Effect of Grinding with Hydroxypropyl Cellulose on the Dissolution and Particle Size of a Poorly Water-Soluble Drug
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概要
- 論文の詳細を見る
A new benzofuroquinoline derivative, 3,9-bis(N, N-dimethylcarbamoyloxy)-5H-benzofuro[3,2-c]quinoline-6-one (KCA-098), shows poor oral absorption due to practical insolubility in water. In this study, a co-grinding technique employing a water-soluble polymer was used for improvement of the dissolution rate of KCA-098.Powder X-ray diffraction patterns and IR spectra of KCA-098 showed the conversion of the drug from a crystal state to an amorphous state by grinding with a polymer such as hydroxypropyl cellulose (HPC-SL) or polyvinylpyrrolidone (PVP K30). The particle size of KCA-098 was remarkably reduced to a submicron size by grinding with HPC-SL. The co-ground mixture with HPC-SL showed a repid dissolution rate and maintained supersaturation for more than 1 h. On the other hand, the co-ground mixture with PVP K30 showed rapid dissolution and supersaturation for a shorter period. These data suggest that the rapid dissolution rate was obtained by the conversion of the drug particles from a crystal to amorphous state by grinding with water-soluble polymers and that a reduction in particle size to the submicron level led to the maintenance of supersaturation due to good dispersion.
- 公益社団法人日本薬学会の論文
- 1999-09-15
著者
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IMAI TERUKO
Faculty of Pharmaceutical Science, Kumamoto University
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OTAGIRI MASAKI
Faculty of Pharmaceutical Science, Kumamoto University
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SAITO Noriyasu
Pharmaceutical Laboratories, Kissei Pharmaceutical Co., Ltd.,
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YAMADA Tatsuhiko
Pharmaceutical Laboratories, Kissei Pharmaceutical Co., Ltd.,
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Yamada Tatsuhiko
Pharmaceutical Laboratories Kissei Pharmaceutical Co. Ltd.
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Yamada T
Department Of Radiopharmacy Tohoku Pharmaceutical University
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Otagiri M
Graduate School Of Pharmaceutical Sciences Kumamoto University
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Saito Noriyasu
Pharmaceutical Laboratories Kissei Pharmaceutical Co. Ltd.
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Otagiri M
Kumamoto Univ. Kumamoto Jpn
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Yamada Takehisa
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Imai T
Faculty Of Pharmaceutical Sciences Kumamoto University
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Otagiri Masaki
Faculty Of Pharmaceutical Science Kumamoto University
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Sato Noriyasu
Pharmaceutical Laboratories, Kissei Pharmaceutical Co., Ltd.,
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