黄芩-黄连煎煮共沉淀的物质基础、形貌以及对煎煮液体内过程的影响研究  

Composition and morphology of Scutellariae Radix-Coptidis Rhizoma decoction co-precipitate and effect on in vivo behavior of decocting liquid

作　　者：林龙飞[1] 陈功森 李慧[1] 杨洪军[2] LIN Long-fei;CHEN Gong-sen;LI Hui;YANG Hong-jun(Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700,China;China Academy of Chinese Medical Sciences,Beijing 100700,China)

机构地区：[1]中国中医科学院中药研究所,北京100700 [2]中国中医科学院,北京100700

出　　处：《中国中药杂志》2023年第21期5790-5797,共8页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(82204637)。

摘　　要：黄芩-黄连为许多复方中常配伍相须使用的清热燥湿经典药对,其在合煎过程中会产生大量沉淀,但沉淀物的成分组成、形貌结构,以及是否会影响黄芩-黄连煎煮液的体内行为,目前尚未见明确报道。该研究采用高效液相色谱、高分辨质谱等对黄芩-黄连煎煮共沉淀物质基础进行分析,采用扫描电子显微镜、质谱成像分析其外观形貌,并采用大鼠分析共沉淀对黄芩-黄连煎煮液中主要成分体内过程的影响。研究结果表明,盐酸黄连碱、盐酸小檗碱、表小檗碱、巴马汀、黄芩苷、千层纸素A-7-O-β-D-葡萄糖醛酸苷、汉黄芩苷、黄芩素8个成分是共沉淀的主要组成成分,其中又以黄芩苷、盐酸小檗碱含量最高,约占总重的60%,此外共沉淀中含有18%鞣质;形貌分析表明黄芩-黄连煎煮共沉淀的粒径为600 nm左右的类球形微粒;药代动力学研究表明,通过口服给予大鼠黄芩-黄连合煎液冻干粉及单煎液冻干粉,其主要成分黄芩苷体内的AUC与C_(max)、t_(1/2)、T_(max)等均有明显差异。以上说明,煎煮过程产生的沉淀会影响黄芩-黄连药对主要成分的体内行为,会使黄芩苷在体内的吸收程度降低、减少药物突释程度,一定程度上可避免不良反应或副作用的发生。Scutellariae Radix-Coptidis Rhizoma(SR-CR) herbal pair is commonly used in many compound prescriptions for their synergistic heat-clearing and dampness-drying properties.During the decoction process,a substantial amount of precipitate is generated.However,there have been no explicit reports on the composition,morphology,and potential effects of this precipitate on the in vivo behavior of SR-CR decoction.This study employed high-performance liquid chromatography(HPLC),high-resolution mass spectrometry,and other techniques to analyze the composition of the co-precipitate in the decoction of SR-CR.Scanning electron microscopy and mass spectrometry imaging were used to analyze its appearance and morphology.Additionally,rats were used to investigate the effects of the co-precipitate on the in vivo behavior of the main components in the SR-CR decoction.The research findings indicated that eight components,including coptisine,berberine,epiberberine,palmatine,baicalin,oroxylin A-7-O-β-D-glucuronide,wogonoside and baicalein,constituted the primary composition of the co-precipitate.Among these,baicalin and berberine hydrochloride were the most abundant,accounting for about 60% of the total weight.Moreover,the co-precipitate contained 18% tannins.Morphological analysis revealed that the particles in the SR-CR decoction precipitate were spherical microparticles with an average diameter of around 600 nm.Pharmacokinetic research demonstrated that there were significant differences in the AUC,C_(max),t_(1/2),and T_(max) of baicalin,a major component,in rats administered with lyophilized powders of the combined decoction and single decoctions of SR-CR orally,suggesting that the precipitate generated during the decoction process can affect the in vivo behavior of the main components of the SR-CR decoction.It can reduce the absorption of baicalin in the body,decrease the extent of rapid drug release,and to a certain extent,prevent adverse reactions or side effects.

关 键 词：黄芩-黄连 共沉淀 成分组成 形貌分析 药代动力学 

分 类 号：R285.5[医药卫生—中药学]