PMID- 32567749
OWN - NLM
STAT- MEDLINE
DCOM- 20210520
LR  - 20210520
IS  - 1520-636X (Electronic)
IS  - 0899-0042 (Linking)
VI  - 32
IP  - 8
DP  - 2020 Aug
TI  - Enantioselective LC-MS/MS method for the determination of cloperastine 
      enantiomers in rat plasma and its pharmacokinetic application.
PG  - 1129-1138
LID - 10.1002/chir.23257 [doi]
AB  - Cloperastine is a central antitussive used to reduce the frequency and intensity 
      of coughing on a short-term basis. In this study, a reliable chiral LC-MS/MS 
      technology has been developed for the quantification of cloperastine enantiomers 
      in the rat plasma. Carbinoxamine was selected as the internal standard. The 
      enantioseparation of cloperastine was performed on a Chiralpak IA column with a 
      mobile phase composed of acetonitrile-water-ammonium hydroxide (80:20:0.1, v/v/v) 
      at a flow rate of 0.6 mL/min. Cloperastine enantiomers were detected by mass 
      spectrometry in multiple reaction monitoring mode with a positive electrospray 
      ionization source. The method was validated over the linear concentration range 
      of 0.05 to 10.0 ng/mL (5.0 x 10(-4) ng to 0.10 ng) for both enantiomers. The 
      lower limit of quantification (LLOQ) for each analyte was determined as 0.05 
      ng/mL. The relative standard deviations (RSDs) of intraday and interday precision 
      was less than 13.9%, and the relative error (RE) of accuracy ranged from -5.4% to 
      6.1%, which were within the acceptance criteria. Finally, an application to the 
      stereoselective pharmacokinetics of cloperastine in rats was successfully 
      realized in our assay. The developed method on a commercially available Chiralpak 
      IA column under isocratic mobile phase is advantageous to analyze cloperastine 
      enantiomers in plasma samples collected for enantioselective metabolism or drug 
      interaction studies.
CI  - (c) 2020 Wiley Periodicals LLC.
FAU - Lun, Jia
AU  - Lun J
AD  - Department School of Pharmacy, Institution Shenyang Pharmaceutical University, 
      Shenyang, China.
FAU - Zhao, Pengfei
AU  - Zhao P
AD  - Department School of Pharmacy, Institution Shenyang Pharmaceutical University, 
      Shenyang, China.
FAU - Jiang, Zhen
AU  - Jiang Z
AD  - Department School of Pharmacy, Institution Shenyang Pharmaceutical University, 
      Shenyang, China.
FAU - Song, Yongbo
AU  - Song Y
AD  - Department School of Life Science and Biopharmaceutics, Institution Shenyang 
      Pharmaceutical University, Shenyang, China.
FAU - Guo, Xingjie
AU  - Guo X
AUID- ORCID: 0000-0003-4722-0193
AD  - Department School of Pharmacy, Institution Shenyang Pharmaceutical University, 
      Shenyang, China.
LA  - eng
PT  - Journal Article
DEP - 20200622
PL  - United States
TA  - Chirality
JT  - Chirality
JID - 8914261
RN  - 0 (Piperidines)
RN  - 69M5L7BXEK (cloperastine)
SB  - IM
MH  - Animals
MH  - Chromatography, Liquid/*methods
MH  - Limit of Detection
MH  - Piperidines/*blood/chemistry/*pharmacokinetics
MH  - Rats
MH  - Stereoisomerism
MH  - Tandem Mass Spectrometry/*methods
MH  - Tissue Distribution
OTO - NOTNLM
OT  - LC-MS/MS
OT  - antitussive drug
OT  - cloperastine
OT  - enantioseparation
OT  - pharmacokinetics
EDAT- 2020/06/23 06:00
MHDA- 2021/05/21 06:00
CRDT- 2020/06/23 06:00
PHST- 2020/03/02 00:00 [received]
PHST- 2020/04/28 00:00 [revised]
PHST- 2020/06/02 00:00 [accepted]
PHST- 2020/06/23 06:00 [pubmed]
PHST- 2021/05/21 06:00 [medline]
PHST- 2020/06/23 06:00 [entrez]
AID - 10.1002/chir.23257 [doi]
PST - ppublish
SO  - Chirality. 2020 Aug;32(8):1129-1138. doi: 10.1002/chir.23257. Epub 2020 Jun 22.