摘要
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 。
AIM:To clarify the difference in the absorption of Breviscapine from vaired intestinal segments,to investigate the mechanism of Breviscapine from intestine at different concentrations, and to study the effect of pH value and some absorption enhancer on the absorption of Breviscapine.METHOD:Testing their absorption and wall intestinal permeability with the use of an in situ rat intestine technique.RESULT:When the concentration was raised from 50 to 400 μg/ml,the uptake of Breviscapine increased and did not appeal saturable,whereas the permeability coefficience kepted at an equilibrium level. The absorption of Breviscapine was not influenced by pH value between pH 6 0 and pH 7 4 The percentage disappearance and the permeability coefficience of Breviscapine from vaired intestinal segments kept at the same level. And the absorption enhancer Τween 80 and Phospholipid in rat intestine could enhance the absorption of Breviscapine. The pharmacokinetic parameters were as follows: k a=0 0163±0 0064 min -1 ,and k e=0 0668±0 015min -1 .CONCLUSION:The absorption of Breviscapine by intestine is mainly via passive transport mechanism.And so,the bioavailability of Breviscapine would be improved with enhancing the solubility in light and permeability of intestinal wall. Breviscapine can be absorbed in whole intestinal segments,so Breviscapine sustained release tablets can be prepared.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2003年第1期65-69,共5页
Journal of China Pharmaceutical University
关键词
灯盏花素
小肠吸收
在体循环
吸收促进剂
Breviscapine
Intestinal absorption
In situ recirculation
Absorption enhancer
