TY - JOUR
T1 - Chirobiotic V Versus Chiralpak ID for the Enantioselective Chromatographic Separation of Chloroquine: Stability and Validation Study
AU - Aburachid Cardoso, Priscila
AU - Beltrao Pereira, Diego
AU - Farrag El-behairy, Mohammed
AU - GHANEM, Ashraf
AU - Pianetti, Gerson Antonio
AU - Costa Cesar, Isabela
N1 - Publisher Copyright:
© 2019 The Author(s). Published by Oxford University Press. All rights reserved.
Copyright:
Copyright 2021 Elsevier B.V., All rights reserved.
PY - 2019/5
Y1 - 2019/5
N2 - Chloroquine is a chiral antimalarial drug and demonstrates enantioselective pharmacodynamic and pharmacokinetic properties. However, this drug is administered as racemate. The knowledge of stereoselective aspects of these agents may be useful to better understand their mechanisms of action and to optimize their safety and/or clinical efficacy. In this study, an enantioselective analytical method for the quantification of chloroquine enantiomers was developed using HPLC-UV. The chromatographic conditions were: Chirobiotic V column (100 × 2.1 mm, 5 μm) at 25°C, mobile phase containing methanol:acetic acid:triethylamine (100:0.12:0.12), flow rate 1 mL/min, injection volume 10 μL and detection at 258 nm. The validation parameters evaluated were selectivity, linearity, precision, accuracy, and robustness. In addition, a stability study after forced degradation of chloroquine enantiomers was performed. The enantioseparation of chloroquine using a polysaccharide-based chiral stationary phase (Chiralpak ID) at different mobile phase composition was evaluated and the chromatographic performance of both columns was compared. Thus, a stability-indicating chiral analytical method was developed and fully validated, allowing the separation of chloroquine enantiomers and its degradation products in tablets available in Brazil.
AB - Chloroquine is a chiral antimalarial drug and demonstrates enantioselective pharmacodynamic and pharmacokinetic properties. However, this drug is administered as racemate. The knowledge of stereoselective aspects of these agents may be useful to better understand their mechanisms of action and to optimize their safety and/or clinical efficacy. In this study, an enantioselective analytical method for the quantification of chloroquine enantiomers was developed using HPLC-UV. The chromatographic conditions were: Chirobiotic V column (100 × 2.1 mm, 5 μm) at 25°C, mobile phase containing methanol:acetic acid:triethylamine (100:0.12:0.12), flow rate 1 mL/min, injection volume 10 μL and detection at 258 nm. The validation parameters evaluated were selectivity, linearity, precision, accuracy, and robustness. In addition, a stability study after forced degradation of chloroquine enantiomers was performed. The enantioseparation of chloroquine using a polysaccharide-based chiral stationary phase (Chiralpak ID) at different mobile phase composition was evaluated and the chromatographic performance of both columns was compared. Thus, a stability-indicating chiral analytical method was developed and fully validated, allowing the separation of chloroquine enantiomers and its degradation products in tablets available in Brazil.
KW - Enantioselective Chromatographic Separation
KW - Chloroquine
UR - http://www.scopus.com/inward/record.url?scp=85068495843&partnerID=8YFLogxK
UR - http://www.mendeley.com/research/chirobiotic-v-versus-chiralpak-id-enantioselective-chromatographic-separation-chloroquine-stability
U2 - 10.1093/chromsci/bmz014
DO - 10.1093/chromsci/bmz014
M3 - Article
SN - 0021-9665
VL - 57
SP - 443
EP - 450
JO - Journal of Chromatographic Science
JF - Journal of Chromatographic Science
IS - 5
ER -