目的：评价山楂叶总黄酮过饱和自乳化释药系统在水性介质的分散过程中油相的脂链长度与沉淀抑制能力的关系。方法以前期优化的山楂叶总黄酮自乳化处方为基础（吐温80- Transcutol P -油酸乙酯=47：40：13），将处方油相分别替换为长链油相 Labrafil M 1944、Castor oil 及中链油相 Labrafac CC、Capryol 90和正辛酸；在体外模拟胃肠道溶出环境中，考察各油相过饱和自乳化处方的溶出度、载药前后的粒径变化。结果中链油相处方过饱和载药后粒径明显增大，粒径大小受不同溶出介质的影响明显，体外溶出30 min 左右开始出现沉淀；长链油相处方的粒径受过饱和载药和溶出介质的影响不明显，体外溶出90 min 无沉淀现象的出现。结论与中链油相相比，长链油相更有助于提高山楂叶总黄酮过饱和自乳化体系的沉淀抑制能力。%Objective To evaluate the effect of lipid chain length on the precipitation of crataegi folium flavonoids from supersaturatable self - emulsifying drug delivery system(SEDDS)on dispersion into aqueous medium. Methods Based on the pre - optimized prescription of crataegi folium flavonoids SEDDS(Tween 80 - Transcutol P - ethyl oleate = 47:40:13), two more long chain lipid Labrafil M 1944 and Castor oil,and three medium chain lipid Labrafac CC,Capryol 90 and n -Capr - ylic acid were studied. The supersaturation SEDDS of long chain and medium chain lipid were evaluated for drug re-lease and droplets size in simulated gastrointestinal dissolution environment. Results The droplets size of medium chain lipid SEDDS significantly increased after loading with crataegi folium flavonoids,and it was obviously affected by the disso-lution medium. However,the long chain lipid SEDDS showed stable after loading with drug as well as in different dissolution media. The in vitro dissolution test showed that the long chain lipids SEDDS effectively sustained a supersaturated state by retarding precipitation kinetics,whereas medium chain lipids SEDDS showed precipitation within 30 min. Conclusion Compared with the medium chain lipid,the long chain lipid has a stronger ability to inhibit the precipitation.
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