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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 investigate the absorption characteristics and absorption enhancement effect of tortoise shell flavone self-microemulsified pellets in the rat small intestine and investigate the absorption site and absorption mechanism of the self-microemulsified capsules. Methods The eversion oval sac model of rats was used. The naringin and neohesperidin were used as the characteristic components of the self-microemulsifying microemulsion of tomabearing and the HPLC-MS The concentration of drug in the jejunum of the duodenum, jejunum, ileum and the mass concentration of different doses of the drug were measured by the drug concentration in rats. The same mass concentration of the microemulsified drug was compared with that of the toxin Absorption effect. Results The cumulative absorption of naringin and neohesperidin in different segments of naringin from microemulsified microemulsions decreased by duodenum, jejunum and ileum, but the absorption difference was very small, that is, twelve The intestine to the ileum is the effective absorption site of tortoise shell flavone. The absorbency of jejunal segment increases with the increase of time when the concentration of the tobestoside flavonoids self-microemulsifiable pellets are 3.6, 7.2 and 12.0 mg / mL, respectively, showing the first-order absorption kinetics; Naringin and neo- The absorption rate constant (Ka) of glycosides increased with the increase of the mass concentration of the drug solution (P <0.05), indicating that it was absorbed passively. Under the same dose of administration, naringin and neohesperidin showed a significant increase in rat jejunum 90 The cumulative absorption amount of min was 1.3 times that of the extract of the effective part of euprytis flavone. Conclusion The upper middle part of the small intestine of rats is the best absorption site of the microemulsified microemulsions of euprytis flavone. The absorption is a first-order kinetic process, and the absorption mechanism may be passive diffusion. Compared with the extract of effective parts of tortoise-flavone, Self-microemulsifying pellets can significantly improve intestinal absorption of naringin and neohesperidin.