Is the full potential of the biopharmaceutics classification system reached?

European Journal of Pharmaceutical Sciences

Volumn 57, Issue 1, 2014, Pages 224-231

  Bergström, Christel A S ^a   Andersson, Sara B E ^a   Fagerberg, Jonas H ^a   Ragnarsson, Gert ^b   Lindahl, Anders ^b  

^a UPPSALA UNIVERSITY   (Sweden)

^b MEDICAL PRODUCTS AGENCY   (Sweden)

Author keywords

Biopharmaceutics classification system; Biorelevant dissolution; Dose number; In silico; Poorly soluble; Solubility

Indexed keywords

AMLODIPINE; BENZNIDAZOLE; BUSPIRONE; CAFFEINE; CARBAMAZEPINE; CHLOROQUINE; CISAPRIDE; CITALOPRAM; CYCLOPHOSPHAMIDE; DAPSONE; DESIPRAMINE; DIAZEPAM; DIETHYLCARBAMAZINE; DILTIAZEM; DIPHENHYDRAMINE; DISOPYRAMIDE; DOXAZOSIN; DOXEPIN; DOXYCYCLINE; ENALAPRIL; EPHEDRINE; LANSOPRAZOLE; LORAZEPAM; NEVIRAPINE; OFLOXACIN; PHENAZOPYRIDINE; PRAZIQUANTEL; RIFAMPICIN; ROFECOXIB; UNINDEXED DRUG; DRUG;

ACIDITY; ARTICLE; BIOPHARMACEUTICS CLASSIFICATION SYSTEM; DIET RESTRICTION; DRUG ABSORPTION; DRUG CLASSIFICATION; DRUG SOLUBILITY; IN VITRO STUDY; IN VIVO STUDY; INTESTINE FLUID; LIPOPHILICITY; ORAL DRUG ADMINISTRATION; PH; PHARMACEUTICS; PRIORITY JOURNAL; SIMULATION; SMALL INTESTINE; SMALL INTESTINE ABSORPTION; SOLUBILIZATION; ANIMAL; BIOLOGICAL MODEL; CHEMISTRY; CLASSIFICATION; COMPUTER SIMULATION; HUMAN; INTESTINE; INTESTINE ABSORPTION; METABOLISM; NOMENCLATURE; PERMEABILITY; PHARMACOKINETICS; PROCEDURES; REPRODUCIBILITY; SOLUBILITY;

ADMINISTRATION, ORAL; ANIMALS; BIOPHARMACEUTICS; COMPUTER SIMULATION; HUMANS; HYDROGEN-ION CONCENTRATION; INTESTINAL ABSORPTION; INTESTINES; MODELS, BIOLOGICAL; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; REPRODUCIBILITY OF RESULTS; SOLUBILITY; TERMINOLOGY AS TOPIC;

EID: 84899957723     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2013.09.010     Document Type: Article

References (52)

1. G.L. Amidon, H. Lennernas, V.P. Shah, and J.R. Crison 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. L.Z. Benet The role of BCS (biopharmaceutics classification system) and BDDCS (Biopharmaceutics Drug Disposition Classification System) in drug development J. Pharm. Sci. 102 2013 34 42
3. C.A. Bergstrom, M. Strafford, L. Lazorova, A. Avdeef, K. Luthman, and P. Artursson Absorption classification of oral drugs based on molecular surface properties J. Med. Chem. 46 2003 558 570 (Pubitemid 36182757)
4. C.A. Bergstrom, C.M. Wassvik, K. Johansson, and I. Hubatsch Poorly soluble marketed drugs display solvation limited solubility J. Med. Chem. 50 2007 5858 5862 (Pubitemid 350106040)
5. L.L. Brunton Goodman and Gilman's The Pharmacological Basis of Therapeutics: Digital Edition 2005 McGraw-Hill Professional Publishing
6. J.M. Butler, and J.B. Dressman The Developability Classification System: application of biopharmaceutics concepts to formulation development J. Pharm. Sci. 99 2010 4940 4954
7. W.L. Chiou, and A. Barve Linear correlation of the fraction of oral dose absorbed of 64 drugs between humans and rats Pharm. Res. 15 1998 1792 1795 (Pubitemid 28524594)
8. K.A. Chu, and S.H. Yalkowsky An interesting relationship between drug absorption and melting point Int. J. Pharm. 373 2009 24 40
9. S. Clarysse, J. Brouwers, J. Tack, P. Annaert, and P. Augustijns Intestinal drug solubility estimation based on simulated intestinal fluids: comparison with solubility in human intestinal fluids Eur. J. Pharm. Sci. 43 2011 260 269
10. J.A. Cook, and H. Bockbrader An industrial implementation of the biopharmaceutics classification system Dissol. Technol. 9 2002 6 9
11. J.A. Cook, B.M. Davit, and J.E. Polli Impact of biopharmaceutics classification system-based biowaivers Mol. Pharm. 7 2010 1539 1544
12. B.M. Davit, M.L. Chen, D.P. Conner, S.H. Haidar, S. Kim, C.H. Lee, R.A. Lionberger, F.T. Makhlouf, P.E. Nwakama, D.T. Patel, D.J. Schuirmann, and L.X. Yu Implementation of a reference-scaled average bioequivalence approach for highly variable generic drug products by the US Food and Drug Administration AAPS J. 14 2012 915 924
13. J. Dressman, J. Butler, J. Hempenstall, and C. Reppas The BCS: where do we go from here? Pharm. Tech. 25 2001 68 76
14. J.B. Dressman, and C. Reppas In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs Eur. J. Pharm. Sci. 11 Suppl 2 2000 S73 80
15. EMA, 2010. Committe for Medicinal Products for Human Use. Guideline on the investigation of bioequivalence. < http://www.emea.europa.eu/docs/en-GB/ document-library/Scientific-guideline/2010/01/WC500070039.pdf > (accessed 3.05.13).
16. J.H. Fagerberg, Y. Al-Tikriti, G. Ragnarsson, and C.A. Bergstrom Ethanol effects on apparent solubility of poorly soluble drugs in simulated intestinal fluid Mol. Pharm. 9 2012 1942 1952
17. J.H. Fagerberg, O. Tsinman, N. Sun, K. Tsinman, A. Avdeef, and C.A. Bergstrom Dissolution rate and apparent solubility of poorly soluble drugs in biorelevant dissolution media Mol. Pharm. 7 2010 1419 1430
18. FDA, 2000. US 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/downloads/Drugs/./Guidances/ucm070246.pdf > (accessed 3.05.13).
19. E.D. Gamsiz, M. Ashtikar, J. Crison, W. Woltosz, M.B. Bolger, and R.L. Carrier Predicting the effect of fed-state intestinal contents on drug dissolution Pharm. Res. 27 2010 2646 2656
20. J. Gan, Q. Ruan, B. He, M. Zhu, W.C. Shyu, and W.G. Humphreys In vitro screening of 50 highly prescribed drugs for thiol adduct formation-comparison of potential for drug-induced toxicity and extent of adduct formation Chem. Res. Toxicol. 22 2009 690 698
21. H. Jung, L. Medina, L. Garcia, I. Fuentes, and R. Moreno-Esparza Absorption studies of albendazole and some physicochemical properties of the drug and its metabolite albendazole sulphoxide J. Pharm. Pharm. 50 1998 43 48 (Pubitemid 28052519)
22. K. Kleberg, J. Jacobsen, and A. Mullertz Characterising the behaviour of poorly water soluble drugs in the intestine: application of biorelevant media for solubility, dissolution and transport studies J. Pharm. Pharm. 62 2010 1656 1668
23. H. Lennernas Clinical pharmacokinetics of atorvastatin Clin Pharmacokinet 42 2003 1141 1160 (Pubitemid 37357650)
24. H. Lennernas, and B. Abrahamsson The use of biopharmaceutic classification of drugs in drug discovery and development: current status and future extension J. Pharm. Pharm. 57 2005 273 285 (Pubitemid 40326200)
25. M. Lindenberg, S. Kopp, and J.B. Dressman Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system Eur. J. Pharm. Biopharm. 58 2004 265 278 (Pubitemid 39037234)
26. U. Loos, E. Musch, J.C. Jensen, G. Mikus, H.K. Schwabe, and M. Eichelbaum Pharmacokinetics of oral and intravenous rifampicin during chronic administration Klinische Wochenschrift 63 1985 1205 1211 (Pubitemid 16169743)
27. A. Mathur, K. Venkatesan, V.P. Bharadwaj, and G. Ramu Evaluation of effectiveness of clofazimine therapy. I. Monitoring of absorption of clofazimine from gastrointestinal tract Indian J. Lepr. 57 1985 146 148 (Pubitemid 15030393)
28. R. Mellaerts, R. Mols, P. Kayaert, P. Annaert, J. Van Humbeeck, G. Van den Mooter, J.A. Martens, and P. Augustijns Ordered mesoporous silica induces pH-independent supersaturation of the basic low solubility compound itraconazole resulting in enhanced transepithelial transport Int. J. Pharm. 357 2008 169 179
29. S.D. Mithani, V. Bakatselou, C.N. TenHoor, and J.B. Dressman Estimation of the increase in solubility of drugs as a function of bile salt concentration Pharm. Res. 13 1996 163 167 (Pubitemid 26076314)
30. E. Nicolaides, M. Symillides, J.B. Dressman, and C. Reppas Biorelevant dissolution testing to predict the plasma profile of lipophilic drugs after oral administration Pharm. Res. 18 2001 380 388 (Pubitemid 32595828)
31. D.M. Oh, R.L. Curl, and G.L. Amidon Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: a mathematical model Pharm. Res. 10 1993 264 270 (Pubitemid 23041742)
32. G. Ottaviani, D.J. Gosling, C. Patissier, S. Rodde, L. Zhou, and B. Faller What is modulating solubility in simulated intestinal fluids? Eur. J. Pharm. Sci. 41 2010 452 457
33. M.A. Perez, M.B. Sanz, L.R. Torres, R.G. Avalos, M.P. Gonzalez, and H.G. Diaz A topological sub-structural approach for predicting human intestinal absorption of drugs Eur. J. Med. Chem. 39 2004 905 916 (Pubitemid 39389100)
34. J.E. Polli, B.S. Abrahamsson, L.X. Yu, G.L. Amidon, J.M. Baldoni, J.A. Cook, P. Fackler, K. Hartauer, G. Johnston, S.L. Krill, R.A. Lipper, W.A. Malick, V.P. Shah, D. Sun, H.N. Winkle, Y. Wu, and H. Zhang Summary workshop report: bioequivalence, biopharmaceutics classification system, and beyond AAPS J. 10 2008 373 379
35. J.E. Polli, L.X. Yu, J.A. Cook, G.L. Amidon, R.T. Borchardt, B.A. Burnside, P.S. Burton, M.L. Chen, D.P. Conner, P.J. Faustino, A.A. Hawi, A.S. Hussain, H.N. Joshi, G. Kwei, V.H. Lee, L.J. Lesko, R.A. Lipper, A.E. Loper, S.G. Nerurkar, J.W. Polli, D.R. Sanvordeker, R. Taneja, R.S. Uppoor, C.S. Vattikonda, I. Wilding, and G. Zhang Summary workshop report: biopharmaceutics classification system-implementation challenges and extension opportunities J. Pharm. Sci. 93 2004 1375 1381 (Pubitemid 38725012)
36. C.W. Pouton Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system Eur. J. Pharm. Sci. 29 2006 278 287 (Pubitemid 44740131)
37. D. Psachoulias, M. Vertzoni, K. Goumas, V. Kalioras, S. Beato, J. Butler, and C. Reppas Precipitation in and supersaturation of contents of the upper small intestine after administration of two weak bases to fasted adults Pharm. Res. 28 2011 3145 3158
38. E. Ramirez, O. Laosa, P. Guerra, B. Duque, B. Mosquera, A.M. Borobia, S.H. Lei, A.J. Carcas, and J. Frias Acceptability and characteristics of 124 human bioequivalence studies with active substances classified according to the Biopharmaceutic Classification System Br. J. Clin. Pharmacol. 70 2010 694 702
39. E. Rinaki, A. Dokoumetzidis, G. Valsami, and P. Macheras Identification of biowaivers among Class II drugs: theoretical justification and practical examples Pharm. Res. 21 2004 1567 1572 (Pubitemid 41184386)
40. E. Rinaki, G. Valsami, and P. Macheras Quantitative biopharmaceutics classification system: the central role of dose/solubility ratio Pharm. Res. 20 2003 1917 1925 (Pubitemid 38005521)
41. T. Sanghvi, N. Ni, M. Mayersohn, and S.H. Yalkowsky Predicting passive intestinal absorption using a single parameter Qsar. Comb. Sci. 22 2003 247 257 (Pubitemid 36723088)
42. E. Soderlind, E. Karlsson, A. Carlsson, R. Kong, A. Lenz, S. Lindborg, and J.J. Sheng Simulating fasted human intestinal fluids: understanding the roles of lecithin and bile acids Mol. Pharm. 7 2010 1498 1507
43. K. Sugano Fraction of a dose absorbed estimation for structurally diverse low solubility compounds Int. J. Pharm. 405 2011 79 89
44. T. Takagi, C. Ramachandran, M. Bermejo, S. Yamashita, L.X. Yu, and G.L. Amidon A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan Mol. Pharm. 3 2006 631 643 (Pubitemid 46087480)
45. D. Taubert, N. von Beckerath, G. Grimberg, A. Lazar, N. Jung, T. Goeser, A. Kastrati, A. Schomig, and E. Schomig Impact of P-glycoprotein on clopidogrel absorption Clin. Pharmacol. Ther. 80 2006 486 501 (Pubitemid 44767878)
46. M.V. Varma, I. Gardner, S.J. Steyn, P. Nkansah, C.J. Rotter, C. Whitney-Pickett, H. Zhang, L. Di, M. Cram, K.S. Fenner, and A.F. El-Kattan pH-Dependent solubility and permeability criteria for provisional biopharmaceutics classification (BCS and BDDCS) in early drug discovery Mol. Pharm. 9 2012 1199 1212
47. WHO, 2006. Proposal to waive in vivo bioequivalence requirements for the WHO model list of essential medicines immediate release, solid oral dosage forms. In: Fortieth report of the WHO Expert Committee on Specifications for Pharmaceutical Preparations. Geneva, World Health Organization. Technical Report Series, no. 937, Annex 8.
48. C.Y. Wu, and L.Z. Benet Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system Pharm. Res. 22 2005 11 23 (Pubitemid 40558141)
49. Y. Yang, P.J. Faustino, D.A. Volpe, C.D. Ellison, R.C. Lyon, and L.X. Yu Biopharmaceutics classification of selected beta-blockers: solubility and permeability class membership Mol. Pharm. 4 2007 608 614 (Pubitemid 47310172)
50. M. Yazdanian, K. Briggs, C. Jankovsky, and A. Hawi The "high solubility" definition of the current FDA Guidance on Biopharmaceutical Classification System may be too strict for acidic drugs Pharm. Res. 21 2004 293 299 (Pubitemid 38221975)
51. L.X. Yu, G.L. Amidon, J.E. Polli, H. Zhao, M.U. Mehta, D.P. Conner, V.P. Shah, L.J. Lesko, M.L. Chen, V.H. Lee, and A.S. Hussain Biopharmaceutics classification system: the scientific basis for biowaiver extensions Pharm. Res. 19 2002 921 925 (Pubitemid 34804232)
52. C. Zhu, L. Jiang, T.M. Chen, and K.K. Hwang A comparative study of artificial membrane permeability assay for high throughput profiling of drug absorption potential Eur. J. Med. Chem. 37 2002 399 407 (Pubitemid 34465549)