Leveraging elevated temperature and particle size reduction to extract API from various tablet formulations.

Several sample preparation techniques were evaluated for extracting active pharmaceutical ingredient (API) from immediate release (IR) and controlled release (CR) tablet formulations. These techniques utilized either elevated temperature [e.g.

Comparison of extraction techniques for spray dried dispersion tablet formulations.

Non-traditional sample preparation/extraction techniques that utilized the Caliper Life Sciences Tablet Processing Workstation II (TPW II), Microwave Assisted Extraction (MAE), and Accelerated Solvent Extraction (ASE) were evaluated for the extraction of Compound A from a 50 mgA, 15% Spray Dried Dispersion (SDD) immediate released (IR) tablet formulation. The TPW II consistently provided complete recoveries with very short preparation/extraction times (approximately 30 min). MAE also provided complete recovery of the API from the tablet formulation, but required approximately twice the extraction time, while ASE provided the lowest recovery of the three non-traditional techniques.

N-methylation and N-formylation of a secondary amine drug (varenicline) in an osmotic tablet.

Significant degradation of the amine-based smoking cessation drug varenicline tartrate in an early development phase osmotic, controlled-release (CR) formulation yields predominantly two products: N-methylvarenicline (NMV) and N-formylvarenicline (NFV). NMV is produced by reaction of the amine moiety with both formaldehyde and formic acid in an Eschweiler-Clarke reaction, while NFV is formed by reaction of formic acid alone with varenicline. This represents the first report of these reactions occurring on storage of solid pharmaceutical formulations.