Polymorphic Crystallization Design to Prevent the Degradation of the β-Lactam Structure of a Carbapenem

The cooling crystallization of carbapenem CS-023 was performed at 25 °C in an aqueous solution. Tetrahydrate crystals (form H) were obtained. Hydrate are promising drugs, but there has been problems manufacturing such crystals. During crystallization, a dissolution process high temperature 70 utilized. main problem that the degradation rate high, as expressed half-life period 2.97 h. Poor solvent using ethanol observed °C. Thus, different polymorph (Form A) Form A comprised CS-023, 5/2 ethanol, and 1/2 H2O. A, containing is not suitable drug. then transformed to another hydrate or tetrahydrate H. Another polymorph, B, obtained through solid phase transformation further H, humidity over 80% RH. This process, which proceeded low °C, helped prevent thereby avoiding wastage. Furthermore, solid-phase transition could be controlled with vapor composition.