| Co-Investigator(Kenkyū-buntansha) |
NIWA Toshiyuki Gifu Pharmaceutical University, Assistant Professor, 薬学部, 助手 (30198543)
HINO Tomoaki Gifu Pharmaceutical University, Assistant Professor, 薬学部, 助手 (90208778)
TAKEUCHI Hirofumi Gifu Pharmaceutical University, Associate Professor, 薬学部, 助教授 (50171616)
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| Research Abstract |
A novel controlled drug release floating system with micro-hollow spheres of polymer, termed microballoons, was developed for pharmaceutical, chemical and pesticide by the "emulsion -solvent-diffusion" method. In this system, the drug, eg. ibuprofen or tranilast, was entrapped in the outer polymer (acrylic resin) shell of the device. The device was characterized with small particle size, 100-500) Am, and low specific gravity, -0.8. Those properties resulted in forming a multiple unit floating system, which released slowly the drug in acidic medium. In alkaline solution, the drug release rate increased due to the increase in the dissolution property of polymer. The crystalline form of the drug and the drug release profiles from microballoon were controlled by changing the ratio of polymer to drug in the device. An in vivo X-ray radiographical study with barium sulfate contained in the shell of device proved that the microballoons orally adwinistered to humans were dispersed in the upper part of stomach. This finding suggested a prolonged residence time of the device in the stomach.
The emulsion-solvent-diffusion method can apply further to design the particulate properties of drug crystals for direct tabletting by transforming them into the spherically agglomerated crystals.
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