Preparation and Quality Evaluation of Clozapine Nanosuspensions for Pediatric Use

OBJECTIVE  To prepare clozapine nanosuspensions(CLZ-NS) for pediatric use, optimize the formulation and preparation process, and evaluate their properties.

METHODS The CLZ-NS was prepared by the nano-precipitation method, and then the formulation process was optimized by orthogonal design. The microstructure of CLZ-NS was observed by transmission electron microscopy. The particle size and polydispersity index of the nanoparticles were determined by granulometer. The in vitro release was evaluated by dissolution test.

RESULTS The optimal formulation process of CLZ-NS were as follows: CLZ-to-lecithin ratio(1∶5), the mass of Poloxamer 407 was 10 mg, organic phase-aqueous phase(1∶5). CLZ-NS exhibited spherical morphology with an average particle size of (98.78±2.37)nm and a polydispersity index of 0.155±0.027. The in vitro release study showed that the cumulative release of CLZ-NS group was 78.92% in 24 h, which was significantly higher than that of CLZ raw material group(32.97%), showing a rapid release characteristic.

CONCLUSION The determined CLZ-NS formulation is reasonable, the preparation process is simple, and the dissolution rate is fast, laying the foundation for its application in the field of pediatric medication.