Factors Affecting the Dissolution Rate of Sulpiride from Tablets Coated with Polyvinylacetal Diethylaminoacetate, a Gastric-Fluid-Soluble Polymer. II. Effect of Mechanical Destructive Force and Film Coating Strength in the Gastrointestinal Tract
スポンサーリンク
概要
- 論文の詳細を見る
The bioavabilaility of sulpiride (SP) from a tablet coated with AEA^[○!R] (polyvinylacetal diethylaminoacetate), a gastric-fluid-soluble polymer, is very poor in low gastric acidity subjects in the fasting state but improves after food intake. To analyze factors affecting SP bioavailability from AEA^[○!R] film-coated tablets (AEA^[○!R] tablets), we prepared AEA^[○!R] cast film and AEA^[○!R] tablets and determined the effects of mechanical destructive force and film coating strength in the gastrointestinal (GI) tract on SP dissolution from the tablets. With the paddle method, rapid SP dissolution occurred at pH 4.0 or below but not at pH 5.0 or above. Using the disintegration test method, dissolution at pH 5.0-5.8 markedly increased as the film coating broke due to an increase in the mechanical destructive force and a change in film coating strength. Microscopic observation of AEA^[○!R] film coating at pH 5.0 supported the marked decrease in the cast film strength observed in pH 5.0 medium with an increase in film swelling. Thus, one important factor affecting AEA^[○!R] film coating strength is its swelling rate. After food intake, SP bioavailability from AEA^[○!R] tablet improves, probably due to increased mechanical destructive force with GI motility and decreased film coating strength in GI fluids with increased film swelling in the pH environment after the meal (pH 5.85). This increased SP dissolution rate from AEA^[○!R] tablet leads to enhanced absorption. We concluded that the increase in mechanical destructive force acting on the tablet after food intake is one of the powerful factors leading to improved drug bioavailability.
- 公益社団法人日本薬学会の論文
- 1995-12-15
著者
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水野 亘恭
Faculty of Pharmaceutical Sciences, Osaka University
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水野 亘恭
武庫川女子大学薬学部
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Tanaka T
Osaka Univ. Osaka Jpn
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新熊 傳治
兵庫医科大
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山中 要
兵庫医科大
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田中 恒雄
Department Of Pharmacy Hyogo College Of Medicine
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Hamaguchi T
Department Of Pharmacy Hyogo College Of Medicine
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濱口 常男
Department of Pharmacy, Hyogo College of Medicine
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新熊 傳治
Department of Pharmacy, Hyogo College of Medicine
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山中 要
Department of Pharmacy, Hyogo College of Medicine
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三宅 正敏
Technological Development Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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田村 繁樹
Technological Development Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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三宅 正敏
Technological Development Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Tamura Sadaaki
Faculty Of Integrated Art And Sciences Hiroshima University
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Tamura S
Technological Development Laboratories Fujisawa Pharmaceutical Co. Ltd.
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田村 繁樹
Technological Development Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Miyake M
Technological Development Laboratories Fujisawa Pharmaceutical Co. Ltd.
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水野 亘恭
武庫川女子大・薬
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水野 亘恭
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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