Current methodologies used for evaluation of intestinal permeability and absorption

Journal of Pharmacological and Toxicological Methods

Volumn 44, Issue 1, 2000, Pages 301-312

  Balimane, Praveen V ^a   Chong, Saeho ^a   Morrison, Richard A ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Absorption; In silica; In vitro; In vivo; Permeability; Physicochemical properties

Indexed keywords

ACICLOVIR; CHLOROTHIAZIDE; DIGOXIN; GRISEOFULVIN; HYDROCHLOROTHIAZIDE; PHENYTOIN; PREDNISOLONE;

ARTICLE; DRUG ABSORPTION; DRUG PENETRATION; DRUG SCREENING; EVALUATION; HUMAN; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; LIPOPHILICITY; METHODOLOGY; NONHUMAN; PHYSICAL CHEMISTRY;

ANIMALS; CELL LINE; CHROMATOGRAPHY; HUMANS; INTESTINAL ABSORPTION; INTESTINE, SMALL; PERMEABILITY; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; SOLUBILITY;

EID: 0034458680     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1056-8719(00)00113-1     Document Type: Article

References (69)

1. Cell cultures as models for drug absorption across the intestinal mucosa
2. Intestinal drug absorption and metabolism in cell cultures: Caco-2 and beyond
3. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells
4. Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2)
5. Caco-2 monolayers in experimental and theoretical predictions of drug transport
6. Immobilized-liposome chromatographic analysis of drug partitioning into lipid bilayers
7. The application of cell culture systems in drug discovery and development
8. Morphology of the intestinal mucosa
9. The Madin-Darby canine kidney (MDCK) epithelial cell monolayer as a model cellular transport barrier
10. Evaluation of Biocat intestinal epithelium differentiation environment (3-day cultured Caco-2 cells) as an absorption screening model with improved productivity
11. In vitro permeability through Caco-2 cells is not quantitatively predictive of in vivo absorption for peptide-like drugs absorbed via the dipeptide transporter system
12. Rapid calculation of polar molecular surface area and its application to the prediction of transport phenomena: 1. Prediction of intestinal absorption
13. Transcellular uptake mechanisms of the intestinal epithelial barrier: Part 1
14. Comparison of canine and human gastrointestinal physiology
15. Absorption potential: Estimating the fraction absorbed for orally administered compounds
16. A correlation for permeabilities of passively transported compounds in monkey and rabbit jejunum
17. Correlation between oral drug absorption in humans, and apparent drug permeability in TC-7 cells, a human epithelial cell line: Comparison with the parental Caco-2 cell line
18. Characterization of human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability
19. In vitro systems for studying intestinal drug absorption
20. Physical model approach to the design of drugs with improved intestinal absorption
21. Quantitative approaches to delineate passive transport mechanism in cell culture monolayers
22. A reevaluation of the importance of partition coefficients in the gastrointestinal absorption of nutrients
23. MDCK (Madin-Darby canine kidney) cells: A tool for membrane permeability screening
24. Physicochemical high throughput screening: Parallel artificial membrane permeation assay in the description of passive absorption processes
25. Comparison of the gastrointestinal anatomy, physiology and biochemistry of humans and commonly used laboratory animals
26. Absorption prediction from physicochemical parameters
27. Noncovalent immobilized artificial membrane chromatography, an improved method for describing peptide-lipid bilayer interactions
28. Human intestinal permeability
29. Jejunal permeability: A comparison between the Ussing chamber technique and the single pass perfusion in humans
30. Development of a more rapid culture system for Caco-2 monolayers
31. An automated system for maintaining Caco-2 cell cultures and performing high throughput permeability screening
32. Species similarities and differences in pharmacokinetics
33. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
34. Functional morphology of the mucosa of the small intestine
35. The use of isolated vesicles to study epithelial transport processes
36. Evaluation of dynamic polar molecular surface area as predictor of drug absorption: Comparison with other computational and experimental predictors
37. Polar molecular surface properties predict the intestinal absorption of drugs in humans
38. Immobilized artificial membranes
39. Solid phase membrane mimetics: Immobilized artificial membranes
40. Methods of study of intestinal absorption and metabolism
41. Comparison of the permeability characteristics of a human colonic epithelial (Caco-2) cell line to colon of rabbit, monkey, and dog intestine and human drug absorption
42. Flux measurements across Caco-2 monolayers may predict transport in human large intestinal tissue
43. An automated system for the determination of intestinal permeability (Caco-2 cells) in support of drug discovery
44. Absorption of drugs from the rat small intestine
45. Oral absorption of anti-AIDS nucleoside analogues: 1. Intestinal transport of didanosine in rat and rabbit preparations
46. Prediction of the intestinal absorption of endothelin receptor antagonists using three theoretical methods of increasing complexity
47. Use of immobilized artificial membrane chromatography for drug transport applications
48. Comparison of intestinal permeabilities determined in multiple in vitro and in situ models: Relationship to absorption in humans
49. A conditionally immortalized epithelial cell line for studies of intestinal drug transport
50. The effect of surgical bowel manipulation and anesthesia on intestinal glucose absorption in rats
51. Membrane transport of drugs in different regions of the intestinal tract of the rat
52. Active transport of sidium as a source of electric current in the short-circuited isolated frog skin
53. Oral absorption of anti-acquired immune deficiency syndrome nucleoside analogues: 2. Carrier-mediated intestinal transport of stavudine in rat and rabbit preparations
54. Heterogeneity in the human intestinal cell line Caco-2 leads to differences in transepithelial transport
55. Prediction of human intestinal absorption of drug compounds from molecular structure
56. The use of sacs of everted small intestine for the study of the transference of substances from the mucosal to the serosal surface
57. Immobilized artificial membranes - Screens for drug membrane interactions