The revised 2010 EMA guideline for the Investigation of bioequivalence for immediate release oral formulations with systemic action

Journal of Pharmacy and Pharmaceutical Sciences

Volumn 15, Issue 3, 2012, Pages 376-388

  Verbeeck, Roger K ^a   Musuamba, Flora T ^b  

^a UNIVERSITÉ CATHOLIQUE DE LOUVAIN   (Belgium)

^b RHODES UNIVERSITY   (South Africa)

Author keywords

[No Author keywords available]

Indexed keywords

CLOPIDOGREL; DRUG; DRUG METABOLITE; HIGHLY VARIABLE DRUG; HIGHLY VARIABLE DRUG PRODUCT; MYCOPHENOLIC ACID 2 MORPHOLINOETHYL ESTER; NARROW THERAPEUTIC INDEX DRUG; PARENT DRUG; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; DOSAGE STRENGTH; DRUG ACTIVITY; DRUG APPROVAL; DRUG BLOOD LEVEL; DRUG CONTROL; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG HALF LIFE; DRUG POTENCY; DRUG SCREENING; HUMAN; IMMEDIATE RELEASE FORMULATION; IMMEDIATE RELEASE ORAL DOSAGE FORM; MAXIMUM PLASMA CONCENTRATION; METHODOLOGY; PLASMA CONCENTRATION-TIME CURVE; PRACTICE GUIDELINE; PRODUCT PARAMETERS; RESEARCH SUBJECT; SINGLE DRUG DOSE; STATISTICAL ANALYSIS; STUDY DESIGN; SYSTEMIC ACTION; TIME TO MAXIMUM PLASMA CONCENTRATION; EUROPEAN UNION; METABOLISM; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS; THERAPEUTIC EQUIVALENCE;

ADMINISTRATION, ORAL; EUROPEAN UNION; GUIDELINES AS TOPIC; HUMANS; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; THERAPEUTIC EQUIVALENCY;

EID: 84863422476     PISSN: None     EISSN: 14821826     Source Type: Journal    
DOI: 10.18433/j3vc8j     Document Type: Article

References (70)

1. Nation RL, Sansom LN. Bioequivalence requirements for generic products. Pharmac Ther 1994; 62: 41-55.
2. Midha KK, McKay G. Bioequivalence: its history, practice and future. AAPS J 2009; 11: 664-70.
3. CPMP Note for Guidance on the Investigation of Bioavailability and Bioequivalence, Brussels, December 1991.
4. Pharmacokinetic studies in man, 1987 (http://www.emea.europa.eu/pdfs/human/ewp/3cc3aen.pdf).
5. EMEA Note for Guidance on the Investigation of Bioavailability and Bioequivalence, London, July 26, 2001, CPMP/EWP/QWP/EMEA (http://www.emea.europa.eu/pdfs/human/qwp/140198enfin.pdf).
6. EMEA Recommendation on the Need for Revision of CHMP "Note for Guidance on the Investigation of Bioavailability and Bioequivalence", London, May 2007, EMEA/CHMP/EWP/200943/2007.
7. EMEA Concept Paper on BCS-Biowaiver, EMEA/CHMP/EWP/213035/2007, May 20, 2007 (http://www.emea.europa.eu/pdfs/human/ewp/21303507en.pdf).
8. Verbeeck RK, Warlin J. The European Union, in Kanfer I, Shargel L (eds), Generic Drug Product Development: International Regulatory Requirements for Bioequivalence, Informa Healthcare, New York, NY, pp. 95-113, 2010.
9. EMEA Guideline on the Investigation of Bioequivalence, CPMP/EWP/QWP/1401/98 Rev. 1/Corr **, London, January 20, 2010.
10. EMA Questions & Answers: Positions on specific questions addressed to the Pharmacokinetics Working Party, EMA/618604/2008 Rev. 3, February 16, 2012.
11. EMEA Guideline on Clinical Development of Fixed Combination Medicinal Products, CHMP/EWP/240/95 Rev. 1, February 19, 2009 http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500003686.pdf
12. EMEA Note for Guidance on Modified Release Oral and Transdermal Dosage Forms: Section II (Pharmacokinetic and Clinical Evaluation), CPMP/EWP/280/96Corr * London, July 28,1999, (http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500003126.pdf
13. EMEA Concept Paper on the need for revision of the note for guidance on modified release oral and transdermal dosage forms: section II (pharmacokinetic and clinical evaluation), EMA/CHMP/EWP/1303/2010,May 20, 2010 (http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/06/WC500091662.pdf).
14. FDA Guidance for Industry: Bioequivalence Recommendations for Specific Products, CDER/FDA, Washington, June 2010 (http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm072872.pdf).
15. Hauschke D, Steinijans VW, Diletti E, Burke M. Sample size determination for bioequivalence assessment using a multiplicative model. J Pharmacokinet Biopharm 1992; 20: 557-61.
16. HPFB Guidance for Industry: Conduct and Analysis of Bioavailability and Bioequivalence Studies - Part A: Oral Dosage Formulations, not in Modified used for Systemic Effects, Ottawa, 1992(http://www.hc-sc.gc.ca/dhp-mps/alt_formats/hpfb-dgpsa/pdf/prodpharma/bio-a-eng.pdf).
17. NIHS Japan Guideline for Bioequivalence Studies of Generic Products, December 2006 http://www.nihs.go.jp/drug/be-guide(e)/be2006e.pdf
18. WHO Expert Committee on Specifications for Pharmaceutical Preparations, Annex 7: Multisource (generic) pharmaceutical products -guidelines on registration requirements to establish interchangeability. WHO Technical Report Series No. 937, 2006 (http://www.who.int/medicines/publications/pharmprep/PDF_TRS953_WEB.pdf).
19. Pocock SJ. Group sequential methods in the design and analysis of clinical trials.Biometrika 1977; 64: 191-99.
20. Potvin D, DiLiberti CE, Hauck WW, Parr AF, Schuirmann DJ, Smith RA. Sequential design approaches for bioequivalence studies with crossover designs. Pharmaceut Stat 2008; 7: 245-62.
21. Montague TH, Potvin D, DiLiberti CE, Hauck WW, Parr AF, Schuirmann DJ. Additional results for "Sequential design approaches for bioequivalence studies with crossover designs. Pharmaceut. Stat. 10, published on-line Feb 10, 2011.
22. Common Technical Document for the Registration of Pharmaceuticals for Human Use: Organisation of Common Technical Document, CPMP/ICH/2887/99, London, February 2004.
23. Jackson AJ, Robbie G, Marroum P. Metabolites and bioequivalence: past en present. Clin Pharmacokinet 2004; 43: 655-72.
24. Midha KK, Rawson MJ, Hubbard JW. The role of metabolites in bioequivalence. Pharm Res 2004; 21: 1331-44.
25. Plosker GL, Lyseng-Williamson KA. Clopidogrel - a review of its use in the revention of thrombosis. Drugs 2007; 67: 613-46.
26. Lenz TL, Wilson AF. Clinical pharmacokinetics of antiplatelet agents used in the secondary prevention of stroke. Clin Pharmacokinet 2003; 42: 909-20.
27. Nirogi RV, Kandikere VN, Shukla M, Mudigonda K, Maurya S, Boosi R. Quantification of clopidogrel in human plasma by sensitive liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom 20: 1695-1700.
28. Silvestro L, Gheorghe MC, Tarcomnicu J, Savu S, Savu SR, Iordachescu A, Dulea C.Development and validation of an HPLC-MS/MS method to determine clopidogrel in human plasma: use of incurred samples to test back-conversion. J Chromatogr B 2010; 878: 3134-42.
29. Richter W, Erenmemisoglu A, Van der Meer MJ, Emritte N, Tuncay E, Koytchev R. Bioequivalence study of two different clopidogrel bisulfite film-coated tablets. Arzneim-Forsch/Drug Res 2009; 59: 297-302.
30. El Ahmady O, Ibrahim M, Hussain AM, Bustami RT. Bioequivalence of two oral formulations of clopidogrel tablets in healthy male volunteers. Int J Clin Pharmacol Ther 2009; 47: 780-84.
31. Di Girolamo G, Czerniuk P, Bertuola R, Keller GA. Bioequivalence of two tablet formulations of clopidogrel in healthy Argentinian volunteers: a single-dose, randomized-sequence, open-label crossover study. Clin Ther 2010; 32: 161-70.
32. Staatz CE, Tett SE. Clinical pharmacokinetics and pharmacodynamics of mycophenolate in solid organ transplant recipients. Clin Pharmacokinet 2007; 46:13-58.
33. Guidance on Losartan Potassium, FDA, May 2008 (http://www.fda.gov/Downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm088645.pdf).
34. Schuirmann DJ. A comparison of the two onesided tests procedure and the power approach for assessing the equivalence of average bioavailability. J Pharmacokinet Biopharm 1987; 15: 657-80.
35. Boddy WO, Snikeris FC, Kringle RO, Wei GCG, Oppermann JA, Midha KK. An approach for widening the bioequivalence acceptance limits in the case of highly variable drugs. Pharm Res 1995; 12: 1865-68.
36. Tothfalusi L, Endrenyi L, Midha KK, Rawson MJ, Hubbard JW. Evaluation of bioequivalence of highly-variable drugs and drug products. Pharm Res 2001; 18:728-33.
37. Haidar SH, Davit B, Chen M-L, Conner D, Lee LM, Li QH, Lionberger R, Makhlouf F, Patel D, Schuirmann DJ, Yu LX. Bioequivalence approaches for highly variable drugs and drug products. Pharm Res 2008; 25: 237-41.
38. Tothfalusi L, Endrenyi L, Garcia Arieta A. Evaluation of bioequivalence for highly variable drugs with scaled average bioequivalence. Clin Pharmacokinet 2009; 48: 725-43.
39. Blume H, Midha KK. Bio-international'92, conference on bioavailability, bioequivalence and pharmacokinetic studies: Bad Homburg, Germany, 20-22, May 1992. Eur J Pharm Sci 1993; 1: 165-71.
40. Davit BM, Conner DP, Fabian-Fritsch B, Haidar S, Jiang X, Patel DT, Seo PRH, Suh K, Thompson CL, Yu LX. Highly variable drugs: observations from bioequivalence data submitted to the FDA for new generic drug applications. AAPS J 2008; 10: 148-56.
41. Midha KK, Rawson MJ, Hubbard JW. The bioequivalence of highly variable drugs and drug products. Int J Clin Pharmacol Ther 2005; 43: 485-98.
42. Tsang YC, Pop R, Gordon P, Hems J, Spino M. High variability in drug pharmacokinetics complicates determination of bioequivalence: experience with verapamil. Pharm Res 1996; 13: 846-50.
43. Shah VP, Yacobi A, Barr WH, Benet LZ, Breimer D, Dobrinska MR, Endrenyi L, Fairweather W, Gillespie W, Gonzales MA, Hooper J, Jackson A, Lesko LJ, Midha KK, Noonan PK, Pataik R, Williams RL. Evaluation of orally administered highly variable drugs and drug formulations. Pharm.Res 1996; 13:1590-94.
44. FDA Draft Guidance on Progesterone, February 2011(http://www.fda.gov/downloads/drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM209294.pdf).
45. Tothfalusi L, Endrenyi L. Sample sizes for designing bioequivalence studies for highly variable drugs. J Pharm Pharmaceut Sci 2012; 15: 73-84.
46. 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 2012; 29: 1066-77.
47. Benet LZ, Goyan JE. Bioequivalence and narrow therapeutic index drugs. Pharmacotherapy 1995; 15: 433-40.
48. Levy G. What are narrow therapeutic index drugs? Clin Pharmacol Ther 1998; 63: 501-05.
49. Danish Health and Medicines Authority: Bioequivalence and labelling of medicinal Products with regard to generic substitution, February 07, 2012 (http://laegemiddelstyrelsen.dk/en/topics/authorisa tion-and-supervision/licensing-of-medicines/marketing-authorisation/application-for-marketing-authorisation/bioequivalence-and-labelling-of-medicine--bstitution).
50. Danish Health and Medicines Authority: Generic substitution terminated for oral medicines containing cyclosporine or tacrolimus, July 13, 2011(http://laegemiddelstyrelsen.dk/en/topics/authorisation-and-supervision/licensing-of-medicines/news/generic-substitution-terminated-for-oral--tacrolimus).
51. Belgian Federal Agency for Medicines and Health Products: International Non-Proprietary Name (INN) Prescription, December 09, 2011.
52. Benet LZ. Relevance of pharmacokinetics in narrow therapeutic index drugs. Transplant Proc 1999; 31: 1642-44.
53. Kesselheim AS, Misono AS, Lee JL, Stedman MR, Brookhart MA, Choudhry NK, Shrank WH. Clinical equivalence of generic and brand-name drugs used in cardiovascular disease. J Am Med Assoc 2008; 300: 2514-26.
54. Verbeeck RK. Bioequivalence, therapeutic equivalence and generic drugs. Acta Clin Belg 2009; 64: 379-83.
55. Gagne JJ, Avorn J, Shrank WH, Schneeweiss S. Refilling and switching of antiepileptic drugs and seizure-related events. Cin Pharmacol Ther 2010; 88:347-53.
56. Moore N, Berdaï D, Bégaud B. Are generic drugs really inferior medicines? Clin Pharmacol Ther 2010; 88: 302-04.
57. HPFB Guidance for Industry: Bioequivalence requirements: critical dose drugs, Ottawa, May 31, 2006(http://www.hc-sc.gc.ca/dhp-mps/alt_formats/pdf/prodpharma/applic-demande/guide-ld/bio/critical_dose_critique-eng.pdf).
58. FDA Guidance for Industry: Bioavailability and Bioequivalence Studies for Orally Administered Drug Products - General Considerations, CDER/FDA, Washington, March 2003 (http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070124.pdf).
59. Williams RL. Therapeutic equivalence of generic drugs - Response to National Association of Boards of Pharmacy, Center for Drug Evaluation and Research, FDA, 1997 (www.fda.gov/cder/news.ntiletter.htm).
60. FDA Meeting of the Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Topic 1: Revising the Bioequivalence (BE) Approaches for Critical Dose Drugs, April 13, 2010 (http://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/AdvisoryCommitteeforPharmaceutical-ScienceandClinicalPharmacology/UCM207955.pdf).
61. FDA ACPS-CP Meeting: Bioequivalence and Quality Standards for Narrow Therapeutic Index Drug Products, July 26, 2011 (http://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/AdvisoryCommitteeforPharmaceuticalScienceandClinicalPharmacology/UCM263465.pdf).
62. Bialer M, Midha KK. Generic products of anti-epileptic drugs: a perspective on bioequivalence and interchangeability. Epilepsia 2010; 51: 941-50.
63. Amidon GL, Lennernas H, Shah VP, Crison JR. 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.
64. FDA Guidance for Industry: Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System, CDER/FDA, Washington, August 2000 (http://www.fda.gov/cder/guidance/index.htm).
65. Blume HH, Schug BS. The biopharmaceutics classification system (BCS): class III drugs - better candidates for BA/BE waiver? Eur J Pharm Sci 1999; 9:117-21.
66. Yu LX, Amidon GL, Polli JE, Zhao H, Mehta MU, Conner DP, Shah VP, Lesko LJ, Chen M-L, Lee VHL, Hussain AS. Biopharmaceutics classification system: the scientific basis for biowaiver extensions. Pharm Res 2002; 19: 921-25.
67. Polli JE, Yu LX, Cook JA et al. Summary workshop report: Biopharmaceutics Classification System - implementation challenges and extension opportunities. J Pharm Sci 2004; 93: 1375-81.
68. Jantratid E, Prakongpan S, Amidon GL, Dressman JB. Feasibility of biowaiver extension to biopharmaceutics classification system III drug products-cimetidine. Clin Pharmacokinet 2006; 45: 385-99.
69. Wu C-Y, 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.
70. WHO Expert Committee on Specifications for Pharmaceutical Preparations, Annex 8: Proposal to waive in vivo bioequivalence requirements for WHO Model List of Essential Medicines immediate-release, solid oral dosage forms. WHO Technical Report Series No. 937, 2006 (http://www.who.int/medicines/publications/phar mprep/PDF_TRS953_WEB.pdf).