基于中药整体成分的参白纳米混悬剂大鼠体内药代动力学分析  

In vivo Pharmacokinetic Analysis of Shenbai Nanosuspension in Rats Based on Overall Composition of Chinese Materia Medica

作　　者：刘伟婷 简凤娇 黄可心 李孝栋[1] LIU Weiting;JIAN Fengjiao;HUANG Kexin;LI Xiaodong(School of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou 350122,China)

机构地区：[1]福建中医药大学药学院,福州350122

出　　处：《中国实验方剂学杂志》2024年第2期164-171,共8页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：福建省高校产学合作项目(2021Y4016)。

摘　　要：目的:明确参白纳米混悬剂中药物整体成分大鼠体内药代动力学测定方法的科学性,为多成分复杂体系中药制剂的体内研究提供方法指导和理论依据。方法:采用吸波面积法(AUAWC)测定不同时间大鼠血浆中参白汤剂与参白纳米混悬剂中总皂苷和总多糖等为主的整体成分药物浓度,高效液相色谱法(HPLC)测定个体成分人参皂苷Rg1的药物浓度,并进行方法学验证。将获得整体成分的药代动力学参数与人参皂苷Rg1的药代动力学参数比较,评价2种制剂的体内运行特点。结果:AUAWC与HPLC的方法学考察均符合要求。AUAWC分析显示,参白汤剂组与参白纳米混悬剂组中整体成分房室拟合均呈一室模型,半衰期(t_(1/2))分别为2.43 h和2.04 h,参白纳米混悬剂的相对生物利用度为138.99%;HPLC检测显示,参白汤剂组和参白纳米混悬剂组中人参皂苷Rg1呈二室模型,分布半衰期(t_(1/2α))分别为0.13 h和2.55 h,消除半衰期(t_(1/2β))分别为14.28 h和3.85 h,参白纳米混悬剂相对生物利用度为127.49%。与参白汤剂比较,参白纳米混悬剂中整体成分和人参皂苷Rg1的达峰时间(t_(max))、达峰浓度(C_(max))与药-时曲线下面积(AUC)增加。结论:建立的AUAWC可用于中药制剂整体成分药代动力学的研究,与HPLC测得的个体成分结果具有互补性,可为中药新剂型的体内研究提供有益借鉴。Objective:To clarify the scientific validity of in vivo pharmacokinetic determination of the whole drug composition in Shenbai nanosuspension in rats,and to provide methodological guidance and theoretical basis for the in vivo study of multi-component complex system of traditional Chinese medicine(TCM)preparations.Method:The concentration of the overall components,mainly total saponins and total polysaccharides in Shenbai decoction and Shenbai nanosuspension,was determined in rat plasma at different times by area under the absorbance-wavelength curve method(AUAWC),and the concentration of individual ginsenoside Rg1 was determined by high performance liquid chromatography(HPLC),and the methodology was verified.The pharmacokinetic parameters of the whole component were compared with those of ginsenoside Rg1 to evaluate the in vivo operational characteristics of the two preparations.Result:The methodological investigations of AUAWC and HPLC were in accordance with the requirements.AUAWC analysis showed that the overall components in both the decoction group and the nanosuspension group showed a one-compartment model,with half-life(t_(1/2))of 2.43 h and 2.04 h,respectively.The relative bioavailability of Shenbai nanosuspension was 138.99%.HPLC assay showed that ginsenoside Rg1 in the decoction group and the nanosuspension group showed a two-compartment model,with distribution half-life(t_(1/2α))of 0.13 h and 2.55 h,and elimination half-life(t_(1/2β))were 14.28 h and 3.85 h,respectively.The relative bioavailability of Shenbai nanosuspension was 127.49%.Compared with Shenbai decoction,the time to peak(t_(max)),peak concentration(C_(max))and area under the drug-time curve(AUC)of the overall components and ginsenoside Rg1 in Shenbai nanosuspension were increased.Conclusion:The established AUAWC can be used for the pharmacokinetic study of the overall components of TCM preparations,which is complementary to the results of individual components measured by HPLC,and can provide useful reference for the in vivo study of ne

关 键 词：中药整体成分 参白纳米混悬剂 吸波面积法 高效液相色谱法(HPLC) 药代动力学 抗肿瘤 生物利用度 

分 类 号：R22[医药卫生—中医基础理论] R94[医药卫生—中医学] R28[理学—分析化学] O657[理学—化学]