大鼠口服二苯乙烯苷及其β-环糊精包合物的组织分布研究

Study on Tissue Distribution of Stilbene Glycoside( THSG) and its β-cyclodextrin Inclusion

目的:通过对大鼠分别灌胃给予二苯乙烯苷(THSG)单体及其β-环糊精(β-CD)包合物,研究THSG在大鼠主要8种脏器组织中的含量-时间分布。方法:首先将给药后15,30,60 min各组织样品取出后处理,随后采用高效液相-紫外法(HPLC-UV)测定生物样品中THSG含量。结果:THSG在多个组织中均能被检测到,证明其体内组织分布较为广泛,THSG-β-CD包合物对大鼠灌胃给药后,虽然THSG的血药浓度较给予同剂量的THSG单体有显著增加,但在脾脏、肺、脑、胰腺中的分布并无显著差异;而在心脏、肾脏、脂肪组织中的分布则表现出含量达峰时间延后的特点。结论:β-CD的包合作用仅改变了药物在组织中的达峰时间,并不会造成药物在组织中的蓄积。

Objective： The tissue distribution characteristics of stilbene glycoside （THSG） and its β- cyclodextrin inclusion in 8 tissues after oral administration to rats were studied. Method ： The samples of 8 different tissues were collected at 15, 30, 60 rain, respectively. The content of THSG was determined by HPLC-UV. Result： The HPLC-UV method established was available for analysis of THSG in tissues and met the requirements of biological sample analysis. There was no significant difference of THSG concentration in the spleen, lung, brainand pancreas between THSG group and β-CD-THSG complex group. However, the concentration of THSG in the tissues materials of heart, kidneys and fat was higher by given β-CD-THSG complex. In addition, tmax of THSG in tissues was delayed by given β-CD-THSG complex, which was observed obviously in heart, liver, spleen and fat tissue. Conclusion：β -CD inclusion only changed the tmax of THSG in the tissues, and will not cause the accumulation in the tissues.