513
Views
16
CrossRef citations to date
0
Altmetric
Reviews

Current regulatory approaches of bioequivalence testing

(Lecturer in Pharmacokinetics) & (Professor in Biopharmaceutics - Pharmacokinetics)
Pages 929-942 | Published online: 11 Jun 2012

Bibliography

  • Sisko A, Truffer C, Keehan S, National health spending projections: the estimated impact of reform through 2019. Health Aff 2010;29:1933-41
  • Carpenter D, Tobbell DA. Bioequivalence: the regulatory career of a pharmaceutical concept. Bull Hist Med 2011;85:93-131
  • Niazi S. Handbook of bioequivalence testing. 1st edition. Informa Healthcare; NY: 2007
  • Chen ML, Shah VP, Crommelin DJ, Harmonization of regulatory approaches for evaluating therapeutic equivalence and interchangeability of multisource drug products: workshop summary report. Eur J Pharm Sci 2011;44:506-13
  • Chen ML, Shah VP, Crommelin DJ, Harmonization of regulatory approaches for evaluating therapeutic equivalence and interchangeability of multisource drug products: workshop summary report. AAPS J 2011;13:556-64
  • European Medicines Agency, Evaluation of Medicines for Human Use, CPMP. Note for guidance on the investigation of bioavailability and bioequivalence. London: 2001
  • European Medicines Agency, Evaluation of Medicines for Human Use, CHMP. Guideline on the investigation of bioequivalence. London: 2010
  • Food and Drug Administration, Center for Drug Evaluation and Research (CDER), bioavailability and bioequivalence studies for orally administered drug products, general considerations. Rockville, MD: 2003
  • Chen ML, Shah V, Patnaik R, Bioavailability and bioequivalence: an FDA regulatory overview. Pharm Res 2001;18:1645-50
  • Bois F, Tozer T, Hauck W, Bioequivalence: performance of several measures of extent of absorption. Pharm Res 1993;11:715-22
  • Bois F, Tozer T, Hauck W, Bioequivalence: performance of several measures of rate of absorption. Pharm Res 1994;11:966-74
  • Chen ML, Lesko LJ, Williams RL. Measures of exposure versus measures of rate and extent of absorption. Clin Pharmacokinet 2001;40:565-72
  • Rescigno A. Bioequivalence. Pharm Res 1992;9:925-8
  • Chinchilli VM, Elswick RK. The multivariate assessment of bioequivalence. J Biopharm Stat 1997;7:113-23
  • Moore J, Flanner H. Mathematical comparison of curves with an emphasis on in vitro dissolution profiles. Pharm Tech 1996;20:64-74
  • Polli JE, McLean AM. Novel direct curve comparison metrics for bioequivalence. Pharm Res 2001;18:734-41
  • Karalis V, Macheras P. Pharmacodynamic considerations in bioequivalence assessment: comparison of novel and existing metrics. Eur J Pharm Sci 2003;19:45-56
  • Endrenyi L, Tothfalusi L. Without extrapolation, Cmax/AUC is an effective metric in investigations of bioequivalence. Pharm Res 1995;12:937-42
  • Macheras P, Symillides M, Reppas C. An improved intercept method for the assessment of absorption rate in bioequivalence studies. Pharm Res 1996;13:1755-8
  • Chen ML. An alternative approach for assessment of rate of absorption in bioequivalence studies. Pharm Res 1992;9:1380-5
  • Macheras P, Symillides M, Reppas C. The cutoff time point of the partial area method for assessment of rate of absorption in bioequivalence studies. Pharm Res 1994;11:831-4
  • Midha KK, Hubbard JW, Rawson MJ The application of partial areas in assessment of rate and extent of absorption in bioequivalence studies of conventional release products: experimental evidence. Eur J Pharm Sci 1994;2:351-63
  • Reppas C, Lacey LF, Keene ON, Evaluation of different metrics as indirect measures of rate of drug absorption from extended release dosage forms at steady-state. Pharm Res 1995;12:103-7
  • Endrenyi L, Csizmadia F, Tothfalusi L, The duration of measuring partial AUCs for the assessment of bioequivalence. Pharm Res 1998;15:399-404
  • Endrenyi L, Csizmadia F, Tothfalusi L, Metrics comparing simulated early concentration profiles for the determination of bioequivalence. Pharm Res 1998;15:1292-9
  • Chen ML, Davit B, Lionberger R, Using partial area for evaluation of bioavailability and bioequivalence. Pharm Res 2011;28:1939-47
  • Tozer TN, Bois FY, Hauck WW, Absorption rate vs. exposure: which is more useful for bioequivalence testing? Pharm Res 1996;13:453-6
  • Food and Drug Administration, Center for Drug Evaluation and Research (CDER), statistical approaches to establishing bioequivalence. Rockville, MD: 2001
  • Westlake WJ. The design and analysis of comparative blood-level trials. In: Swarbrick J, editor. Current concepts in the pharmaceutical sciences, dosage form design and bioavailability. Lea and Febiger, Philadelphia 1973. p. 149-79
  • Westlake WJ. Bioavailability and bioequivalence of pharmaceutical formulations. In: Peace KE, editor. Biopharmaceutical statistics for drug development. Marcel Dekker, Inc.; New York 1988. p. 329-52
  • Schuirmann D. A comparison of the two one-sided tests procedure and the power approach for assessing the equivalence of average bioavailability. J Pharmacokinet Biopharm 1987;15:657-80
  • Hauck WW, Anderson S. Types of bioequivalence and related statistical considerations. Int J Clin Pharmacol Ther Toxicol 1992;30:181-7
  • Schall R, Luus H. On population and individual bioequivalence. Stat Med 1993;12:1109-24
  • Chinchilli VM. The assessment of individual and population bioequivalence. J Biopharm Stat 1996;6:1-14
  • Anderson S, Hauck W. Consideration of individual bioequivalence. J Pharmacokinet Biopharm 1990;18:259-73
  • Hauck W, Anderson S. Individual bioequivalence: what matters to the patient. Stat Med 1991;10:959-60
  • Schall R, Williams R. Towards a practical strategy for assessing individual bioequivalence. J Pharmacokinet Biopharm 1996;24:133-49
  • Patnaik R, Lesko L, Chen ML, Individual bioequivalence: new concepts in the statistical assessment of bioequivalence metrics. Clin Pharmacokinet 1997;33:1-6
  • Midha K, Rawson M, Hubbard J. Individual and average bioequivalence of highly variable drugs and drug products. J Pharm Sci 1997;86:1193-7
  • Endrenyi L, Amidon G, Midha K, Individual bioequivalence: attractive in principle, difficult in practice. Pharm Res 1998;15:1321-5
  • Haidar S, Davit B, Chen ML, Bioequivalence approaches for highly variable drugs and drug products. Pharm Res 2008;15:237-41
  • Haidar S, Makhlouf F, Schuirmann D, Evaluation of a scaling approach for the bioequivalence of highly variable drugs. AAPS J 2008;10:450-4
  • Food and Drug Administration, Office of Generic Drugs, Draft Guidance for Industry on Bioequivalence Recommendations for Progesterone Capsules, Feb2011
  • Shah V, Yacobi A, Barr W, Evaluation of orally administered highly variable drugs and drug formulations. Pharm Res 1996;13:1590-4
  • Blume H, Elze M, Potthast H, Practical strategies and design advantages in highly variable drug studies: multiple dose and replicate administration design. In: Blume H, Midha K, editors. Bio-international 2: bioavailability, bioequivalence and pharmacokinetic studies. Medpharm Scientific Publishers; Stuttgart: 1995. p. 117-22
  • El-Tahtawy A, Jackson A, Ludden T. Comparison of single and multiple dose pharmacokinetics using clinical bioequivalence data and monte carlo simulations. Pharm Res 1994;11:1330-6
  • El-Tahtawy A, Jackson A, Ludden T. Evaluation of bioequivalence of highly variable drugs using monte carlo simulations. Part I: estimation of rate of absorption for single and multiple dose trials using Cmax. Pharm Res 1995;12:1634-41
  • Jackson A. Prediction of steady-state bioequivalence relationships using single dose data I-linear kinetics. Biopharm Drug Dispos 1987;8:483-96
  • Benet L. Bioavailability and bioequivalence: definitions and difficulties in acceptance criteria. In: Midha KK, Blume HH, editors. Bio-International: bioavailability, bioequivalence and pharmacokinetics. Medpharm Scientific; Stuttgart: 1995. p. 27-35
  • McGilveray I, Midha K, Skelly J, Consensus report from “Bio-International ‘89”: issues in the evaluation of bioavailability data. J Pharm Sci 1990;79:945-6
  • Blume H, Midha K. Bio-International ‘92, Conference on bioavailability, bioequivalence and pharmacokinetic studies. J Pharm Sci 1993;82:1186-9
  • Van Peer A. Variability and impact on design of bioequivalence studies. Basic Clin Pharmacol Toxicol 2010;106:146-53
  • Tothfalusi L, Endrenyi L, Midha K. Scaling or wider bioequivalence limits for highly variable drugs and for the special case of Cmax. Int J Clin Pharmacol Ther 2003;41:217-25
  • Blume HH, McGilveray IJ, Midha KK. Bio-International 94, conference on bioavailability bioequivalence and pharmacokinetic studies. Eur J Pharm Sci 1995;3:113-24
  • Boddy A, Snikeris F, Kringle R, An approach for widening the bioequivalence acceptance limits in the case of highly variable drugs. Pharm Res 1995;12:1865-8
  • Tothfalusi L, Endrenyi L. Limits for the scaled average bioequivalence of highly variable drugs and drug products. Pharm Res 2003;20:382-9
  • Karalis V, Symillides M, Macheras P. Novel scaled average bioequivalence limits based on GMR and variability considerations. Pharm Res 2004;21:1933-42
  • Karalis V, Macheras P, Symillides M. Geometric mean ratio dependent scaled bioequivalence limits with leveling-off properties. Eur J Pharm Sci 2005;26:54-61
  • Kytariolos J, Karalis V, Macheras P, Novel scaled bioequivalence limits with leveling-off properties. Pharm Res 2006;23:2657-64
  • Karalis V, Symillides M, Macheras P. On the leveling-off properties of the new bioequivalence limits for highly variable drugs of the EMA guideline. Eur J Pharm Sci 2011;44:497-505
  • Karalis V, Symillides M, Macheras P. Bioequivalence of highly variable drugs: a comparison of the newly proposed regulatory approaches by FDA and EMA. Pharm Res 2011; published online 28 December 2011; doi: 10.1007/s11095-011-0651-y
  • Tothfalusi L, Endrenyi L, Arieta AG. Evaluation of bioequivalence for highly variable drugs with scaled average bioequivalence. Clin Pharmacokinet 2009;48:725-43
  • Tothfalusi L, Endrenyi L. Sample sizes for designing bioequivalence studies for highly variable drugs. J Pharm Pharm Sci 2011;15:73-84
  • Karalis V, Symillides M, Macheras P. Comparison of the reference scaled bioequivalence semi-replicate method with other approaches: focus on human exposure to drugs. Eur J Pharm Sci 2009;38:55-63
  • Midha K, Rawson M, Hubbard J. The Role of metabolites in bioequivalence. Pharm Res 2004;21:1331-44
  • Midha K, Shah V, Singh G, Conference report: bio-international 2005. J Pharm Sci 2007;96:747-54
  • Houston JB. Importance of metabolites in bioequivalence. In: McGilveray JJ, Dighe SV, French IW, editors. Proceedings bio-international 89: issues in the evaluation of bioavailability data. Toronto, Canada, 1989. p. 99-100
  • Jackson AJ, Robbie G, Marroum P. Metabolites and bioequivalence: past and present. Clin Pharmacokinet 2004;43:655-72
  • Karalis V, Macheras P. Examining the role of metabolites in bioequivalence assessment. J Pharm Pharm Sci 2010;13:198-217
  • Welling PG. Influence of food and diet on gastrointestinal drug absorption: a review. J Pharmacokinet Biopharm 1977;5:291-334
  • Olanoff L, Walle T, Cowart T, Food effects on propranolol systemic and oral clearance: support for a blood flow hypothesis. Clin Pharmacol Ther 1986;40:408-14
  • Gupta S, Benet L. High-fat meals increase the clearance of cyclosporine. Pharm Res 1990;7:46-8
  • Food and Drug Administration, Center for Drug Evaluation and Research (CDER), Guidance for industry food-effect bioavailability and fed bioequivalence studies. 2002
  • European Medicines Agency, Note for guidance on modified release oral and transdermal dosage forms: section II (pharmacokinetic and clinical evaluation). Committee for Proprietary Medicinal Products (CPMP). CPMP/EWP/280/96 1999
  • European Medicines Agency, CHMP efficacy working party therapeutic subgroup on pharmacokinetics (EWP-PK). Questions & answers on the bioavailability and bioequivalence guideline. London: 2006
  • Food and Drug Administration, Guidance for Industry, Immediate Release Solid Oral Dosage Forms Scale-Up and Post-approval Changes: Chemistry, Manufacturing, and Controls, In Vitro Dissolution Testing, and In Vivo Bioequivalence Documentation. 1995
  • Shah V, Tsong Y, Sathe P. In vitro dissolution profile comparison – statistics and analysis of the similarity factor, f2. Pharm Res 1998;15:889-96
  • Amidon G, Lennernas H, Shah V, A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995;12:413-20
  • Wu C, Benet LZ. Predicting drug disposition via application of BCS: transport/ absorption/ elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 2005;22:11-23
  • Chen ML, Amidon GL, Benet LZ, The BCS, BDDCS, and regulatory guidances. Pharm Res 2011;28:1774-8
  • Dahan A, Miller JM, Amidon GL. Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs. AAPS J 2009;11:740-6
  • Food and Drug Administration, Center for Drug Evaluation and Research (CDER), Guidance for Industry Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System, 2000
  • Custodio J, Wu C, Benet L. Predicting drug disposition, absorption/ elimination/ transporter interplay and the role of food on drug absorption. Adv Drug Deliv Rev 2008;60:717-33
  • Benet L. Predicting drug disposition via application of a biopharmaceutics drug disposition classification system. Basic Clin Pharmacol Toxicol 2010;106:162-7
  • Benet LZ, Broccatelli F, Oprea TI. BDDCS applied to over 900 drugs. AAPS J 2011;13:519-47
  • Benet LZ, Amidon GL, Barends DM, The use of BDDCS in classifying the permeability of marketed drugs. Pharm Res 2008;52:483-8
  • Broccatelli F, Cruciani G, Benet LZ, BDDCS class prediction for new molecular entities. Mol Pharm 2012; published online 7 February 2012; doi:10.1021/mp2004302
  • Takagi T, Ramachandran C, Bermejo M, A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain and Japan. Mol Pharm 2006;3:631-43
  • Chen ML, Yu L. The use of drug metabolism for prediction of intestinal permeability. Mol Pharm 2009;6:74-81
  • Morais JA, Lobato Mdo R. The new European Medicines Agency guideline on the investigation of bioequivalence. Basic Clin Pharmacol Toxicol 2010;106:221-5
  • Marzo A, Fontana E. Critical considerations into the new EMA guideline on bioequivalence. Arzneimittel-Forschung 2011;61:207-20
  • Schellekens H, Klinger E, Muhlebach S, The therapeutic equivalence of complex drugs. Regul Toxicol Pharmacol 2011;59:176-83
  • European Medicines Agency, Evaluation of Medicines for Human Use, CHMP. Guideline on similar biological medicinal products containing biotechnology-derived proteins as active substance: quality issues. London: 2006
  • European Medicines Agency, Evaluation of Medicines for Human Use, CHMP. Guideline on immunogenicity assessment of biotechnology-derived therapeutic proteins. London: 2007
  • European Medicines Agency, Guidance on similar medicinal products containing recombinant erythropoietins. EMEA/CHMP/BMWP/94526/2005, 2006
  • European Medicines Agency, Guideline on similar biological medicinal products containing monoclonal antibodies, Draft guideline. EMA/CHMP/BMWP/403543/2010, 2010
  • Schrempf W, Ziemmsen T. Glatiramer acetate: mechanisms of action in multiple sclerosis. Autoimmune Rev 2007;6:469-75
  • European Medicines Agency, Committee for Medicinal Products for Human Use, CHMP. Reflection paper on non-clinical studies for generic nanoparticle iron medicinal product applications. EMA/CHMP/SWP/100094/2011, 2011
  • Van Gelder T. European Society for Organ Transplantation Advisory Committee: recommendations on generic substitution of immunosuppressive drugs. Transpl Int 2011;24:1135-41
  • European Medicines Agency, Guideline on the use of pharmacogenetic methodologies in the pharmacokinetic evaluation of medicinal products. EMA/CHMP/37646/2009, 2012

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.