Permeability of lipophilic compounds in drug discovery using in-vitro human absorption model, Caco-2

International Journal of Pharmaceutics

Volumn 222, Issue 1, 2001, Pages 77-89

  Krishna, Gopal ^a   Chen, Kwang Jong ^a   Lin, Chin Chung ^b   Nomeir, Amin A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b Valeant Pharmaceuticals International   (United States)

Author keywords

Bovine serum albumin; Caco 2; Lipophilic compounds; Non specific binding; Oral absorption; Permeability

Indexed keywords

BOVINE SERUM ALBUMIN; DIMETHYL SULFOXIDE; MANNITOL; NEW DRUG; PROGESTERONE; PROPRANOLOL; SCH A; SCH B; UNCLASSIFIED DRUG;

APICAL MEMBRANE; ARTICLE; BASOLATERAL MEMBRANE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CONTROLLED STUDY; DRUG ABSORPTION; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG STRUCTURE; HUMAN; HUMAN CELL; IN VITRO STUDY; LIPOPHILICITY; MONKEY; NONHUMAN; PRIORITY JOURNAL; TRANSPORT MEDIUM;

CACO-2 CELLS; CHEMISTRY, PHARMACEUTICAL; HUMANS; MANNITOL; MOLECULAR WEIGHT; PERMEABILITY; PROGESTERONE; PROPRANOLOL; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0035800246     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0378-5173(01)00698-6     Document Type: Article

References (18)

1. Caco-2 monolayers in experimental and theoretical predictions of drug transport
2. Evidence of a polarized efflux system in Caco-2 cells capable of modulating cyclosporine A transport
3. The use of the intestinal epithelial cell culture model, Caco-2, in pharmaceutical development
4. Pharmacokinetics and mechanisms of drug absorption in drug discovery, preclinical and Phase I studies
5. Absorption of Cam-2445, an NK1 neurokinin receptor antagonist: In vivo, in situ, and in vitro evaluations
6. Age dependent expression of P-glycoprotein gp 170 in Caco-2 cell monolayers
7. Functional expression of p-glycoprotein in the apical membranes of human intestinal Caco-2 cells
8. Dissociation and association rate constants changes following bilirubin binding affinity decreases
9. Higher-throughput P-glycoprotein assay for screening compounds in drug discovery
10. Specific inhibitors distinguish the chloride channel and drug transporter functions associated with the human multidrug resistance p-glycoprotein
11. The use of surfactants to enhance the permeability of peptides through Caco-2 cells by inhibition of an apically polarized efflux system
12. Permeable support type influences the transport of compounds across Caco-2 cells
13. Effect of restricted conformational flexibility on the permeation of model hexapeptides across Caco-2 cell monolayers
14. Comparison of the permeability characteristic of a human colonic epithelial (Caco-2) cell line to colon of rabbit, monkey, and dog intestine and human drug absorption
15. Identification of pharmacokinetically stable 3,10-dibromo-8-chlorobenzo-cycloheptapyridine farensyl protein transferase inhibitors with potent enzyme and cellular activities
16. Intestinal absorption screening of mixtures from combinatorial libraries in the Caco-2 model
17. High lipophilicity decreases drug transport across intestinal epithelial cells
18. In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man- fact or myth