摘要
【目的】研究超微粉碎技术对黄连解毒散有效成分小檗碱的药代动力学影响。【方法】黄连解毒散分别制成超微粉和普通细粉,给家兔灌服,用HPLC法测定家兔体内小檗碱的血药浓度,血药浓度-时间数据经PKS(Pharmaceutical Kinetics Software)药代动力学分析软件处理,比较黄连解毒散超微粉和细粉中的小檗碱在家兔体内的药代动力学参数。【结果】黄连解毒散超微粉和细粉中小檗碱的药代动力学最佳模型均为一级吸收二室模型。其主要药动学参数分别是:吸收相半衰期(t1/2α)为1.08和1.33h,消除相半衰期(t1/2β)为28.72和23.56h,达峰时间(Tpeak)为1.480和1.934h,达峰浓度(Cmax)为0.0913和0.0565μg·ml-1,药时曲线下面积(AUC)为0.895和0.613(μg·ml-1)·h。与细粉比较,黄连解毒散超微粉达峰时间缩短;达峰浓度提高;药时曲线下面积增加。【结论】超微粉碎技术可以提高黄连解毒散有效成分小檗碱的生物利用度。
【Objective】 To study the pharmacokinetics of berberine in ultramicro pulverization of Huanglian jiedusan （HLJDS） in rabbits in vitro.【Method】 The plasma concentration of berberine was determined by HPLC in two groups of rabbits after they were administered with ultramicro-pulverised powder and with ordinary powder of HLJDS by gastrogavage, respectively. The plasma concentration-time data of berberine was analyzed by Pharmaceutical Kinetics Software （PKS）. Pharmacokinetic characteristics in both groups were compared.【Result】Two-compartment open model was the optimum one of berberine in the groups. The pharmacokinetic parameters were as follows： t1/2α was1.08h and 1.33h, t1/2β was 28.72 h and 23.56 h, Tpeak was 1.480 h and 1.934 h, Cmax was 0.0913 μg·ml^-1 and 0.0565 μg·ml^-1, AUC was 0.895 （μg·ml^-1）·h and 0.613 （μg·ml^-1）·h, respectively. 【Conclusion】Tpeak was shorter, Cmax was higher and bioavailability was better in ultramicro-pulverised powder group than in ordinary powder group. It was indicated that the bioavailability of berberine in HLJDS could be greatly improved by the technique of ultromicro-pulverization.
出处
《中国农业科学》
CAS
CSCD
北大核心
2008年第3期875-879,共5页
Scientia Agricultura Sinica
基金
国际科技合作重点项目(2003DF030008)
福建省科技厅重点项目(2004N031)
福建省自然科学基金项目(B0710002)
关键词
黄连解毒散
超微粉
小檗碱
药代动力学
生物利用度
Huanglian jiedusan （HLJDS）
Ultra-micropowder
Berberine
Pharmacokinetics
Bioavailability
作者简介
马玉芳（1970-），女，宁夏中宁人，副教授，硕士，研究方向为临床兽医学。E-mail：myfau850@sohu.com。
通讯作者黄一帆（1954-），男，福建闽清人，教授，研究方向为天然药物加工应用。Tel：0591-83789712；E-mail：zjhyfang@163.com
