摘要
目的:研究穿山龙薯蓣皂苷纳米结构脂质载体的大鼠在体肠吸收特性。方法:采用高效液相色谱法测定穿山龙薯蓣皂苷纳米结构脂质载体中穿山龙薯蓣皂苷含量;大鼠在体单向灌流法研究吸收部位,药物浓度对穿山龙薯蓣皂苷肠吸收的影响;比较穿山龙提取物和纳米制剂在体肠吸收特性。结果:穿山龙薯蓣皂苷纳米结构脂质载体在大鼠全肠段均有吸收,其在不同肠段的吸收速率常数(absorption rate constant,Ka)和表观吸收系数(apparent absorption coefficient,Papp)从大到小依次为:回肠>空肠>十二指肠>结肠;不同质量浓度(30,60和120μg·m L^-1)的穿山龙薯蓣皂苷纳米结构脂质载体,其Ka和Papp没有显著性差异,提示在实验浓度范围内,穿山龙薯蓣皂苷纳米结构脂质载体在大鼠全肠段的吸收没有浓度依赖性,吸收机制可能属于被动扩散;穿山龙薯蓣皂苷纳米结构脂质载体组和薯蓣皂苷提取物组比较,Ka和Papp有显著性差异(P <0. 05),且纳米制剂在空肠的吸收系数是薯蓣皂苷提取物的1. 28倍。结论:穿山龙薯蓣皂苷纳米结构脂质载体在空肠和回肠肠段吸收良好且吸收速率不受药物浓度的影响,制备成纳米结构脂质载体后能够增加药物的生物利用度,具有良好的应用前景。
Objective:To study the absorption characteristics of the dioscin nano-structured lipid carriers in rat intestine.Methods:High-performance liquid chromatography(HPLC)was used to determine the content of dioscin in the dioscin nano-structured lipid carrier.The absorption site and the effect of drug concentration on intestinal absorption of dioscin in rats were studied by one-way perfusion in vivo.The absorption characteristics of Dioscorea nipponica extract and the nanopreparation in the body intestine were compared.Results:The dioscin nano-structured lipid carriers can be absorbed in whole intestine of rats.The absorption rate constant(Ka)and the apparent absorption coefficient(Papp)of the dioscin nano-structured lipid carrier in different parts of the whole intestine of rats were as follows:ileum>jejunum>duodenum>colon.There was no significant difference in Kaand Pappof the dioscin nano-structured lipid carrier at different mass concentrations(30,60 and 120μg·m L^-1),suggesting that the absorption of the dioscin nano-structured lipid carrier in the whole intestine of rats was not concentration-dependent and the absorption mechanism might be passive diffusion.There were significant differences in Ka and Papp between dioscin nano-structured lipid carrier group and Dioscorea nipponica extract group(P<0.05),in which the Papp of the nano preparation in jejunum was 1.28-folds of that for diosgenin extract.Conclusion:The nano-structured lipid carrier of dioscin was well absorbed in jejunum and ileum,which isnot affected by drug concentration.The preparation of the nanostructured lipid carrier can increase the bioavailability of the drug,obtaining a good application prospect.
作者
胡坤霞
焦莹
巨红叶
韩立柱
王斌
唐志书
宋逍
HU Kun-xia;JIAO Ying;JU Hong-ye;HAN Li-zhu;WANG Bin;TANG Zhi-shu;SONG Xiao(College of Pharmacy,Shanxi University of Chinese Medicine,Xianyang 712046,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2020年第9期1045-1051,共7页
Chinese Journal of New Drugs
基金
国家自然科学基金项目(81373944,81373978)
陕西省科学技术厅课题(2012KTCQ03-13)
陕西省中药基础与新药研究重点实验室(1008)
陕西省中药制药重点学科专项资助(1008)
国家中医药管理局中药制剂三级实验室(1008)。
