcumin microemulsion was evaluated by comparison with suspension.Results The curcumin self-microemulsifying delivery system can emulsified completely within 4 min.Mean particle size of the resultant emulsion was 31.98 nm,and pH approximated to neutral.The dissolution of curcumin self-microemulsifying formulation at 10 min was 100% and the content of drug maintained above 94% with 8 h.Compared with suspension,the area under time-concentration curve(AUC) of micro-emulsion after gavage increased 12-fold.Conclusion The self-microemulsifying delivery system can significantly increase curcumin dissolution in vitro and bioavailability in vivo.更多还原