摘要
中药复方制剂成分复杂,舒肝宁注射液作为临床应用广泛的中药注射剂,其体内过程尚不明确,测定药物的血浆蛋白结合率对药物的药动学、药效学研究具有重要意义。该实验采用平衡透析法结合UPLC-MS/MS技术测定舒肝宁注射液中对羟基苯乙酮、咖啡酸、黄芩素、千层纸素A、栀子苷、黄芩苷、木犀草苷、千层纸素A-7-O-β-D-葡萄糖醛酸苷、野黄芩苷、金丝桃苷10种成分在大鼠及人血浆中的血浆蛋白结合率,为进一步阐明舒肝宁注射液的体内过程及指导临床用药提供理论依据。结果显示,除黄芩素及栀子苷外其他8种成分在人血浆中结合率高于大鼠血浆,且均存在种属差异。在人血浆中,除栀子苷、咖啡酸及黄芩苷外,其余7种成分血浆蛋白结合率均高于80%,其中黄芩素及千层纸素A高于90%,除栀子苷外各成分与血浆蛋白结合程度高。
Traditional Chinese medicine(TCM) compound preparations have complex compositions.As a widely used TCM injection,Shuganning Injection,its in vivo processes are not yet fully understood.Determining the plasma protein binding rate is of great significance for pharmacokinetic and pharmacodynamic studies.In this experiment,the equilibrium dialysis method combined with UPLC-MS/MS technology was used to determine the plasma protein binding rates of 10 components,including p-hydroxyacetophenone,caffeic acid,baicalein,oroxylin A,geniposide,baicalin,cynaroside,oroxylin A-7-O-β-D-glucuronide,scutellarin,and hyperoside,in Shuganning Injection in rat and human plasma to provide a theoretical basis for further elucidating the in vivo processes of Shuganning Injection and guiding clinical medication.The results showed that,except for baicalein and geniposide,the plasma protein binding rates of the other eight components were higher in human plasma than in rat plasma,and there were interspecies differences.In human plasma,except for geniposide,caffeic acid,and baicalin,the plasma protein binding rates of the remaining seven components were above 80%,with baicalein and oroxylin A exceeding 90%.All components exhibit a high level of binding to plasma proteins,with the exception of geniposide.
作者
肖金超
王玲
张丽
迟明艳
黄勇
巩仔鹏
郑林
何峰
XIAO Jin-chao;WANG Ling;ZHANG Li;CHI Ming-yan;HUANG Yong;GONG Zi-peng;ZHENG Lin;HE Feng(State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Provincial Key Laboratory of Pharmaceutics,Guizhou Medical University,Guiyang 550004,China;School of Pharmaceutical Sciences,Guizhou Medical University,Guiyang 550004,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2023年第22期6183-6190,共8页
China Journal of Chinese Materia Medica
基金
贵州省科技成果应用及产业化计划项目(黔科合成果[2022]013)
贵州省高层次创新型人才项目(黔科合平台人才-GCC[2022]031-1)
贵州省科技支撑计划项目(黔科合支撑[2023]一般158,黔科合中引地[2023]006)。
