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目的 :研究灯盏花素最佳吸收部位和探讨灯盏花素的吸收机理。方法 :采用大鼠在体循环方法研究灯盏花素的小肠吸收和肠壁通透性。结果 :在 5 0～ 40 0ug/ml浓度范围内吸收量与浓度呈线性关系 ,无高浓度饱和现象 ,P值基本保持不变 ;在pH 6 0至pH 7 4范围内吸收不受pH影响 ;在各肠段的百分吸收率和肠壁通透系数均无明显差异 ;促吸剂Tween 80和大豆磷脂对灯盏花素具有明显的促进吸收作用 ;吸收动力学参数为 :ka=0 0 163± 0 0 0 64min-1,ke=0 0 668± 0 0 15min-1。结论 :灯盏花素在大鼠小肠主要以被动扩散方式吸收 ,提高药物溶解度和采用促吸方法提高通透性 ,将能有效地促进灯盏花素的吸收 ,达到提高生物利用度的目的 ;灯盏花素在整个肠段均有吸收 ,可以将灯盏花素研制成缓释片剂
Objective: To study the optimum absorption site of breviscapine and to explore the absorption mechanism of breviscapine. METHODS : Rats were used to study the intestinal absorption and permeability of breviscapine in the systemic circulation. RESULTS: There was a linear relationship between the absorption and concentration in the concentration range of 50-400 ug/ml. There was no high concentration saturation, and the P value remained basically unchanged. The pH was not affected by the pH in the range from pH 60 to pH 7.4; Absorption rate and intestinal permeability coefficient were not significantly different in each intestinal segment; Tween 80 and soybean phospholipids had obvious promotion effect on breviscapine; the absorption kinetic parameters were: ka=0 0 163 ± 0 0 0 64min-1, ke = 0 0 668 ± 0 0 15min-1. CONCLUSION: Breviscapine is mainly absorbed in the rat small intestine by passive diffusion. Increasing the solubility of the drug and increasing the permeability by the method of promoting the absorption of breviscapine can effectively promote the absorption of breviscapine and increase the bioavailability. Is absorbed throughout the entire intestine and can be developed into sustained-release tablets of breviscapine