title: 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: Department of Pharmacy, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
authors: Li-Min
authors: LM
authors: Yang
authors: Yi-Fan
authors: YF
authors: Xie
authors: Zhou-Hui
authors: ZH
authors: Gu
authors: Ai-Ling
authors: AL
authors: Wang
authors: Hong-Zhuan
authors: HZ
authors: Chen
authors: Yang
authors: Y
authors: Lu
mesh_terms: D000688:Amylose / Q000031:analogs & derivatives* / Q000737:chemistry; D002219:Carbamates / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid / Q000379:methods / Q000592:standards*; D004340:Drug Contamination; D018721:Muscarinic Agonists / Q000032:analysis / Q000737:chemistry; D048448:Phenylcarbamates / Q000737:chemistry*; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013237:Stereoisomerism; D014326:Tropanes / Q000032:analysis / Q000737:chemistry
chemical_list: D002219:Carbamates; D018721:Muscarinic Agonists; D048448:Phenylcarbamates; D014326:Tropanes; C445088:chiralpak AS; C535253:satropane; C080033:Chiralpak AD; D000688:Amylose