@article{oai:dwcla.repo.nii.ac.jp:00000737,
 author = {伊賀, 勝美 and IGA, Katsumi},
 journal = {総合文化研究所紀要, Bulletin of Institute for Interdisciplinary Studies of Culture Doshisha Women’s College of Liberal Arts},
 month = {Mar},
 note = {AN10052143-20120330-118, 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., 論文 (Article)},
 pages = {118--131},
 title = {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},
 volume = {29},
 year = {2012},
 yomi = {イガ, カツミ}
}