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Simultaneous determination of forsythin and its major metabolites in human plasma via liquid chromatography-tandem mass spectrometry.
Pan, Lu-Lu; Chen, Tao; Hui, Min; Wang, Shuo; Fu, Li; Li, Cui-Yun; Zhang, Hong; Ding, Yan-Hua; Yang, Yong; Zhong, Da-Fang.
Afiliación
  • Pan LL; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; University of Chinese Academy of Sciences, Beijing, 100049, China.
  • Chen T; Suzhou Haike Medical Technology Co., Ltd., Suzhou, 215123, China.
  • Hui M; Dalian Fusheng Pharmaceutical Co., Ltd., Dalian, 116000, China.
  • Wang S; Dalian Fusheng Pharmaceutical Co., Ltd., Dalian, 116000, China.
  • Fu L; Dalian Fusheng Pharmaceutical Co., Ltd., Dalian, 116000, China.
  • Li CY; The First Hospital of Jilin University, Changchun, 130021, China.
  • Zhang H; The First Hospital of Jilin University, Changchun, 130021, China.
  • Ding YH; The First Hospital of Jilin University, Changchun, 130021, China.
  • Yang Y; Suzhou Haike Medical Technology Co., Ltd., Suzhou, 215123, China. Electronic address: yong.yang@hq-biosci.com.
  • Zhong DF; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; University of Chinese Academy of Sciences, Beijing, 100049, China. Electronic address: dfzhong@simm.ac.cn.
J Pharm Biomed Anal ; 198: 113992, 2021 May 10.
Article en En | MEDLINE | ID: mdl-33676168
Forsythiae suspensa is widely used in China as a traditional Chinese medicine. Forsythin is extracted from Forsythiae Fructus and has undergone phase II clinical trials as an antipyretic drug in China. The main metabolites of forsythin in human plasma are aglycone sulfate (KD-2-SO3H) and aglycone glucuronide (KD-2-Glc). In the present study, a sensitive and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and fully validated for the simultaneous analysis of forsythin, KD-2-Glc, and KD-2-SO3H, in human plasma. After precipitating proteins with methanol, these three analytes were separated on a Gemini-C18 column along with teniposide as an internal standard. Mass spectrometry detection, under multiple reaction monitoring, was then carried out in negative mode using the Triple Quad™ 6500+ LC-MS/MS system coupled with an electrospray ionization (ESI) ion source. The transitions of m/z 371.1→356.1 for forsythin, m/z 547.2→356.0 for KD-2-Glc and m/z 451.2→356.2 for KD-2-SO3H were chosen to effectively maintain the balance between selectivity and sensitivity. The developed method was linear over the following concentrations in human plasma samples: 1.00-1000 ng/mL for forsythin, 2.50-2500 ng/mL for KD-2-Glc, and 5.00-5000 ng/mL for KD-2-SO3H. Assays were validated and satisfied the acceptance criteria recommended by the CFDA guidance. Furthermore, this LC-MS/MS method was successfully implemented in a Phase I, first-in-human, dose-escalation pharmacokinetic study among Chinese healthy participants after single oral administration of forsythin tablets.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Preparaciones Farmacéuticas / Espectrometría de Masas en Tándem Tipo de estudio: Guideline Límite: Humans País/Región como asunto: Asia Idioma: En Revista: J Pharm Biomed Anal Año: 2021 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Preparaciones Farmacéuticas / Espectrometría de Masas en Tándem Tipo de estudio: Guideline Límite: Humans País/Región como asunto: Asia Idioma: En Revista: J Pharm Biomed Anal Año: 2021 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido