7-3,5-DIHYDROXY-2-(3-HYDROXY-5-PHENYL-PENT-1-ENYL)-CYCLOPENTYL-N-ETHYL-HEPT-5-ENAMIDE (BIMATOPROST) IN CRYSTALLINE FORM II, METHOD FOR PREPARATION, AND METHOD FOR USE THEREOF

摘要

PROBLEM TO BE SOLVED: To provide a new crystalline form of 7-[3,5-dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-N-ethyl-hept-5-enamide (bimatoprost).SOLUTION: The present invention provides a new crystalline form of 7-[3,5-dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-N-ethyl-hept-5-enamide (bimatoprost), designated as crystalline form II. The new crystalline form is the most stable form known to date of bimatoprosts. Moreover, it has been found that bimatoprost crystalline form II is readily prepared from crystalline form I or can be directly prepared from amorphous bimatoprost.SELECTED DRAWING: Figure 1