In vitro-in vivo extrapolation (IVIVE) for predicting human intestinal absorption and first-pass elimination of drugs: principles and applications.
Drug Dev Ind Pharm
; 40(8): 989-98, 2014 Aug.
Article
em En
| MEDLINE
| ID: mdl-23981203
ABSTRACT
Oral administration remains the preferred dosing method in clinical practice and drug development. Oral bioavailability (F) is a function of the fraction absorbed (Fabs), gastrointestinal or gut wall availability (FG), and hepatic availability (FH). Therefore, predicting intestinal absorption (Fabs) and first-pass elimination (FG and FH) from in vitro data may facilitate the selection of more orally bioavailable drug candidates in earlier stages of drug discovery and development. This review provides an overview of the determinants of intestinal absorption and first-pass elimination of drugs and focuses on the principles and applications of conventional in vitro--in vivo extrapolation (IVIVE) methods to predict Fabs, FG, and FH in humans.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Preparações Farmacêuticas
/
Absorção Intestinal
Tipo de estudo:
Prognostic_studies
/
Risk_factors_studies
Limite:
Humans
Idioma:
En
Revista:
Drug Dev Ind Pharm
Ano de publicação:
2014
Tipo de documento:
Article