부산대학교 도서관

At present, the vast majority of new chemical entities emerging have acceptable permeability but a very limited absorption due to its low solubility (according to BCS Class 2). For this reason, research and development of new chemical entities has advanced the study and selection of formulations based on solid solutions and solid suspensions. These formulations are obtained when the active ingredient is in the form of a solution or a suspension embedded molecularly into an excipient or mixture of excipients. This can be extremely advantageous to improve the solubility of the active ingredient. This thesis is the result of collaboration between various disciplines, to achieve viable and improved formulations containing class 2 molecules (as BCS), and focuses on formulation aspects of this study, the methodology used to screen and characterize viable formulations, the scale-up, manufacturing of samples for “in vivo" studies and finally moving these concepts to the development of dosage forms. In the experimental studies, rapid screening of binary and ternary formulations for the study of solid solutions and suspensions using innovative and efficient techniques were carried out. It has been proven that the rapid screening techniques at laboratory scale using the melt press and "solvent casting" are viable and representative, qualitatively, of the results obtained by extrusion techniques. We also demonstrated the feasibility of industrial formulations obtained in the screening, and have confirmed the relation of the results, qualitatively; to the "in vivo" studies. Subsequently the results of the screening were the basis for the development of dosage forms that allowed oral administration of low solubility drugs that were proven stable.