摘要
目的 分析艽龙胶囊在大鼠体内入血成分及其药代动力学与组织分布特性.方法 大鼠灌胃给予1.2 g/kg的艽龙胶囊后,采用HPLC法分析艽龙胶囊在大鼠体内入血成分的组织器官(心、肝、脾、肺、肾、胃、胰腺、大脑、十二指肠、结肠、回肠)10、60、120、240、360、540 min的药物浓度,并用DAS2.0软件计算药代动力学参数.结果 入血主要成分为马钱苷酸(Loga)、獐牙菜苦苷(Swert)、6-O-β-D-葡萄糖基龙胆苦苷(Glu)、龙胆苦苷(Gent)和獐牙菜苷(Sweroside,Swero)等5种成分;大鼠灌胃给药后,于60 min时各有效成分在血浆及组织中达到较高的浓度,各有效成分在胃肠道中均较高,其中龙胆苦苷含量最高.大脑和肺中含量均较低.结论 建立的HPLC法准确、方便,适用于艽龙胶囊在大鼠体内的药代动力学及组织分布的研究;血浆及组织中,尤其是消化器官中上述5种成分含量较高,说明其可能是制剂的主要功效成分.
Abstract
Objective To study the pharmacokinetics,and tissue distribution of Gentiana capsules in rats.Methods After intragastric administration of 1.2g/kg of Gentiana Longa capsules to rats,HPLC method was used to detect the drug concentrations in plasma and tissues(heart,liver,spleen,lung,kidney,stomach,pancreas,brain,duodenum,colon,ileum)at 10,60,120,240,360,540 min.The pharmacokinetic parameters were calculated by the DAS2.0.Result The main five components in the plasma were Loganic acid(Loga),Swertiamarin(Swert),and 6-O-β-D-glucosylgentiopicroside(Glu),Gentiopicroside(Gent),and Swertide(Swero).After intragastric adminis-tration in rats,the effective components reached high concentrations in plasma and tissues at 60 minutes.The con-tent of various active ingredients in the gastrointestinal tract was relatively high,with the highest content of gentiop-icroside.The content of various active ingredients in the brain and lungs was relatively low.Conclusion The estab-lished HPLC method is accurate,convenient,and suitable for the study of the pharmacokinetics and tissue distribu-tion of Gentiana macrophylla capsules in rats.The content of the above five components in plasma and tissues is high,especially in digestive organs,indicates that they may be the main functional components of the capsule.
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