糖転移化合物の新規医薬品添加剤への応用を目指した製剤設計及び処方検討に関する研究

開発段階での医薬品候補化合物の水溶性が極端に低下する中、候補となる難水溶性薬物の溶解性の改善かつ吸収性の増大が、医薬品開発の継続や製品化において鍵となる。しかし、既存の製剤技術や処方設計では十分な結果が得られない場合も多く、新たな製剤技術や処方設計による溶解性の改善が強く望まれている。我々は、近年の酵素合成技術の革新によって開発され、機能性食品添加剤として使用され始めた糖転移化合物に着目した。糖転移化合物は、既存の化合物に糖を転移することで、水溶性を増大させた化合物の総称であり、食品分野においては広く使用され、安全性が確保されている。本研究の目的は、糖転移化合物α-glucosyl hesperidin (Hsp-G) 及び α-glucosyl Stevia (Stevia-G)を用いて、難水溶性化合物の溶解性及び吸収性改善効果を目指した新規の処方検討を行い、改善効果の評価、メカニズムの解明、新規処方設計の提案により、糖転移化合物の医薬品添加剤や機能性食品添加剤としての可能性を見出すことにある。While the water solubility of new drug candidates in the development phase is often extremely poor, the improvement ofthe dissolution and absorption of poorly water soluble drug candidates is a key factor in the continuation of drug development andmaking new drugs. Since the existing technology and formulation design cannot produce acceptable results for poorly water solubledrugs in many cases, improvement in dissolution with new techniques and formulation designs is essential. We focused ontransglycosylated compounds which were recently developed by innovation of enzyme synthesis technology and have begun to beused as functional food additives. A transglycosylated compound is the general term for compounds which increase water solubilityby the addition of sugar to an existing compound making it safe and widely used in the food industry. The purpose of this study wasto evaluate the potential of Hsp-G and Stevia-G as pharmaceutical excipients and functional food additives to enhance the dissolutionand absorption of poorly water soluble drugs using a new formulation, as well as an evaluation of the improvement and mechanismof dissolution enhancement effect

BioHackathon series in 2011 and 2012: penetration of ontology and linked data in life science domains

The application of semantic technologies to the integration of biological data and the interoperability of bioinformatics analysis and visualization tools has been the common theme of a series of annual BioHackathons hosted in Japan for the past five years. Here we provide a review of the activities and outcomes from the BioHackathons held in 2011 in Kyoto and 2012 in Toyama. In order to efficiently implement semantic technologies in the life sciences, participants formed various sub-groups and worked on the following topics: Resource Description Framework (RDF) models for specific domains, text mining of the literature, ontology development, essential metadata for biological databases, platforms to enable efficient Semantic Web technology development and interoperability, and the development of applications for Semantic Web data. In this review, we briefly introduce the themes covered by these sub-groups. The observations made, conclusions drawn, and software development projects that emerged from these activities are discussed

Water-assisted synthesis of mesoporous calcium carbonate with a controlled specific surface area and its potential to ferulic acid release

A carbonation process to control the specific surface area of mesoporous calcium carbonate and the dissolution profile of ferulic acid on mesoporous carbonate particles are presented. The effects of water content on the physicochemical properties, specific surface area, pore size, crystallinity, and morphology are evaluated. Mesoporous calcium carbonate particles are synthesised with well-controlled specific surface areas of 38.8 to 234 m2 g-1. Each of the submicron-size secondary particles consists of a primary particle of nano-size. During secondary particle formation, primary particle growth is curbed in the case with less water content. By contrast, growth is promoted via dissolution and recrystallisation in the presence of water. The release rates of ferulic acid are gradually enhanced with increasing specific surface area of the mesoporous calcium carbonate, that reflects crystallinity of ferulic acid