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消化管および肝で初回通過効果を受ける薬物のバイオアベイラビリティを経口クリアランスから予測する方法
https://dwcla.repo.nii.ac.jp/records/737
https://dwcla.repo.nii.ac.jp/records/73787255fb0-fe8d-4c36-8d22-5e1b8e390e4d
Item type | 紀要論文 / Departmental Bulletin Paper(1) | |||||
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公開日 | 2012-03-30 | |||||
タイトル | ||||||
タイトル | 消化管および肝で初回通過効果を受ける薬物のバイオアベイラビリティを経口クリアランスから予測する方法 | |||||
言語 | ||||||
言語 | jpn | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | departmental bulletin paper | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
別タイトル | ||||||
その他のタイトル | Prediction of the oral bioavailability of a drug subjected to both intestinal and hepatic first-pass effects from oral clearance data | |||||
著者 |
伊賀, 勝美
× 伊賀, 勝美× IGA, Katsumi |
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著者 所属 | ||||||
値 | 同志社女子大学薬学部医療薬学科 | |||||
著者所属(翻訳) | ||||||
値 | Doshisha Women's College of Liberal Arts, Faculty of Pharmaceutical Sciences, Department of Clinical Pharmacy | |||||
著者 外部リンク | ||||||
表示名 | 同志社女子大学研究者データベース - 伊賀勝美 | |||||
URL | http://research-db.dwc.doshisha.ac.jp/rd/html/japanese/researchersHtml/2691/2691_Researcher.html | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | A simple method was derived for predicting the ora1 bioavailability (F) -- as the product of intestinal availability (Fg) and hepatic availability (Fh) -- of a drug subjected to both intestinal and hepatic first-pass effects. Oral clearance (CL/F) data, rather than in-vitro metabolic clearance data, is used together with the unbound fraction in blood protein (fbu), Caco-2 cell membrane permeability (Papp, Caco-2), and efflux ratio in membrane permeation (ER). Fg was expressed as Fg = 1/(1 + Fg × (CL/F)/H), where H was SF (scaling factor) × fbu × (1 + ER) × Papp, Cao-2, and SF was determined to be approximately 5 from the ratio of gut-wall intrinsic clearance to hepatic intrinsic clearance (ν g/h = O.Ol) -- a correlation between the extent of absorption (Fa) and Papp, Caco-2 for BCS Class III drugs (m = 0.035 s/nm) and intestinal transit time (τ = 3hr). Fg, Fh, and F for CYP3A4 substrates known to exhibit significant gut-wall extraction were successfully predicted using the present method. The results demonstrated the method's usefulness for predicting the oral bioavailability of a drug subjected to both gut-wall extraction and hepatic extraction, as well as understanding gut-wall extraction in relation to CL/F, fbu, Papp, Caco-2, and ER. | |||||
内容記述 | ||||||
内容記述タイプ | Other | |||||
内容記述 | 論文 (Article) | |||||
書誌情報 |
総合文化研究所紀要 en : Bulletin of Institute for Interdisciplinary Studies of Culture Doshisha Women’s College of Liberal Arts 巻 29, p. 118-131, 発行日 2012-03-30 |
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出版地 | ||||||
出版者 | 京都 | |||||
出版者 | ||||||
出版者 | 同志社女子大学総合文化研究所 (教育・研究推進センター) | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 09100105 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AN10052143 | |||||
論文ID(NAID) | ||||||
識別子タイプ | NAID | |||||
関連識別子 | 40019427482 | |||||
ID | ||||||
内容記述タイプ | Other | |||||
内容記述 | AN10052143-20120330-118 |