摘要
目的考察β-蜕皮甾酮的肠道吸收特性,探究β-蜕皮甾酮生物利用度低的原因。方法采用大鼠在体单向肠灌流模型,运用HPLC法测定药物浓度。分别考察小肠吸收部位(十二指肠、空肠、回肠、结肠),药物浓度,灌流液pH值,肠道菌群对β-蜕皮甾酮吸收的影响。结果β-蜕皮甾酮在不同肠段的吸收速率常数(K_a)由高到低依次为回肠、结肠、空肠、十二指肠;以β-蜕皮甾酮浓度为50、100、200μg·mL^(-1)的含药缓冲液在空肠进行吸收实验,K_a和小肠有效渗透系数(P_(eff))差异无统计学意义;药物的吸收程度在空肠随pH值升高而增加;大鼠肠道菌群失衡会干扰β-蜕皮甾酮的吸收。结论β-蜕皮甾酮在各个肠段均有吸收,但在肠道下部吸收较好;吸收机制为被动扩散;药物在碱性环境下吸收较好;肠道菌群对β-蜕皮甾酮吸收有显著影响。
Objective To determine the intestinal absorption characteristics ofβ-ecdysterone and to explore the reasons for the low bioavailability ofβ-ecdysterone.Methods A rat model of in vivo intestinal perfusion was established to determine the drug concentration by HPLC.The absorption sites of the small intestine(the duodenum,the jejunum,the ileum,and the colon),drug concentration,and pH of perfusateand and intestinal flora were investigated for the absorption ofβ-ecdysterone.Results The order of absorption rate constant(Ka)ofβ-ecdysterone in different intestinal segments from high to low was the ileum,the colon,the jejunum and the duodenum.The drug-containing buffer was 50,100,and 200μg·mL-1 in the mass concentration.In the experiment,there was no significant difference between Ka and Peff.The degree of drug absorption increased with the increase of pH value.The imbalance of intestinal flora in the rats interfered with the absorption ofβ-ecdysterone.Conclusionβ-ecdysterone is absorbed in all intestinal segments,but better absorbed in the lower part of the intestine.The absorption mechanism is passive diffusion,with better absorption in the alkaline environment.The intestinal flora has a significant effect on the absorption ofβ-ecdysterone.
作者
戴浩志
朱裕林
陈卫东
DAI HAO-Zhi;ZHU YU-Lin;CHEN WEI-Dong(School of Pharmaceutical Sciences,Anhui University of Chinese Medicine,Hefei 230012;Department of Pharmacy,First Affiliated Hospital,Bengbu Medical College,Bengbu Anhui 233004)
出处
《中南药学》
CAS
2019年第5期687-691,共5页
Central South Pharmacy
基金
安徽省自然科学基金(No.1608085QH213)
关键词
β-蜕皮甾酮
在体单向肠灌流
吸收
肠道菌群
β-ecdysterone
in vivo intestinal perfusion
absorption
intestinal flora
