Analysis of dissolution kinetics and first-pass elimination of orally administered drugs and its application to prediction of absorption behavior after oral administration
| Project/Area Number |
21590158
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Medical pharmacy
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| Research Institution | Okayama University |
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Principal Investigator |
KIMURA Toshikiro 岡山大学, 大学院・医歯薬学総合研究科, 特命教授 (10025710)
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| Co-Investigator(Kenkyū-buntansha) |
HIGAKI Kazutaka 岡山大学, 大学院・医歯薬学総合研究科, 教授 (60284080)
OGAWARA Kenichi 岡山大学, 大学院・医歯薬学総合研究科, 准教授 (30291470)
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| Project Period (FY) |
2009 – 2011
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| Project Status |
Completed (Fiscal Year 2011)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2011: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2010: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2009: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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| Keywords | 消化管吸収 / 初回通過効果 / 難溶解性薬物 / P-glycoprotein / Cytochrome P450 3A / 自己乳化型マイクロエマルション製剤(SMEDDS) / 経口吸収 / 自己乳化型マイクロエマルション製剤 / 胆汁 / 膵リパーゼ / 放出 / グリセオフルビン / ムチン層 / griseofulvin / 自己乳化型マイクロエマルション / 油脂成分 / 界面活性剤 / 補助界面活性剤 / SMEDDS製剤 / 経口投与 / 経口窒収 / quinidine / 発現タンパク量 / 吸収クリアランス / 小腸抽出率 |
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| Research Abstract |
The large variability in absorption behavior of griseofulvin would be attributed to the large variability in in vivo dissolution behavior after oral administration. We successfully described the individual absorption behavior of griseofulvin based on the data of gastrointestinal transit and the estimated in vivo dissolution behavior. SMEDDS significantly increased the bioavailability and reduced the interindividual difference in absorption behavior of griseofulvin. Both CYP3A and P-gp significantly contributed to the intestinal extraction of digoxin, but neither would affect the absorption clearance.
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Report
(4 results)
Research Products
(36 results)
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[Journal Article]2010
Author(s)
檜垣和孝
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Journal Title
難水溶性薬物の物性評価と製剤設計の新展開(シーエムシー出版)
Pages: 151-160
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