Development and validation of a reversed-phase HPLC method for determination of lesatropane and enantiomeric impurity.

Abstract

Lesatropane is a novel muscarinic receptor agonist and is currently being under preclinical development in China as a single enantiomer drug for the treatment of primary glaucoma. A reversed-phase chiral HPLC method for determination of lesatropane and enantiomeric impurity was developed. Enantiomeric separation of lesatropane from its enantiomer (desatropane) was achieved in normal-phase mode with Chiralpak AD-H and in reversed-phase mode with Chiralpak AS-RH. The conditions using a Chiralpak AS-RH column and mobile phase of K(2) HPO(4) -KH(2) PO(4) (pH 7.0; 0.02 M)-acetonitrile (69:31, v/v) at a flow rate of 0.5 ml/min have been fully validated with satisfactory specificity, linearity, accuracy, and precision. The method was found to be suitable for the simultaneous quantitation of lesatropane and enantiomeric impurity desatropane.

• Authors: Li-Min Yang, Yi-Fan Xie, Zhou-Hui Gu, Ai-Ling Wang, Hong-Zhuan Chen, Yang Lu
• Journal: Chirality (Chirality) Vol. 23 Issue 8 Pg. 581-4 (Sep 2011) ISSN: 1520-636X [Electronic] United States
• PMID: 21748809 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Validation Study)
• Copyright: Copyright © 2011 Wiley-Liss, Inc.

Chemical References

• Carbamates
• Muscarinic Agonists
• Phenylcarbamates
• Tropanes
• chiralpak AS
• satropane
• Chiralpak AD
• Amylose

Topics

• Amylose (analogs & derivatives, chemistry)
• Carbamates (chemistry)
• Chromatography, High Pressure Liquid (methods, standards)
• Drug Contamination
• Muscarinic Agonists (analysis, chemistry)
• Phenylcarbamates (chemistry)
• Reproducibility of Results
• Sensitivity and Specificity
• Stereoisomerism
• Tropanes (analysis, chemistry)