Sustained release, polymer-encapsulated olanzapine depots

CHED 207

Noemia T. Elfes1, Marc M. Baum, m.baum@oak-crest.org1, and Thomas J. Smith2. (1) Department of Chemistry, Oak Crest Institute of Science, 2275 E. Foothill Blvd., Pasadena, CA 91107, (2) Auritec Pharmaceuticals, 2275 E. Foothill Blvd., Pasadena, CA 91107
More than a million Americans suffer from schizophrenia. Olanzapine, an atypical antipsychotic, is one of the best agents for outpatient therapy but patients often do not take their pills. This leads to frequent readmission. Depot formulations of older antipsychotics have demonstrated that the strategy of infrequent injectable dosing improves outcomes but there is no depot formulation of olanzapine available. We have previously presented our data on a novel sustained release injectable depot formulation of olanzapine (Arunraj, K.; Phu, F.; Baum, M. M.; Smith, T. Abstr. Pap. Am. Chem. Soc. 2005, 229, CHED1134). We now present improvements in the formulation leading to greater reproducibility and more linear drug release. Polymer coating of drug particles is achieved with multiple laminations of polyvinyl alcohol and polylactic acid. Animal data suggests that a monthly injection of this formulation could sustain antipsychotic drug levels. This work has important implications for the outpatient management of schizophrenia.