Department of Pharmaceutical Analysis and Analytical Chemistry, College of Pharmacy, Harbin Medical University, China.
Key Laboratory of Chinese Materia Medica (Ministry of Education), Heilongjiang University of Chinese Medicine, China.
J Ethnopharmacol. 2019 Jul 15;239:111896. doi: 10.1016/j.jep.2019.111896. Epub 2019 Apr 24.
Coptidis rhizoma (CR) is the dried rhizome of the ranunculaceous plant CR. For decades in China, this plant has been used to treat hypertension, hyperlipidemia, and chronic diarrhea and has been officially included in the Chinese Pharmacopoeia. The present paper presents a review of the pharmacokinetics of CR.
The pharmacokinetic studies and differences of 10 alkaloids among Coptis deltoidea C. Y. cheng et Hsiao, Coptis chinensis Franch and Coptis teeta Wall. Are seldom reported. This study is the first to determine corydaline, dehydrocorydaline, tetrahydropalmatine, palmatine, magnoflorine, jatrorrhizine, berberine, worenine, berberrubine, and coptisine, which adopted an ultrahigh-performance liquid chromatography-electrospray ionization-tandem mass spectrometry, simultaneously.
Chromatographic separation was performed within 8 min by using an Agilent SB-C column (150 mm × 2.1 mm, 1.8 μm) with gradient mobile phase consisting of 0.3% acetic acid water (v/v) and acetonitrile at a flow rate of 0.3 mL/min. Multiple reaction monitoring mode was used to detect the tandem mass spectrum in the positive ionization mode by electrospray ionization source.
The method was fully validated to be linear over a wide concentration (r > 0.9916), and the linear concentration range was 0.195-2260 ng/mL. Intra- and interday precisions were below 14.19% and 18.56% for the 10 analytes, respectively. The accuracy ranged from -9.30% to 6.31%. The extraction recovery of the 10 alkaloids and internal standard ranged from 79.76% to 95.37%. Pharmacokinetic comparative study showed that the C and AUC values of dehydrocorydaline, tetrahydropalmatine, palmatine, magnoflorine, jatrorrhizine, berberine, worenine, berberrubine, and coptisine increased significantly (p < 0.05), which was different for beagles after oral administration. The results can help determine the mechanism of action and guide clinical application of these three extracts.
This validated method was successfully applied for the pharmacokinetics study of beagle plasma after oral administration of three CR extract types.
黄连（CR）是毛茛科植物 CR 的干燥根茎。在中国，几十年来，这种植物一直被用于治疗高血压、高血脂和慢性腹泻，并已被正式列入《中国药典》。本文对 CR 的药代动力学进行了综述。
黄连属植物 Coptis deltoidea C. Y. cheng et Hsiao、Coptis chinensis Franch 和 Coptis teeta Wall 的 10 种生物碱的药代动力学研究和差异很少有报道。本研究首次采用超高效液相色谱-电喷雾串联质谱法同时测定了延胡索乙素、脱氢延胡索碱、四氢巴马汀、黄连碱、小檗碱、吴茱萸碱、盐酸巴马汀、黄连碱、吴茱萸次碱、小檗碱。
采用 Agilent SB-C 柱（150mm×2.1mm，1.8μm），以 0.3%（v/v）乙酸水和乙腈为流动相，梯度洗脱，流速为 0.3mL/min，在 8min 内完成色谱分离。采用电喷雾电离源正离子模式下的多反应监测模式进行串联质谱检测。
该方法在较宽的浓度范围内（r＞0.9916）具有良好的线性关系，线性浓度范围为 0.195-2260ng/mL。10 种分析物的日内和日间精密度均低于 14.19%和 18.56%。准确度在-9.30%至 6.31%之间。10 种生物碱和内标物的提取回收率在 79.76%至 95.37%之间。药代动力学比较研究表明，口服后犬体内脱氢延胡索碱、四氢巴马汀、黄连碱、小檗碱、吴茱萸碱、盐酸巴马汀、黄连碱、吴茱萸次碱、小檗碱和小檗碱的 C 和 AUC 值显著增加（p＜0.05）。这些结果可以帮助确定这三种提取物的作用机制，并指导临床应用。
本研究建立的方法可用于犬口服三种 CR 提取物后血浆的药代动力学研究。
