Formulation Studies and Application of Their Experimental Techniques to Drug Discoveries

Abstract

In my first experience as a researcher, I isolated and performed structural predictions of the novel compounds, cis- and trans-palythenic acids, from Noctiluca milialis. I then worked for a pharmaceutical company in a research laboratory of pharmaceutics. I examined an inclusion complex of cinnarizine with β-cyclodextrin, and found that the inclusion complex did not improve the oral bioavailability of cinnarizine. However, the bioavailability of the inclusion complex after its oral administration was improved by a competing agent. This was the first study to show the potential of a competing agent to improve bioavailability. I subsequently joined a laboratory performing drug discovery research and used experimental techniques from pre-formulation studies. A screening system of solubility for drug design and discovery was constructed to increase the solubilities of compounds synthesized in the laboratory. This screening system contributed to the discovery of a phosphodiesterase type 5 inhibitor with sufficient solubility. As a visiting lecturer at a university, I prepared amoxicillin intragastric buoyant sustained-release tablets for the eradication of Helicobacter pylori and applied cinnarizine as a competing agent. I established a laboratory of pharmaceutics at a university in Tochigi. To develop an enema with fluticasone propionate for ulcerative colitis, I investigated its physicochemical properties and methods to improve its solubility. After moving to another university in Kagawa, I developed a method to reduce the amount of drugs remaining on the surfaces of a pestle and mortar following the grinding of tablets, and new cleaning agents for an automatic dividing packaging machine were discovered.