温莪术油自乳化释药系统的制备及小肠吸收

Preparation of zedoaryturmeric oil self-emulsifying deliverysystem and its absorption in intestine

目的制备温莪术油自乳化释药系统（zedoary turmeric oil self-emulsifying drug delivery sys—tem，ZTOSEDDS）并进行评价。方法以总油相质量分数（X2）、磷脂与脱氧胆酸钠的质量比（墨）和混合表面活性剂与乙醇的质量比（X3）为考察对象，自乳化液粒径（Y1）和自乳化时间（y2）作为质量评价指标，采用Box—Behnken效应面法筛选ZTO SEDDS的最佳处方。以温莪术油为对照，呋喃二烯和栊牛儿酮为检测指标，采用大鼠离体非翻转肠囊法对优化处方的小肠吸收进行评价。结果ZTO SEDDS的载药量质量分数为32．9％。乳化后平均粒径为（212．4±3．5）Nm，自乳化1min内达到平衡。大鼠离体小肠吸收实验表明，ZTOSEDDS中呋喃二烯和栊牛儿酮的表观渗透系数（P）约为1．3×10-6cm·s-1和6．4×10～cm·s-1，比温莪术油提高了3．2—4．0倍。结论ZTO SEDDS能显著改善温莪术油的小肠吸收行为。

Objective To prepare and evaluate zedoary turmeric oil self-emulsifying delivery system （ZTO SEDDS）. Methods Self-emulsions were optimized by Box-Behnken experimental design. The proportion of amount of total oil （ X1 ）, phospholipid to sodium deoxycholate （ X2 ） and mixed surfactants to ethanol （ X3 ）, which is XI：X2：X3, were characterized. The particle diameters of self-emulsifying liquid （ Y1 ）and self-emulsi- fication times（ I12 ） were taken as the specifications of quality control. With zedoary turmeric oil as the control group, non everted gut sac method was applied to investigate the absorption of the optimized formulation by determining the concentrations of furanodiene and germacrone. Results The drug loading of ZTO SEDDS was 32. 9%. The optimized formulation could fully emulsify within 1 min and the mean particle size was （212.4 ＋ 3.5 ）nm. The intestinal absorption results showed that the Papp of the furanodiene and germacrone in the ZTO SEDDS were （ 1.3 x 10 -6 ） cm. s - 1 and （6. 4 x 10 - 6 ） cm. s - 1, respectively, which were 3.2 - 4. 0 times higher than that of the oil. Conclusions ZTO SEDDS can significantly improve the absorption in intes- tine of rats.