柿叶提取物自微乳化释药系统大鼠在体肠吸收研究  

In situ Absorption of Self-Microemulsifying Drug Delivery System of Diospyros kaki L.f. Extract in Rats′ Intestine

作　　者：崔升淼[1] 李婉文[2] 赵春顺[2] 

机构地区：[1]广东药学院,广州510006 [2]中山大学,广州510006

出　　处：《中国药学杂志》2013年第9期715-719,共5页Chinese Pharmaceutical Journal

基　　金：广东省科技计划项目(2006B35604007)

摘　　要：目的考察柿叶提取物自微乳化释药系统(SMEDDS)的大鼠在体肠吸收特征。方法采用大鼠在体小肠灌流实验模型,以高效液相色谱法测定灌流液中槲皮素、山柰酚和酚红的浓度,研究了不同药物浓度、不同吸收部位以及不同剂型对柿叶提取物大鼠肠吸收的影响。结果柿叶提取物自微乳化释药系统浓度的改变对提取物中槲皮素和山柰酚的Ka和P均无显著影响;十二指肠和回肠为柿叶提取物自微乳化释药系统的主要吸收部位;柿叶提取物自微乳化释药系统中槲皮素和山柰酚的吸收速率常数Ka和相对吸收百分率P均显著大于溶液组(P<0.05)。结论柿叶提取物在大鼠小肠主要通过被动扩散方式吸收,柿叶提取物自微乳化释药系统全肠吸收效果优于溶液剂。OBJECTIVE To investigate the intestinal absorption behaviors of Diospyros kaki L.f. extract （PLE） in self-microe- mulsifying drug delivery system （SMEDDS）. METHODS The concentration of quercetin, kaempferol and phenol red in rat intestinal perfusion solution was determined by HPLC. Rat single-pass intestinal perfusion technique was employed to assay the effects of concen- trations of PLE in perfusion solution, intestinal segments and different formulations on the drug percentage absorbed （P） and the ab- sorption rate constant （ Ka ）. RESULTS No significant changes of K and P were observed in different PLE concentrations. The main absorption segments of SMEDDS in rat intestines were the duodenum and ileum. The values of Ka and P of SMEDDS were significantly higher than the PLE solution （ P 〈 0. 05 ）. CONCLUSION The absorption mechanism of PLE conforms to passive diffusion. The PLE SMEDDS presented the high absorption rate than conventional solution in rat intestine, which illustrates the potential use of SMEDDS for the delivery o f PLE by the oral route.

关 键 词：柿叶提取物 自微乳化释药系统 在体肠吸收 

分 类 号：R944[医药卫生—药剂学]