摘要
目的:研究二氢杨梅素(dihydromyricetin,DMY)在大鼠胃和肠道中的吸收行为,为DMY新制剂的研究与开发提供依据。方法:运用在体胃研究模型和在体肠单向灌流模型,采用高效液相色谱法研究DMY在大鼠胃和不同肠段的吸收情况,并考察药物浓度(20,40,80μg·mL^(-1))对DMY肠吸收的影响。结果:DMY的胃吸收百分率为(2.3±0.9)%。在各肠段的吸收中,DMY的P_(eff)<5.0×10^(-5)cm·s^(-1),其中在空肠和结肠中的K_(a)和P_(eff)大于十二指肠和回肠(P<0.05)。以空肠为吸收肠段,与低、中浓度组相比,高浓度组中DMY的K_(a)和P_(eff)明显降低(P<0.05)。结论:胃部不是DMY的主要吸收和代谢部位。DMY为低渗透性药物,其在空肠和结肠部位的吸收较好。另外,DMY在吸收过程中存在高浓度饱和现象,表明DMY在肠道的转运可能有载体参与。
OBJECTIVE To investigate the absorption behavior of dihydromyricetin(DMY) in the stomach and intestine of rats,so as to provide a basis for the research and development of new DMY formulations.METHODS Using an in vivo gastric study model and an in vivo intestinal single pass perfusion model,the absorption of DMY in the stomach and different intestinal segments of rats was investigated by high performance liquid chromatography,and the effects of drug concentrations(20,40,80 μg·mL^(-1)) on the intestinal absorption of DMY were examined.RESULTS The percentage absorption of DMY in the stomach was(2.3±0.9)%.It was found the P_(eff) of DMY was lower than 5.0×10^(-5)cm·s^(-1).DMY was better absorbed in the jejunum and colon compared to the duodenum and ileum(P<0.05).Further,using the jejunum as the absorbing intestinal segment,K_(a) and P_(eff) of DMY were significantly lower in the high concentration group compared to those in the low and medium concentration groups(P<0.05).CONCLUSION The stomach is not the main site of absorption and metabolism of DMY.DMY is a low permeability drug,but it is better absorbed in the jejunum and colonic sites.In addition,the presence of high concentration saturation of DMY during absorption suggests that the drug DMY may have the involvement of carriers in the intestinal transit.
作者
赵诗莹
朱昱锦
任桥
毛家敏
刘小媛
叶静
张全
许小红
ZHAO Shi-ying;ZHU Yu-jin;REN Qiao;MAO Jia-min;LIU Xiao-yuan;YE Jing;ZHANG Quan;XU Xiao-Hong(Pharmaceutical Research Institute,School of Pharmacy,Chengdu Medical College,Sichuan Chengdu 610500,China;Development and Regeneration Key Lab of Sichuan Province,Chengdu Medical College,Sichuan Chengdu 610500,China)
出处
《中国医院药学杂志》
CAS
北大核心
2022年第14期1410-1414,共5页
Chinese Journal of Hospital Pharmacy
基金
国家自然科学基金(编号:81603045)
四川省医学青年创新研究项目(编号:Q20049)
成都医学院校基金(编号:CYZYB2011)。
关键词
二氢杨梅素
单向灌流法
在体胃吸收
在体肠吸收
质量法
dihydromyricetin
in situ single pass perfusion
gastric absorption
intestinal absorption
weight method
