Biopharmaceutics classification systems for new molecular entities (BCS-NMEs) and marketed drugs (BCS-MD): Theoretical basis and practical examples

International Journal of Pharmaceutics

Volumn 361, Issue 1-2, 2008, Pages 70-77

  Papadopoulou, Vasiliki ^a   Valsami, Georgia ^a   Dokoumetzidis, Aristides ^b   Macheras, Panos ^a  

^a UNIVERSITY OF ATHENS   (Greece)

^b UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

Absorption; Biopharmaceutics Classification System; Marketed drugs; New molecular entities; Solubility dose ratio

Indexed keywords

ALLOPURINOL; FUROLIN; IBUPROFEN; METOPROLOL TARTRATE; NAPROXEN; NITROFURANTOIN; PARACETAMOL; ZYLAPUR;

ARTICLE; DRUG ABSORPTION; DRUG PENETRATION; DRUG SOLUBILITY; INTESTINE TRANSIT TIME; INTESTINE WALL; PRIORITY JOURNAL; THEORETICAL STUDY;

BIOPHARMACEUTICS; DOSE-RESPONSE RELATIONSHIP, DRUG; GASTROINTESTINAL TRANSIT; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; SOLUBILITY;

EID: 47949129181     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2008.05.021     Document Type: Article

References (34)

1. Amidon G.L., Lennernäs H., Shah V.P., and 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. 12 (1995) 413-420
2. Amidon G.L. Solubility, intrinsic dissolution and solubilization: influence on absorption. In: Amidon G.L., Robinson J.R., and Williams R.L. (Eds). Scientific Foundations for Regulating Drug Product Quality (1997), AAPS Press
3. Benet L., Amidon G., Barends D., Lennernas H., Polli J., Shah V., Stavstansky S., and Yu L. The use of BDDCS in classifying the permeability of marketed drugs. Pharm. Res. 25 (2008) 483-488
4. Bergstrom C.A.S., Strafford M., Lazorova L., Avdeef A., Luthman K., and Artursson P. Absorption classification of oral drugs based on molecular surface properties. J. Med. Chem. 46 (2003) 558-570
5. Dokoumetzidis A., Papadopoulou V., and Macheras P. Analysis of dissolution data using modified versions of Noyes-Whitney equation and the Weibull function. Pharm. Res. 23 (2006) 256-261
6. Dressman J.B., Amidon G.L., and Fleisher D. Absorption potential: estimating the fraction absorbed for orally administered compounds. J. Pharm Sci. 74 (1985) 588-589
7. Faassen F., and Vromans H. Biowaivers for oral immediate-release products, complication of linear pharmacokinetics. Clin. Pharmacok. 43 (2004) 1117-1126
8. Fagerholm U. Evaluation and suggested improvements of the biopharmaceutics classification system (BCS). J. Pharm. Pharmacol. 59 (2007) 751-757
9. FDA, 2000. Guidance for Industry, Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System. FDA/CDER, Washington, DC.
10. Gu C.H., Li H., Levons J., Lentz K., Gandhi R., Raghavan K., and Smith R. Predicting effect of food on extent of drug absorption based on physicochemical properties. Pharm. Res. 24 (2007) 1118-1130
11. Johnson K.C., and Swindell A.C. Guidance in the setting of drug particle size specifications to minimize variability in absorption. Pharm. Res. 13 (1996) 1795-1798
12. Kalampokis A., Argyrakis P., and Macheras P. A heterogeneous tube of intestinal drug absorption based on probabilistic concepts. Pharm. Res. 16 (1999) 1764-1769
13. Kasim N.A., Whitehouse M., Ramachandran C., Bermejo M., Lennernäs H., Hussain A.S., Junginger H.E., Stavchansky S.A., Midha K.K., Shah V.P., and Amidon G.L. Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol. Pharmacol. 1 (2004) 85-96
14. Kaus L.C., Gillespie W.R., Hussain A.S., and Amidon G.L. The effect of in vivo dissolution, gastric emptying rate, and intestinal transit time on the peak concentration and area-under-the-curve of drugs with different gastrointestinal permeabilities. Pharm. Res. 16 (1999) 272-280
15. Lindenberg M., Kopp S., and Dressman J.B. Classification of orally administered drugs on the World Health Organisation model list of essential medicines according to the biopharmaceutics classification system. Eur. J. Pharm. Sci. 58 (2004) 265-278
16. Linnankoski J., Makela J., Ranta V.-P., Urti A., and Ylipertula M. Computational prediction of oral drug absorption based on absorption rate constants in humans. J. Med. Chem. 49 (2006) 3674-3681
17. Macheras P.E., and Symillides M.Y. Toward a quantitative approach for the prediction of the fraction of dose absorbed using the absorption potential concept. Biopharm. Drug Dispos. 10 (1989) 43-53
18. Mueller E.A., Kovarik J.M., van Bree J.B., Tetzloff W., Grevel J., and Kutz K. Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharm. Res. 11 (1994) 301-304
19. Noyes A.S., and Whitney W.R. The rate of solution of solid substances in their own solutions. J. Am. Chem. Soc. 19 (1897) 930-934
20. Oh D.M., Curl R.L., and Amidon G.L. Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: a mathematical model. Pharm Res. 10 (1993) 264-270
21. 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 FR.A., Loper A.E., Nerurkar S.G., Polli J.W., Sanvordeker D.R., Taneja R., Uppoor R.S., Vattikonda C.S., Wilding I., and Zhang G. Summary workshop report: biopharmaceutics classification system-implementation challenges and extension opportunities. J. Pharm. Sci. 93 (2004) 1375-1381
22. Rinaki E., Dokoumetzidis A., and Macheras P. The mean dissolution time depends on dose/solubility ratio. Pharm. Res. 20 (2003) 406-408
23. Rinaki E., Valsami G., and Macheras P. Quantitative biopharmaceutics classification system: the central role of dose/solubility ratio. Pharm. Res. 20 (2003) 1917-1925
24. Rinaki E., Dokoumetzidis A., Valsami G., and Macheras P. Identification of biowaivers among class II drugs: theoretical justification and practical examples. Pharm. Res. 21 (2004) 1567-1572
25. Sanghvi T., Ni N., Mayersohn M., and Yalkowsky S.H. Predicting passive intestinal absorption using a single absorption parameter. QSAR 22 (2003) 247-257
26. Sun D., Lennernas H., Welage L.S., Barnetti J.L., Landowski C.P., Foster D., Fleisher D., Lee K.-D., and Amidon G.L. Comparison of human duodenum and Caco-2 gene expression profiles for 12,000 gene sequences tags and correlation with permeability of 26 drugs. Pharm. Res. 19 (2002) 1400-1416
27. U.S.P. 29-NF 24. 2006. The Official Compendia of Standards. U.S. Pharmacopoeia, Rockville, MD, p. 20812.
28. Willmann S., Schmitt W., Keldenich J., Lippert J., and Dressman J.B. A physiological model for the estimation of the fraction dose absorbed in humans. J. Med. Chem. 47 (2004) 4022-4031
29. Winiwarter S., Boham N.M., Ax F., Hallberg A., Lannernas H., and Karlen A. Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters: a multivariate data analysis approach. J. Med. Chem. 41 (1998) 4939-4949
30. Wu C.Y., and Benet L.Z. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system (BDDCS). Pharm. Res. 22 (2005) 11-23
31. Yalkowsky S.H., Johnson J.L., Sanghvi T., and Machatha S.G. A 'rule of unity' for human intestinal absorption. Pharm. Res. 23 (2006) 2475-2481
32. Yazdanian M., Briggs K., Yankovsky C., and Hawi A. The "high solubility" definition on the current FDA guidance on biopharmaceutical classification system may be too strict for acidic drugs. Pharm. Res. 21 (2004) 293-299
33. Yu L.X., Crison J.R., and Amidon G.L. Compartmental transit and dispersion model analysis of small intestinal transit flow in humans. Int. J. Pharm. 140 (1996) 111-118
34. 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., and Hussain A.S. Biopharmaceutics classification system: the scientific basis for biowaiver extensions. Pharm. Res. 19 (2002) 921-925