title: Pharmacokinetics of isochlorgenic acid C in rats by HPLC-MS: Absolute bioavailability and dose proportionality.
abstract: BACKGROUND
  Isochlorgenic acid C (IAC), one of the bioactive compounds of Lonicera japonica, exhibited diverse pharmacological effects. However, its pharmacokinetic properties and bioavailability remained unresolved.
  
  
  OBJECTIVE
  To determine the absolute bioavailability in rats and the dose proportionality on the pharmacokinetics of single oral dose of IAC.
  
  
  METHODS
  A validated HPLC-MS method was developed for the determination of IAC in rat plasma. Plasma concentration versus time data were generated following oral and intravenous dosing. The pharmacokinetic analysis was performed using DAS 3.0 software analysis. Absolute bioavailability in rats was determined by comparing pharmacokinetic data after administration of single oral (5, 10 and 25mgkg(-1)) and intravenous (5mgkg(-1)) doses of IAC. The dose proportionality of AUC(0-∞) and Cmax were analyzed by linear regression.
  
  
  RESULTS
  Experimental data showed that absolute oral bioavailability of IAC in rats across the doses ranged between 14.4% and 16.9%. The regression analysis of AUC(0-∞) and Cmax at the three doses (5, 10 and 25mgkg(-1)) indicated that the equations were y=35.23x+117.20 (r=0.998) and y=121.03x+255.74 (r=0.995), respectively.
  
  
  CONCLUSIONS
  A new HPLC-MS method was developed to determine the bioavailability and the dose proportionality of IAC. Bioavailability of IAC in rats was poor and both Cmax and AUC(0-∞) of IAC had a positive correlation with dose. Evaluation of the pharmacokinetics of IAC will be useful in assessing concentration-effect relationships for the potential therapeutic applications of IAC.
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: hlh1130@163.com.
authors.forename: Li Hua
authors.initials: LH
authors.lastname: Huang
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: 1373625459@qq.com.
authors.forename: Xiao Hong
authors.initials: XH
authors.lastname: Xiong
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: ym12zhong@163.com.
authors.forename: Yun Ming
authors.initials: YM
authors.lastname: Zhong
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: 1147927559@qq.com.
authors.forename: Mei Feng
authors.initials: MF
authors.lastname: Cen
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: 353280336@qq.com.
authors.forename: Xuan Ge
authors.initials: XG
authors.lastname: Cheng
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: wgx306@aliyun.com.
authors.forename: Gui Xiang
authors.initials: GX
authors.lastname: Wang
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: 610253454@qq.com.
authors.forename: Lin Quan
authors.initials: LQ
authors.lastname: Zang
authors.affiliation: Department of pharmacology, School of pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. Electronic address: wsj7272@126.com.
authors.forename: Su Jun
authors.initials: SJ
authors.lastname: Wang
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002726:Chlorogenic Acid / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D008297:Male; D013058:Mass Spectrometry; D015394:Molecular Structure; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: C469310:isochlorogenic acid; D002726:Chlorogenic Acid
keywords: Bioavailability; Dose proportionality; HPLC-MS; Isochlorgenic acid C