Biopartitioning micellar chromatography: an in vitro technique for predicting human drug absorption.
The main oral drug absorption barriers are fluid cell membranes and generally drugs are absorbed by a passive diffusion mechanism. Biopartitioning micellar chromatography (BMC) is a mode of micellar liquid chromatography that uses micellar mobile phases of Brij35 under adequate experimental conditions and can be useful to mimic the drug partitioning process in biological systems. In this paper the usefulness of BMC for predicting oral drug absorption in humans is demonstrated. A hyperbolic model has been obtained using the retention data of a heterogeneous set of 74 compounds, which shows predictive ability for drugs absorbed by passive diffusion. The model obtained in BMC is compared with those obtained using the well-known systems (Caco-2 and TC-7) that use intestinal epithelium cell lines. The use of BMC is simple, reproducible and can provide key information about the transport properties of new compounds during the drug discovery process.
Molero-Monfort
M
M
Departamento de Química Analítica, Universidad de Valencia, Spain.
Escuder-Gilabert
L
L
Villanueva-Camañas
R M
RM
Sagrado
S
S
Medina-Hernández
M J
MJ
D000284:Administration, Oral; D002460:Cell Line; D002853:Chromatography, Liquid / Q000379:methods*; D006801:Humans; D066298:In Vitro Techniques; D007413:Intestinal Mucosa / Q000166:cytology / Q000378:metabolism; D008823:Micelles; D010599:Pharmacokinetics; D013056:Spectrophotometry, Ultraviolet
D008823:Micelles