摘要
目的制备高良姜素自微乳,考察其在大鼠在体肠吸收特征及体内药动学行为。方法建立大鼠在体单向肠灌流实验模型,采用高效液相色谱(HPLC)法测定灌流液中高良姜素浓度,考察高良姜素自微乳在各肠段中的吸收情况,计算相关吸收参数;以高良姜素混悬液为参比制剂,利用DAS2.1软件对大鼠血浆药物浓度-时间曲线进行拟合,计算相关药代动力学参数。结果高良姜素自微乳在大鼠整个肠段都有吸收,在十二指肠、空肠、回肠和结肠中的吸收速率常数(Ka)分别为高良姜素混悬液的2.37、1.70、2.29、3.98倍,表观吸收系数(P_(app))分别为高良姜素混悬液的3.58、2.56、3.57、5.16倍。高良姜素混悬液和自微乳的C_(max)分别为0.245、0.427 mg·L^(-1),t_(max)分别为1.789、1.411 h,AUC_(0-24 h)分别为1.207、2.059 mg·h·L^(-1),高良姜素自微乳相对于混悬液的生物利用度为220%。结论相对于高良姜素混悬液,高良姜素自微乳在各肠段均有良好的吸收,且显著提高了高良姜素在大鼠体内的口服生物利用度。
Objective The galangin self-microemulsion was prepared,and the intestinal absorption characteristics and pharmacokinetics of galangin self-microemulsion in rats were investigated.Methods The model of single-pass intestinal perfusion in rats was established.The concentration of galangin in intestinal perfusion was determined by HPLC to investigate the absorption of galangin self-microemulsion in each intestinal segment,and the relevant absorption parameters were calculated.Using galangin suspensions as a reference,the plasma drug concentrationtime curve was fitted by DAS2.1 software,and the related pharmacokinetic parameters were calculated.Results The galangin self-microemulsion was absorbed throughout the intestinal segments.The absorption rate constants Kain duodenum,jejunum,ileum and colon were 2.37,1.70,2.29 and 3.98 times of that in galangin suspensions,and the apparent absorption coefficients P_(app) were 3.58,2.56,3.57 and 5.16 times of that in galangin suspensions,respectively.The pharmacokinetic parameters C_(max) of galangin suspensions and galangin self-microemulsion were0.245,0.427 mg·L^(-1),tmaxwere 1.789,1.411 h,and AUC_(0-24 h)were 1.207,2.059 mg·h·L^(-1).The bioavailability of galangin self-microemulsion compared with galangin suspensions was 220%.Conclusion Compared with galangin suspensions,galangin self-microemulsion had good absorption in each intestinal segment,which significantly improved the oral bioavailability of galangin in rats.
作者
张欣
陈曦文
卢昊
许汉林
ZHANG Xin;CHEN Xiwen;LU Hao;XU Hanlin(College of Pharmacy,Hubei University of Chinese Medicine,Wuhan 430065 Hubei,China)
出处
《中药新药与临床药理》
CAS
CSCD
北大核心
2021年第11期1699-1704,共6页
Traditional Chinese Drug Research and Clinical Pharmacology
关键词
高良姜素
自微乳
在体肠吸收
药物动力学
口服生物利用度
大鼠
Galangin
self-microemulsion
in situ intestinal absorption
pharmacokinetics
oral bioavailability
rats
