摘要
目的:建立中药复杂体系中多成分在大鼠体内药代动力学研究的评价方法。方法:大鼠口服灌胃白花蛇舌草组分胶囊内容物混悬液,在不同时间点眼眶取血,血浆样品经紫外-可见分光光度扫描,计算吸光度-波长曲线下面积(吸波面积),得各时间点大鼠体内混合药物的血药总质量浓度,结合DAS2.0软件计算药代动力学参数,并与高效液相色谱法(HPLC)获得的槲皮素、齐墩果酸、豆甾醇各单一成分的血药浓度和体内参数相比较,确定2种方法应用的可行性。结果:吸波面积法显示组分胶囊中混合总药物在大鼠体内药-时过程符合一室模型,达峰时间(Tmax),药峰浓度(Cmax)和药时曲线下面积AUC0-∞分别为0.5 h,2.85 mg·L-1和26.81 mg·L-1·min-1。HPLC显示槲皮素、齐墩果酸和豆甾醇的药-时过程均呈一室模型,槲皮素、齐墩果酸、豆甾醇的Tmax分别为1.0,0.5,0.5 h,Cmax分别为0.17,0.69,3.84 mg·L-1,AUC0-∞分别为0.71,10.69,12.49 mg·L-1·min。结论:吸波面积法可用于白花蛇舌草组分胶囊中多成分在大鼠体内药代动力学的研究,与HPLC联用可较好地解决中药制剂中整体和个体成分同步测试的问题,且两者具有较好的互补性。
Objective： To build an evaluation method for in vivo pharmacokinetic study on multicomponents in a complex system of traditional Chinese medicines（ TCMs） in rats. Method： After mixed suspension of capsules with components from Hedyotis diffusa was orally administered to rats,blood samples were collected from eye of rats at different time points. Plasma samples were scanned by ultraviolet-visible spectrophotometer to calculate area under the absorbance-wavelength curve（ AUAWC） and then produce total plasma concentration in rats at each time point. Pharmacokinetic parameters were calculated with DAS2. 0 software and compared with data of every single component-quercetin,oleanolic acid and stigmasterol in plasma samples obtained by high performance liquid chromatography（ HPLC）,in order to determine feasibility of the above two methods. Result： With method of AUAWC,mixed total concentration of capsules conformed to one-compartment model in rats,with Tmaxat 0. 5 h,Cmaxof 2. 85 mg·L^-1,AUC0-∞of 26. 81 mg·L^-1·min^-1. HPLC method also showed a one-compartment model for quercetin,oleanolic acid and stigmasterol,with Tmaxat 1 h,Cmaxof 0. 17mg·L^-1,AUC0-∞of 0. 71 mg·L^-1·min^-1 for quercetin; Tmaxat 0. 5 h,Cmaxof 0. 69 mg·L^-1,AUC0-∞of 10. 69mg·L^-1·min^-1for oleanolic acid; Tmaxat 0. 5 h,Cmaxof 3. 84 mg·L^-1,AUC0-∞of 12. 49 mg·L^-1·min^-1for stigmasterol, respectively. Conclusion： AUAWC can be used to study pharmacokinetics of capsules with components from H. diffusa in rats. Its combination with HPLC can better solve synchronous test for whole and individual components in TCM preparations with a better complementarity between them.
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2015年第16期83-87,共5页
Chinese Journal of Experimental Traditional Medical Formulae
基金
福建省科技平台建设项目(2010Y2004)
关键词
组分胶囊
吸波面积法
白花蛇舌草
槲皮素
齐墩果酸
豆甾醇
capsules with components
area under the absorbance-wavelength curve
Hedyotis diffusa
quercetin
oleanolic acid
stigmasterol
