title: Pharmacokinetics of catechols in human subjects intravenously receiving XueBiJing injection, an emerging antiseptic herbal medicine.
abstract: XueBiJing injection, prepared from a five-herb combination, is extensively used as add-on therapy in routine sepsis care in China. Catechols, derived from the component herb Salvia miltiorrhiza roots (Danshen), are probably important because of their reported antiseptic properties. This study was designed to characterize pharmacokinetics of major circulating Danshen catechols in human subjects intravenously receiving the injection at the label doses. A total of 17 Danshen catechols were detected in XueBiJing injection (content level, 0.1-139.3 μmol/L). After dosing, tanshinol and salvianolic acid B exhibited relatively high levels of systemic exposure with mean elimination half-lives of 0.38 and 0.29 h, respectively. The total plasma clearance and apparent volume of distribution at steady state of tanshinol were 1.07 L/h/kg and 0.40 L/kg, respectively, whereas those of salvianolic acid B were 0.43 L/h/kg and 0.13 L/kg, respectively. Protocatechuic acid and five other catechols were also detected in plasma but at low exposure levels. Although protocatechuic aldehyde had the highest content level in the injection, like the remaining eight catechols, it was undetected in plasma. Protocatechuic aldehyde was extensively converted into protocatechuic acid and other metabolites. The information gained here facilitates understanding the roles of Danshen catechols in therapeutic actions of XueBiJing injection.
authors.affiliation: Graduate School, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Laboratory for DMPK Research of Herbal Medicines, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Xiuxue
authors.initials: X
authors.lastname: Li
authors.affiliation: Laboratory for DMPK Research of Herbal Medicines, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
authors.forename: Chen
authors.initials: C
authors.lastname: Cheng
authors.affiliation: Laboratory for DMPK Research of Herbal Medicines, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Fengqing
authors.initials: F
authors.lastname: Wang
authors.affiliation: Second Affiliated Hospital, Tianjin University of Traditional Chinese Medicine, Tianjin 300150, China.
authors.forename: Yühong
authors.initials: Y
authors.lastname: Huang
authors.affiliation: Laboratory for DMPK Research of Herbal Medicines, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Weiwei
authors.initials: W
authors.lastname: Jia
authors.affiliation: Laboratory for DMPK Research of Herbal Medicines, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Olajide E
authors.initials: OE
authors.lastname: Olaleye
authors.affiliation: Laboratory for DMPK Research of Herbal Medicines, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Meijuan
authors.initials: M
authors.lastname: Li
authors.affiliation: Second Affiliated Hospital, Tianjin University of Traditional Chinese Medicine, Tianjin 300150, China.
authors.forename: Yanfen
authors.initials: Y
authors.lastname: Li
authors.affiliation: Graduate School, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Laboratory for DMPK Research of Herbal Medicines, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China. Electronic address: chli@simm.ac.cn.
authors.forename: Chuan
authors.initials: C
authors.lastname: Li
mesh_terms: D061605:Administration, Intravenous; D000328:Adult; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage*; D002396:Catechols / Q000493:pharmacokinetics*; D002681:China; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage*; D005260:Female; D029001:Herbal Medicine / Q000379:methods; D006801:Humans; D062385:Hydroxybenzoates / Q000008:administration & dosage; D008297:Male; D008517:Phytotherapy / Q000379:methods; D010936:Plant Extracts / Q000008:administration & dosage; D027561:Salvia miltiorrhiza / Q000737:chemistry; D055815:Young Adult
chemical_list: D000891:Anti-Infective Agents, Local; D002396:Catechols; D004365:Drugs, Chinese Herbal; D062385:Hydroxybenzoates; D010936:Plant Extracts; C549376:Xuebijing; C028972:dan-shen root extract; C009091:protocatechuic acid
keywords: Catechol; Danshen; Pharmacokinetics; Salvia miltiorrhiza roots; Sepsis; XueBiJing injection