Liu Si-Yi, Zhang Xiu-Ping, Shang Zhan-Peng, Wang Fei, Zhang Xiao-Xin, Zhang Jia-Yu, Lu Jian-Qiu
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China.
Beijing Institution of Chinese Medicine, Beijing University of Chinese Medicine, Beijing 100029, China.
Zhongguo Zhong Yao Za Zhi. 2016 Jun;41(12):2235-2244. doi: 10.4268/cjcmm20161211.
A rapid and sensitive UHPLC-HR-MSn method was used for the identification of Kudiezi injection and its main metabolites in rat plasma. After the tail intravenous injection of Kudiezi, ACQUITY UHPLC BEH C₁₈ (2.1 mm×100 mm, 1.7 μm) was used, with 0.1% formic acid-acetonitrile solution as the mobile phase for gradient elution. Kudiezi injection and plasma were detected by ESI-LTQ-Orbitrap equipped with an ESI ion source in a negative mode. Based on the accurate mass measurements, the retention time and the mass fragmentation patterns, a total of 53 compounds were tentatively identified and characterized. Furthermore, metabolites in rat plasma after the intravenous administration of Kudiezi injection were also analyzed. A total of 38 compounds were identified, including 27 prototypes and 11 metabolites through metabolic pathways of methylation, glucuronide conjugation, sulfate conjugation and hydrolysis. As a result, UHPLC-LTQ-Orbitrap technique was applied to comprehensively expound Kudiezi injection's chemical components and constituents migrating to rat plasma, and provide scientific basis for further studies on Kudiezi injection's in vivo metabolic process and effective material base.
采用快速灵敏的超高效液相色谱-高分辨质谱联用（UHPLC-HR-MSn）方法鉴定大鼠血浆中苦碟子注射液及其主要代谢产物。尾静脉注射苦碟子后，使用ACQUITY UHPLC BEH C₁₈（2.1 mm×100 mm，1.7 μm）色谱柱，以0.1%甲酸-乙腈溶液为流动相进行梯度洗脱。采用配备电喷雾离子源（ESI）的ESI-LTQ-Orbitrap质谱仪在负离子模式下检测苦碟子注射液和血浆。基于精确质量测定、保留时间和质量碎片模式，共初步鉴定和表征了53种化合物。此外，还分析了静脉注射苦碟子注射液后大鼠血浆中的代谢产物。共鉴定出38种化合物，包括27种原型成分和11种通过甲基化、葡萄糖醛酸结合、硫酸结合和水解代谢途径产生的代谢产物。结果表明，UHPLC-LTQ-Orbitrap技术可用于全面阐述苦碟子注射液的化学成分及其向大鼠血浆中的迁移成分，为进一步研究苦碟子注射液的体内代谢过程和有效物质基础提供科学依据。
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