Biopharmaceutics classification system: Validation and learnings of an in vitro permeability assay

Molecular Pharmaceutics

Volumn 6, Issue 1, 2009, Pages 11-18

  Thiel Demby, Victoria E ^a   Humphreys, Joan E ^a   Williams, Lisa A St John ^a   Ellens, Harma M ^a   Shah, Nipa ^b   Ayrton, Andrew D ^b   Polli, Joseph W ^a,c  

^a GLAXOSMITHKLINE   (United States)

^b GLAXOSMITHKLINE   (United Kingdom)

^c NONE   (United States)

Author keywords

BCS; BDDCS; Biopharmaceutics classification system; Caco 2; In vitro; Intestinal absorption; MDCKII MDR1; P glycoprotein; Passive permeability; Transporter

Indexed keywords

ACICLOVIR; AMOXICILLIN; AMPRENAVIR; ATENOLOL; CARBAMAZEPINE; CIMETIDINE; ELACRIDAR; HYDROCHLOROTHIAZIDE; KETOPROFEN; LABETALOL; LISINOPRIL; METOPROLOL; MINOXIDIL; NADOLOL; NAPROXEN; PINDOLOL; PROPRANOLOL; RANITIDINE; SULPIRIDE; THEOPHYLLINE; TRIMETHOPRIM; VERAPAMIL; DRUG; GLYCOPROTEIN P;

ANIMAL CELL; ARTICLE; CELL LINE; CONTROLLED STUDY; DRUG CLASSIFICATION; DRUG PENETRATION; DRUG TRANSPORT; IN VITRO STUDY; INTESTINE ABSORPTION; NONHUMAN; PRIORITY JOURNAL; CELL MEMBRANE PERMEABILITY; CLASSIFICATION; HUMAN; METABOLISM; PH; PHARMACEUTICS; TIME;

BIOPHARMACEUTICS; CELL LINE; CELL MEMBRANE PERMEABILITY; HUMANS; HYDROGEN-ION CONCENTRATION; P-GLYCOPROTEIN; PHARMACEUTICAL PREPARATIONS; TIME FACTORS;

EID: 62649137652     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp800122b     Document Type: Article

References (23)

1. Center for Drug Evaluation and Research. Food and Drug Administration. Guidance for Industry: Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System. http://www.fda.gov/cder/guidance/ 3618fnl.Pdf 2000.
2. Amidon, G. L.; Lennernäs, H.; Shah, V. P.; Crison, J. R. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 1995, 12, 413-420.
3. Yu, L. X.; Amidon, G. L.; Polli, J. E.; Zhao, H.; Mehta, M. U.; Conner, D. P.; Shah, V. P.; Lesko, L. J.; Chen, M. L.; Lee, V. H.; Hussain, A. S. Biopharmaceutics classification system: the scientific basis for biowaiver extensions. Pharm. Res. 2002, 19, 921-925.
4. Polli, J. W.; Jarrett, J. L.; Studenberg, S. D.; Humphreys, J. E.; Dennis, S. W.; Brouwer, K. R.; Woolley, J. L. Role of P- glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor. Pharm. Res. 1999, 16, 1206-1212.
5. Tran, T. T.; Mittal, A.; Gales, T.; Maleeff, B.; Aldinger, T.; Polli, J. W.; Ayrton, A.; Ellens, H.; Bentz, J. Exact kinetic analysis of passive transport across a polarized confluent MDCK cell monolayer modeled as a single barrier. J. Pharm. Sci. 2004, 93, 2108-2123.
6. Zhao, Y. H.; Le, J.; Abraham, M. H.; Hersey, A.; Eddershaw, P. J.; Luscombe, C. N.; Butina, D.; Beck, G.; Sherborne, B.; Cooper, I.; Platts, J. A. Evaluation of human intestinal absorption data and subsequent derivation of a quantitative structure-activity relationship (QSAR) with the Abraham descriptors. J. Pharm. Sci. 2001, 90, 749-784.
7. Polli, J. W.; Wring, S. A.; Humphreys, J. E.; Huang, L.; Morgan, J. B.; Webster, L. O.; Serabjit-Singh, C. S. Rational use of in vitro P-glycoprotein assays in drug discovery. J. Pharmacol. Exp. Ther. 2001, 299, 620-628.
8. Mahar Doan, K. M.; Humphreys, J. E.; Webster, L. O.; Wring, S. A.; Shampine, L. J.; Serabjit-Singh, C. J.; Adkison, K. K.; Polli, J. W. Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J. Pharmacol. Exp. Ther. 2002, 505, 1029-1037.
9. Polli, J. E.; Yu, L. X.; Cook, J. A.; Amidon, G. L.; Borchardt, R. T.; Burnside, B. A.; Burton, P. S.; Chen, M. L.; Conner, D. P.; Faustino, P. J.; Hawi, A. A.; Hussain, A. S.; Joshi, H. N.; Kwei, G.; Lee, V. H.; Lesko, L. J.; Lipper, R. A.; Loper, A. E.; Nerurkar, S. G.; Polli, J. W.; Sanvordeker, D. R.; Taneja, R.; Uppoor, R. S.; Vattikonda, C. S.; Wilding, I.; Zhang, G. Summary workshop report: biopharmaceutics classification system-implementation challenges and extension opportunities. J. Pharm. Sci. 2004, 95, 1375-1381.
10. Taub, M. E.; Kristensen, L.; Frokjaer, S. Optimized conditions for MDCK permeability and turbidimetric solubility studies using compounds representative of BCS classes I-IV. Eur. J. Pharm. Sci. 2002, 15, 331-340.
11. Irvine, J. D.; Takahashi, L.; Lockhart, K.; Cheong, J.; Tolan, J. W.; Selick, H. E.; Grove, J. R. MDCK (Madin-Darby canine kidney) cells: A tool for membrane permeability screening. J. Pharm. Sci. 1999, 88, 28-33.
12. Lentz, K. A.; Hayashi, J.; Lucisano, L. J.; Polli, J. E. Development of a more rapid, reduced serum culture system for Caco-2 monolayers and application to the biopharmaceutics classification system. Int. J. Pharm. 2000, 200, 41-51.
13. Volpe, D. A. Variability in Caco-2 and MDCK cell-based intestinal permeability assays. J. Pharm. Sci. 2008, 97, 712-725.
14. Yang, Y.; Faustino, P. J.; Volpe, D. A.; Ellison, C. D.; Lyon, R. C.; Yu, L. X. Biopharmaceutics classification of selected beta- blockers: solubility and permeability class membership. Mol. Pharmaceutics 2007, 4, 608-614.
15. Tolle-Sander, S.; Polli, J. E. Method considerations for Caco-2 permeability assessment in the Biopharmaceutics Classification System. Pharm. Forum 2002, 28, 164-172.
16. Deconinck, E.; Hancock, T.; Coomans, D.; Massart, D. L.; Heyden, Y. V. Classification of drugs in absorption classes using the classification and regression trees (CART) methodology. J. Pharm. Biomed. Anal. 2005, 39, 91-103.
17. Blume, H. H.; Schug, B. S. The biopharmaceutics classification system (BCS): class III drugs - better candidates for BA/BE waiver? Eur. J. Pharm. Sci. 1999, 9, 117-121.
18. Fagerholm, U. Evaluation and suggested improvements of the Biopharmaceutics Classification System (BCS). J. Pharm. Pharmacol. 2007, 59, 751-757.
19. Jantratid, E.; Prakongpan, S.; Amidon, G. L.; Dressman, J. B. Feasibility of biowaiver extension to biopharmaceutics classification system class III drug products: cimetidine. Clin. Pharma- cokinet. 2006, 45, 385-399.
20. Benet, L. Z.; Amidon, G. L.; Barends, D. M.; Lennernäs, H.; Polli, J. E.; Shah, V. P.; Stavchansky, S. A.; Yu, L. X. The use of BDDCS in classifying the permeability ofmarketed drugs. Pharm. Res. 2008, 25, 483-488.
21. Kwon, H.; Lionberger, R. A.; Yu, L. X. Impact of P-glycoprotein- mediated intestinal efflux kinetics on oral bioavailability of P-glycoprotein substrates. Mol. Pharmaceutics 2004, 1, 455-465.
22. Cao, X.; Yu, L. X.; Barbaciru, C.; Landowski, C. P.; Shin, H. C.; Gibbs, S.; Miller, H. A.; Amidon, G. L.; Sun, D. Permeability dominates in vivo intestinal absorption of P-gp substrate with high solubility and high permeability. Mol. Pharmaceutics 2005, 2, 329-340.
23. Lin, J. H. How significant is the role of P-glycoprotein in drug absorption and brain uptake. Drugs Today (Barc.) 2004, 40,5-22.