Influence of preparation methods on amorphous cinacalcet hydrochloride

In the present study, amorphous cinacalcet hydrochloride was prepared by three different approaches including rotary evaporation, quench-cooling and lyophilization. Physicochemical properties of prepared amorphous cinacalcet hydrochloride such as thermal behavior, dissolution and stability were investigated. Results showed that there was no difference in dissolution and chemical stability for amorphous cinacalcet hydrochloride prepared by these three different methods; however, these amorphous materials exhibited significant difference in thermodynamic behavior and physical stability: (1)They had similar T_g but with significant difference in T_c(135. 2, 129. 6 and 153. 9 °C for the amorphous products prepared by rotary evaporation, lyophilization and quench-cooling, respectively); (2)These amorphous products were easy to recrystallize under an environment with high temperature and humidity, especially that prepared by quench-cooling. This study provides an experimental basis for screening preparation methods of amorphous materials.