Development of Novel Functional Formulations Based on Pharmaceutical Technologies

Abstract

After 32 years as a researcher in a pharmaceutical company, the author has served as a professor in the Development of Pharmaceutical Engineering and Drug Delivery Science at University of Shizuoka for the past 11 years. The research I was involved in can be categorized into four main items. First, the crystal transformation of clarithromycin (CAM) was focused on to develop the CAM high-loaded sustained release and gastro-floating formulations. Furthermore, the stabilization mechanism of CAM in the gastro-intestinal tract was clarified to elucidate gel formation under conditions of low pH. Second, the development of novel dosage regimens and optimization of formulation design were carried out using powder technology. In this category, a wax matrix formulation for taste masking, highly drug-loaded fine globular granules using a multi-functional rotor processor, and orally disintegrating tablets treated with microwave or high-pressure carbon dioxide were our targets. The third category was the manufacture of dispersion systems including lipid nanoparticles and cubosomes in order to improve the bioavailability and stability of poorly water-soluble drugs. The fourth category was the development and application of novel physical testing methods including investigation of the internal structure of fine granules using microtomography with synchrotron X-ray radiation, dissolution of spherical granules under non-sink conditions, mathematical models to analyze the dissolution behavior of metastable crystals or amorphous drugs and prediction of the available surface area of tablets during dissolution process.