Open questions on bioequivalence: Some problems and some solutions

Pharmacological Research

Volumn 40, Issue 4, 1999, Pages 357-368

  Marzo, A ^a  

^a IPAS SA   (Switzerland)

Author keywords

Bioequivalence; Endogenous substances; EU guidelines; FDA guidelines; Study design

Indexed keywords

CARNITINE; FOLIC ACID; MAGNESIUM ASPARTATE; MORPHINE 6 GLUCURONIDE; MORPHINE SULFATE; POTASSIUM SALT; THYROXINE;

AREA UNDER THE CURVE; BIOASSAY; BIOEQUIVALENCE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG FORMULATION; DRUG HALF LIFE; HUMAN; HUMAN EXPERIMENT; METABOLITE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS; PRACTICE GUIDELINE; PRIORITY JOURNAL; REVIEW; SCIENTIFIC LITERATURE; STATISTICAL ANALYSIS; SUBLINGUAL DRUG ADMINISTRATION; SUSTAINED RELEASE FORMULATION;

EID: 0032825293     PISSN: 10436618     EISSN: None     Source Type: Journal    
DOI: 10.1006/phrs.1999.0528     Document Type: Article

References (66)

1. CPMP working party on efficacy of medicinal products, 1991, The Regulatory Affairs Journal; Volume III; Addendum 2, 1992.
2. CPMP working party on efficacy of medicinal products. 1998.
3. In vivo bioequivalence guida nces. General Information. United States Pharmacopoeia XXIII. 1998;4382-4426.
4. Marzo A. Clinical pharmacokinetic registration file for NDA and ANDA procedures. Pharmacol Res. 36:1997;425-450.
5. Marzo A, Balant L P. The bioequivalence: an updated reappraisal addressed to applications of interchangeable multi-source pharmaceutical products. Arzneim Forsch. 45:1995;109-115.
6. Patniak R N, Lesko L J, Chen M L, Williams R L. Individual bioequivalence. Clin Pharmacokinet. 33:1997;1-6.
7. Marzo A. Open questions in bioequivalence. Pharmacol Res. 32:1995;237-240.
8. Marzo A. Toxicokinetics of endogenous substances: a neglected issue. Arzneim Forsch. 46:1996;1-10.
9. Marzo A, Rescigno A, Arrigoni Martelli E. Some pharmacokinetic considerations about homeostatic equilibrium of endogenous substances. Eur J Drug Metab Pharmacokinet. 18:1993;215-219.
10. Marzo A, Rescigno A. Pharmacokinetics of endogenous substances: some problems and some solutions. Eur J Drug Metab Pharmacokinet. 18:1993;77-88.
11. Cerutti R, Rivolta G, Di Giulio C, Cavalieri L, Grossi E, Vago T, Boldi G, Righini V, Marzo A. Bioequivalence of levothyroxine tablets administered in target population in steady state. Pharmacol Res. 39:1999;193-201.
12. Radwanski E, Perentesis G, Symchowicz S, Zampaglione N. Single and multiple dose pharmacokinetic evaluation of flutamide in normal geriatric volunteers. J Clin Pharmacol. 29:1989;554-558.
13. Schulz M, Schmoldt A, Donn F, Becker H. The pharmacokinetics of flutamide and its major metabolites after a single oral dose and during chronic treatment. Eur J Clin Pharmacol. 34:1988;633-636.
14. Clin Invest. 71:1993;240-246.
15. Garteiz D A, Hook R H, Walker B J, Okerholm R A. Pharmacokinetics and biotransformation studies of terfenadine in man. Arzneim Forsch. 32:1982;1185-1190.
16. Bochner F, Lloyd J V. Aspirine for myocardial infarction. Clin Pharmacokinet. 28:1995;433-438.
17. Marzo A, Mancinelli A, Cardace G, Monti N, Arrigoni Martelli E. NaF and two other esterase inhibitors unaffect acetyl salicylic acid enzyme hydrolysis. J Pharm Pharmacol. 44:1992;768.
18. Osborne R, Joel S, Trew D, Slevin M. Morphine and metabolite behaviour after different routes of morphine administration: demonstration of the importance of the active metabolite morphine-6-glucuronide. Clin Pharmacol Ther. 47:1990;12-19.
19. Osborne R, Thompson P, Joel S, Threw D, Patel N, Slevin M. The analgesic activity of morphine-6-glucuronide. Br J Clin Pharmacol. 34:1992;130-138.
20. Paul D, Standifer K M, Inturrisi C E, Pasternak G W. Pharmacological characterization of morphine 6β-glucuronide, a very potent morphine metabolite. J Pharmacol Exp Ther. 251:1989;477-483.
21. Smith M T, Watt J A, Cramond T. Morphine-3-glucuronide. Life Sci. 47:1990;579-585.
22. Bergstrom R F, Lemberger L, Cerimiele B J, Wolen R L, Kisicki J C. Relative bioequivalence of a fluoxetine oral solution versus the marketed capsule. Pharm Res. 1990.
23. Lemberger L, Bergstrom R F, Wolen R L, Farid N A, Enas C G, Aronoff G R. Fluoxetine: clinical pharmacology and physiologic disposition. J Clin Psychiatry. 1985;14-19.
24. Yacatan G J, Poynor W J, Talbert R L, Floyd B F, Slough C L, Ampulski R S, Benedict J J. Clodronate kinetics and bioavailability. Clin Pharmacol Ther. 31:1982;401-410.
25. Bendetowicz A V, Béguin S, Caplain H, Hemker H C. Pharmacokinetics and pharmacodynamics of a low molecular weight heparin (enoxaparin) after subcutaneous injection, comparison with unfractionated heparin. Thromb Haemost. 71:1994;305-313.
26. Iacobelli M, Clerici G, Marzo A, Dal Bo L. A comparative bioavailability study of two formulations of calcium heparin. Int Med. 6:1998;39-44.
27. Steinijans V W, Hauschke D, Jonkman J HG. Controversies in bioequivalence studies. Clin Pharmacokinet. 22:1992;247-253.
28. Grahnén A. The biopharmaceutical classification system. Eur J Pharm Sci. 1998.
29. Eur J Pharm Sci. 7:1998;1-3.
30. Lennernas H. Human intestinal permeability. J Pharm Sci. 87:1998;403-410.
31. Lennermes H. Human jejunal effective permeability and its correlation with preclinical drug absorption models. J Pharm Pharmacol. 49:1997;627-638.
32. Runkel R, Chaplin M D, Sevelins H, Ortega E, Segre E. Pharmacokinetics of naproxen overdoses. Clin Pharmacol Ther. 20:1976;269-277.
33. Marzo A. Cross-over design in tamoxifen bioequivalence: a borderline situation. J Pharm Pharmacol. 50:1998;1433-1434.
34. Chen M L, Pelsor F R. Half-life revisited: implication in clinical trials and bioavailability/bioequivalence evaluation. J Pharm Sci. 80:1991;406-408.
35. Urso R, Aarons L. Bioavailability of drugs with long elimination half-lives. Eur J Clin Pharmacol. 25:1983;689-693.
36. Rescigno A. Bioequivalence. Pharm Res. 9:1992;925-928.
37. Rescigno A, Marzo A, Thyroff-Friesinger V. Mefenamic acid bioequivalence assessment with a new statistical procedure. Pharmacol Res. 33:1996;149-152.
38. Karim A. Transdermal absorption: a unique opportunity for constant delivery of nitroglycerin. Drug Dev Ind Pharm. 9:1983;671-689.
39. Müller P, Botta L, Ezzet F. Bioavailability of estradiol from a new matrix and a conventional reservoir-type transdermal therapeutic system. Eur J Clin Pharmacol. 51:1996;327-330.
40. Berner B, John V. Pharmacokinetic characterisation of transdermal delivery systems. Clin Pharmacokinet. 26:1994;121-134.
41. Shoenwald R D. Ocular drug delivery. Clin Pharmacokinet. 18:1980;255-269.
42. Juhlin L, Hägglund G, Evers H. Absorption of lidocaine and prilocaine after application of a eutectic mixture of local anaesthetics on the normal and diseased skin. Acta Derm Venereol. 69:1989;18-22.
43. Leier C V, Baker N D, Weber P A. Cardiovascular effects of ophthalmic timolol. Ann Int Med. 104:1986;197-199.
44. Rowbotham M C, Davies P S, Fields H L. Topical lidocaine gel relieves postherpetic neuralgia. Ann Neurol. 37:1995;246-253.
45. Sengupta S, Velpandian T, Kabir S R, Gupta S K. Analgesic efficacy and pharmacokinetics of topical nimesulide gel in healthy human volunteers: double-blind comparison with piroxicam, diclofenac and placebo. Eur Clin Pharmacol. 54:1998;541-547.
46. Shah V P, Flynn G L, Yacobi A, Maibach H I, Bon C, Fleischer N M, Franz T J, Kaplan S A, Kawamoto J, Lesko L J, Marty J P, Pershing L K, Schaefer H, Sequeira J A, Shrivestava S P, Wilkin J, Williams R L. Bioequivalence of topical dermatological dosage forms. Pharm Res. 15:1998;167-171.
47. Müller M, Mascher H, Kikuta C, Schäfer S, Brunner M, Dorner G, Eichler M. Diclofenac concentrations in defined tissue layers after topical administration. Clin Pharmacol Ther. 62:1997;293-299.
48. CPMP working party on safety of medicinal products, 1994, The Regulatory Affairs Journal; Volume III; Addendum 3, 1995.
49. Mehvar R, Jamali F. Bioequivalence of chiral drugs. Clin Pharmacokinet. 33:1997;122-141.
50. Marzo A. Incoming guidelines on chirality: a challenge for pharmacokinetics in drug development. Arzneim Forsch. 44:1994;791-793.
51. Marzo A, Balant L P. Investigation of xenobiotic metabolism by CYP2D6 and CYP2C19: importance of enantioselective analytical methods. J Chromatogr B. 678:1996;73-92.
52. Frye R F, Matzke G R, Adedoyin A, Porter J A, Branch R A. Validation of the five-drug 'Pittsburg cocktail' approach for assessment of selective regulation of drug-metabolizing enzymes. Clin Pharmacol Ther. 39:1997;365-376.
53. Bennet W M, Pulliam J P. Cyclosporine nephrotoxicity. Ann Int Med. 99:1983;851-854.
54. Bertilsson L, Torbjörn T. Clinical pharmacokinetics and pharmacological effects of carbamazepine and carbamazepine-10,11-epoxide. Clin Pharmacokinet. 11:1986;177-198.
55. Wingard L B, O'Reilly R A, Levy G. Pharmacokinetics of warfarin enantiomers: a search for intrasubject correlations. Clin Pharmacol Ther. 23:1978;212-217.
56. Hignite C, Uetrecht J, Tschanz C, Azarnoff D. Kinetics of R and S warfarin enantiomers. Clin Pharmacol Ther. 28:1980;99-105.
57. Palareti G, Legnani C. Warfarin withdrawal. Clin Pharmacokinet. 30:1996;300-313.
58. Grizzle J E. The two-period change-over desing and its use in clinical trials. Senn S,. Cross-over trials in clinical research. 1993;467-480 John Wiley, New York:
59. Marzo A. Pharmacokinetic analysis, bioavailability and operating guidelines. J Pharm Pharmacol. 49:1997;1259-1260.
60. Marzo A, Ceppi Monti N. Acceptable and unacceptable procedures in bioavailability and bioequivalence trials. Pharmacol Res. 38:1998;401-404.
61. Diletti E, Hauschke D, Steinijans V W. Sample size determination: extended tables for the multiplicative model and bioequivalence ranges of 0.9 to 1.11 and 0.7 to 1.43. Int J Clin Pharmacol Ther Toxicol. 30:1992;59-62.
62. Steinijans V W, Hauschke D. International harmonization of regulatory bioequivalence requirements. Clin Res Reg Affairs. 10:1993;203-220.
63. Boddy A W, Snikeris F C, Kringle R O, Wei G CG, Oppermann J A, Midha K K. An approach for widening the bioequivalence acceptance limits in the case of high variability drugs. Pharm Res. 12:1995;1865-1868.
64. Latini R, Tognoni G, Kates R E. Clinical pharmacokinetics of amiodarone. Clin Pharmacokinet. 9:1984;136-156.
65. Mooradian A D. Digitalis: an update of clinical pharmacokinetics, therapeutic monitoring techniques and treatment recommendations. Clin Pharmacokinet. 15:1988;165-179.
66. White N J. Clinical pharmacokinetics of antimalarial drugs. Clin Pharmacokinet. 10:1985;187-215.