玳玳黄酮自微乳化微丸在大鼠小肠的吸收特性和机制研究  

Absorptive characteristic and mechanism of Self-microemulsifying Pellets of Daidai Flavones in small intestines of rats

作　　者：吴晓青[1] 陈丹[1] 程清[1] 任瑞琴[1] 黄庆德[1] 郑利[1] 

机构地区：[1]福建中医药大学药学院,福建福州350108

出　　处：《中草药》2012年第11期2222-2226,共5页Chinese Traditional and Herbal Drugs

基　　金：福建省科技计划重点项目(2010Y0030);福建省科技计划项目(2010Y2004);福建省自然科学基金资助项目(2010J01189;2012J01386)

摘　　要：目的考察玳玳黄酮自微乳化微丸在大鼠小肠的吸收特性和促吸收效果,探讨玳玳黄酮自微乳化微丸的吸收部位及吸收机制。方法采用大鼠离体外翻肠囊模型,以柚皮苷和新橙皮苷作为玳玳黄酮自微乳化微丸的特征成分,高效液相色谱-质谱联用(HPLC-MS)技术检测在相同给药质量浓度下大鼠十二指肠、空肠、回肠及不同给药质量浓度下空肠肠囊内的药物浓度;并比较相同质量浓度玳玳黄酮自微乳化微丸与玳玳黄酮有效部位提取物的吸收效果。结果玳玳黄酮自微乳化微丸中柚皮苷和新橙皮苷在不同肠段中90 min的累积吸收量按十二指肠、空肠、回肠依次下降,但吸收差异很小,即十二指肠至回肠均是玳玳黄酮的有效吸收部位。玳玳黄酮自微乳化微丸质量浓度分别为3.6、7.2、12.0 mg/mL时,在空肠段的吸收随时间的增加而增加,表现出一级吸收动力学过程;柚皮苷和新橙皮苷的吸收速率常数(Ka)均随药液质量浓度的增加而增加(P<0.05),表明其为被动吸收;在相同给药剂量下,柚皮苷和新橙皮苷在大鼠空肠90 min的累积吸收量是玳玳黄酮有效部位提取物的1.3倍。结论大鼠小肠上中段是玳玳黄酮自微乳化微丸的最佳吸收部位;其吸收呈一级动力学过程,吸收机制可能为被动扩散;与玳玳黄酮有效部位提取物比较,玳玳黄酮自微乳化微丸可显著改善柚皮苷和新橙皮苷的肠吸收。Objective To study the intestine absorptive characteristic and absorption efficiency of Self-microemulsifying Pellets of Daidai （Citrus aurantium var. daida） Flavones （SMPDF） in rats and to investigate the absorption sites and absorption mechanism of SMPDF. Methods The isolated everted gut sac model was used, naringin and neohespiridin were chosen as representative compositions, the drug concentration in duodenum, jejunum, and ileum of rats with the same administration dosage, and that in jejunum with the different administration dosages were determined by high performance liquid chromatography with mass （HPLC-MS） detector. The absorption efficiencies of SMPDF and the active fractionextractionofDaidaiflavones were compared. Results In duodenum, jejunum, and ileum of rats, the absorption of naringin and neohespiridin declined in 90 min in turn, but there was no significant difference among them. So duodenum, jejunum, and ileum were all effective absorption sites of Daidai flavones. The absorption in jejunum was increased with time increasing at SMPDF doses of 3.6, 7.2, and 12.0 mg/mL, which was consistent with the first order rate process. The Ka values of naringin and neohespiridin increased along with the increasing dosage of SMPDF （P 〈 0.05）, whieh indicated they were the passive absorption. In the same administration dosage, the accumulative absorption amount of naringin and neohespiridin in SMPDF at 90 min was 1.3-fold as that in the extraction of Daidai flavones. Conclusion The duodenum, jejunum, and ileum of rats are all effective absorption sites of SMPDF. In the test dosage, the absorption of naringin and neohespiridin in the jejunum intestine conforms to the first order rate process and shows the passive absorption. The intestinal absorption of naringin and neohespiridin could be significantly imoroved by SMPDF comparing with the extraction in effective fraction of Daidai flavones.

关 键 词：玳玳黄酮 自微乳化微丸 肠吸收 外翻肠囊模型 新橙皮苷 柚皮苷 HPLC-MS 

分 类 号：R969.1[医药卫生—药理学]