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

Chirality. 2011 Sep;23(8):581-4. doi: 10.1002/chir.20971. Epub 2011 Jul 11.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Validation Study

MeSH terms

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

Substances

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