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目的:研究补肾温肺微乳中淫羊藿苷的大鼠不同肠段的吸收特性,并考察P-糖蛋白(P-gp)对其肠吸收的影响。方法:采用大鼠在体单向肠灌流实验,采用HPLC法测定淫羊藿苷的含量,分别研究肠段不同吸收部位、不同淫羊藿苷浓度、Pgp抑制药维拉帕米对淫羊藿苷单体及其在补肾温肺微乳中吸收的影响。结果:淫羊藿苷单体在各肠段的吸收速率常数(Ka)和表观吸收系数(Papp)差异显著(P<0.01);在0.10~0.40 ml·min-1流速内和0.1~1.0 mg·ml-1质量浓度内,十二指肠吸收速率常数和表观吸收系数无显著差异;补肾温肺微乳中淫羊藿苷的肠灌流试验结果与淫羊藿苷单体相比略小,但无显著差异;P-gp抑制药对淫羊藿苷的肠吸收有影响,加入0.1 mmol·L-1盐酸维拉帕米后,Ka和Papp分别为(2.13±0.66)×10-2h·cm-1和(0.23±0.051)×10-6cm·s-1,与不加P-gp抑制药组相比较差异显著(P<0.01)。结论:淫羊藿苷属于难吸收化合物,淫羊藿苷和补肾温肺微乳中淫羊藿苷在大鼠不同肠段的吸收具有相似的吸收特性;其在大鼠肠内的吸收受P-gp外排转运影响。因此,推测淫羊藿苷可能是P-gp的底物。
OBJECTIVE: To study the absorption characteristics of icaritin in different intestine of rats with tonifying kidney yang lung microemulsion and to investigate the effect of P-glycoprotein (P-gp) on intestinal absorption. Methods: In vivo rat intestinal perfusion experiments using HPLC method determination of icariin content, different parts of the bowel study, different concentrations of icariin, Pgp inhibitor verapamil Epimedium Glycoside Monomers and Their Absorption in Kidney - warming Lung Microemulsions. Results: The difference of the absorption rate constant (Ka) and apparent absorption coefficient (Papp) of icariin monomer in each segment was significant (P <0.01). In the range of 0.10-0.40 ml · min-1, mg · ml-1 mass concentration, the duodenum absorption rate constant and the apparent absorption coefficient was no significant difference; kidney warming lung microemulsion Icariin intestinal perfusion test results compared with Icariin monomer slightly Small, but no significant difference; P-gp inhibitor of icarrin intestinal absorption affected, adding 0.1 mmol·L-1 verapamil hydrochloride, Ka and Papp were (2.13 ± 0.66) × 10- 2h · cm-1 and (0.23 ± 0.051) × 10-6cm · s-1, which were significantly different from those without P-gp inhibitor (P <0.01). Conclusion: Icariin belongs to the refractory compounds. Icariin and Icariin in Wendan warm lung microemulsion have similar absorption characteristics in different intestinal segments of rats. The intestinal absorption of icariin is affected by P -gp efflux transport impact. Therefore, it is speculated that icariin may be the substrate of P-gp.