厚朴排气合剂主要药效成分在不同种属动物血浆中蛋白结合率的比较  

Comparison of protein binding rate of main effective components of Houpu paiqi mixture in animal plasma of different species

作　　者：郭明鑫 范文韬 吴霞[2] 沈颖 胡志强 GUO Mingxin;FAN Wentao;WU Xia;SHEN Ying;HU Zhiqiang(Dept.of Pharmacy,the Affiliated Yixing Hospital of Jiangsu University,Jiangsu Yixing 214200,China;New Drug Research and Development Center of Guangdong Pharmaceutical University,Guangzhou 510006,China)

机构地区：[1]江苏大学附属宜兴医院药学部,江苏宜兴214200 [2]广东药科大学新药研发中心,广州510006

出　　处：《中国药房》2022年第24期2990-2994,共5页China Pharmacy

基　　金：广东省自然科学基金资助项目(No.2018A030313907)。

摘　　要：目的测定厚朴排气合剂主要药效成分厚朴酚、和厚朴酚在不同种属动物血浆中的蛋白结合率并比较种属差异。方法采用平衡透析法,将牛、兔、大鼠血浆(即透析内液)置于4.5、9.0、13.5μg/mL(按厚朴排气合剂饮片质量计)的含药透析液中平衡透析24 h;采用超高效液相色谱-串联三重四极杆质谱技术检测透析内、外液中厚朴酚、和厚朴酚的质量浓度,计算血浆蛋白结合率并进行比较。结果在4.5、9.0、13.5μg/mL质量浓度下,厚朴酚在牛血浆中的蛋白结合率分别为(68.13±4.52)%、(74.34±1.12)%、(86.22±0.50)%,在兔血浆中的蛋白结合率分别为(59.55±4.62)%、(72.81±4.56)%、(86.40±1.91)%,在大鼠血浆中的蛋白结合率分别为(56.63±2.87)%、(77.81±1.83)%、(83.18±0.65)%;和厚朴酚在牛血浆中的蛋白结合率分别为(34.82±1.67)%、(40.29±3.28)%、(63.57±0.59)%,在兔血浆中的蛋白结合率分别为(34.25±5.62)%、(62.12±7.36)%、(80.86±4.01)%,在大鼠血浆中的蛋白结合率分别为(37.06±3.28)%、(52.61±1.69)%、(79.83±7.38)%,组间比较差异大多具有统计学意义(P<0.05或P<0.01)。结论厚朴排气合剂主要药效成分厚朴酚、和厚朴酚的血浆蛋白结合率存在明显的种属差异,且有一定的浓度依赖趋势。OBJECTIVE To determine the protein binding rates of main effective components in Houpu paiqi mixture as magnolol and honokiol in animal plasma of different species,and compare the differences among species.METHODS The plasma of bovine,rabbit and rat(internal dialysate)was placed in 4.5,9.0 and 13.5μg/mL(according to the weight of the decoction pieces of Houpu paiqi mixture)dialysate containing drug for 24 h by equilibrium dialysate method.The concentrations of magnolol and honokiol in dialysis internal and external fluids were determined by ultra-performance liquid chromatography-tandem triple quadrupole mass spectrometry,and the plasma protein binding rates were calculated and compared.RESULTS At the concentrations of 4.5,9.0 and 13.5μg/mL,the protein binding rates of magnolol were(68.13±4.52)%,(74.34±1.12)%and(86.22±0.50)% in bovine plasma,(59.55±4.62)%,(72.81±4.56)% and(86.40±1.91)% in rabbit plasma,and(56.63±2.87)%,(77.81±1.83)%and(83.18±0.65)% in rat plasma,respectively.The protein binding rates of honokiol were(34.82±1.67)%,(40.29±3.28)% and(63.57±0.59)% in bovine plasma,(34.25±5.62)%,(62.12±7.36)% and(80.86±4.01)% in rabbit plasma,and(37.06±3.28)%,(52.61±1.69)% and(79.83±7.38)% in rat plasma,respectively.There was generally statistical significance among those groups(P<0.05 or P<0.01).CONCLUSIONS There are significant species differences in plasma protein binding rates of magnolol and honokiol,the main effective components of Houpu paiqi mixture,in a certain concentration-dependent trend.

关 键 词：厚朴排气合剂 厚朴酚 和厚朴酚 血浆蛋白结合率 平衡透析法 牛血浆 兔血浆 大鼠血浆 

分 类 号：R969.1[医药卫生—药理学] R927.2[医药卫生—药学]