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Titolo:
Molecular and pharmacokinetic properties of 222 commercially available oral drugs in humans
Autore:
Sakaeda, T; Okamura, N; Nagata, S; Yagami, T; Horinouchi, M; Okumura, K; Yamashita, F; Hashida, M;
Indirizzi:
Kobe Univ, Sch Med, Dept Hosp Pharm, Chuo Ku, Kobe, Hyogo 6500017, Japan Kobe Univ Kobe Hyogo Japan 6500017 m, Chuo Ku, Kobe, Hyogo 6500017, Japan Shionogi & Co Ltd, Shionogi Res Labs, Osaka 5530002, Japan Shionogi & Co Ltd Osaka Japan 5530002 ogi Res Labs, Osaka 5530002, Japan Kyoto Univ, Grad Sch Pharmaceut Sci, Dept Drug Delivery Res, Sakyo Ku, Kyoto 6068501, Japan Kyoto Univ Kyoto Japan 6068501 ivery Res, Sakyo Ku, Kyoto 6068501, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 8, volume: 24, anno: 2001,
pagine: 935 - 940
SICI:
0918-6158(200108)24:8<935:MAPPO2>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
IN-VITRO; INTESTINAL-ABSORPTION; MEMBRANE-PERMEABILITY; CACO-2 CELLS; METABOLISM; THROUGHPUT; PREDICT; EFFLUX; MODEL;
Keywords:
oral absorption; exclusion criteria; molecular weight; lipophilicity;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Sakaeda, T Kobe Univ, Sch Med, Dept Hosp Pharm, Chuo Ku, 7-5-2 Kusunoki Cho, Kobe, Hyogo 6500017, Japan Kobe Univ 7-5-2 Kusunoki Cho Kobe Hyogo Japan6500017 17, Japan
Citazione:
T. Sakaeda et al., "Molecular and pharmacokinetic properties of 222 commercially available oral drugs in humans", BIOL PHAR B, 24(8), 2001, pp. 935-940

Abstract

This study was performed to determine the exclusion criteria that differentiate poorly absorbed drugs from good drug candidates, and to accelerate drug development by exclusion of unnecessary assessment. The molecular and pharmacokinetic properties of 222 commercially available oral drugs were tabulated and their correlations were analyzed. The exclusion criteria obtainedwere 1) a molecular weight of more than 500, and 2) a ClogP value of more than 5. Exceptions to molecular weight criteria were compounds with a sugarmoiety., high atomic weight, and large cyclic structure. It was also suggested that being a substrate for MDR1 (P-glycoprotein) does not always result in poor bioavailability, and that drug development by chemical modification of a seed or lead compound with quantitative structure activity relationship analysis can result in lower bioavailability, higher bound fraction and lower urinary excretion, which would hamper later development processes and might result in considerable drug-drug interaction. The criteria should be adjusted according to the pharmacological profiles of the agents in question and depending on the estimated profit, but ignoring these criteria mayresult in a significant waste of time and money during drug development.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/04/20 alle ore 01:18:47