Department of Pharmacy, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
Chirality. 2011 Sep;23(8):581-4. doi: 10.1002/chir.20971. Epub 2011 Jul 11.
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.
左旋曲司氯铵是一种新型的毒蕈碱受体激动剂，目前正在中国进行临床前开发，作为一种单一对映体药物，用于治疗原发性青光眼。本文建立了测定左旋曲司氯铵及其对映异构体杂质的反相手性 HPLC 方法。采用 Chiralpak AD-H 正相模式和 Chiralpak AS-RH 反相模式，实现了左旋曲司氯铵与其对映异构体（去曲司氯铵）的对映体分离。采用 Chiralpak AS-RH 柱和 K2HPO4-KH2PO4（pH7.0；0.02M）-乙腈（69:31，v/v）作为流动相，流速为 0.5ml/min 的条件进行了充分的验证，结果表明该方法具有良好的专属性、线性、准确性和精密度。该方法适用于同时定量测定左旋曲司氯铵和对映异构体杂质去曲司氯铵。
