Single-dose, Two-way Crossover, Bioequivalence Study of Mycophenolate Mofetil 500 mg Tablet Under Fasting Conditions in Healthy Male Subjects

Clinical Therapeutics

Volumn 33, Issue 3, 2011, Pages 378-390

  Patel, Shashank ^a   Chauhan, Vijay ^a   Mandal, Jayanta ^a   Shah, Samir ^a   Patel, Keyur ^a   Saptarshi, Dipak ^a   Maheshwari, Kirti ^a   Jha, Pankaj Kumar ^b   Kale, Prashant ^b   Patel, Kamlesh ^b   Mathew, Philip ^b  

^a Astron Research Limited   (India)

^b Lambda Therapeutic Research Limited   (India)

Author keywords

AUC; Bioequivalence; Dissolution; Mycophenolate mofetil; Mycophenolic acid; Pharmacokinetic

Indexed keywords

MYCOPHENOLIC ACID; MYCOPHENOLIC ACID 2 MORPHOLINOETHYL ESTER;

ADULT; ANALYSIS OF VARIANCE; AREA UNDER THE CURVE; BIOEQUIVALENCE; CONFIDENCE INTERVAL; CONTROLLED STUDY; COUGHING; CROSSOVER PROCEDURE; DIET RESTRICTION; DOG BITE; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG SOLUBILITY; DRUG WITHDRAWAL; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; LEUKOCYTOSIS; LIQUID CHROMATOGRAPHY; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PH; RANDOMIZED CONTROLLED TRIAL; REVIEW; SINGLE DRUG DOSE; TANDEM MASS SPECTROMETRY;

ADMINISTRATION, ORAL; ADOLESCENT; ADULT; CHEMISTRY, PHARMACEUTICAL; CROSS-OVER STUDIES; FASTING; HUMANS; IMMUNOSUPPRESSIVE AGENTS; MALE; MIDDLE AGED; MYCOPHENOLIC ACID; SOLUBILITY; TABLETS; YOUNG ADULT;

EID: 79956003293     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2011.04.003     Document Type: Review

References (37)

1. Speich R., Schneider S., Hofer M., et al. Mycophenolate mofetil reduces alveolar inflammation, acute rejection and graft loss due to bronchiolitis obliterans syndrome after lung transplantation. Pulm Pharmacol Ther 2010, 23:445-449.
2. Heilman R.L., Mazur M.J., Reddy K.S. Immunosuppression in simultaneous pancreas-kidney transplantation: progress to date. Drugs 2010, 70:793-804.
3. Allison A.C., Eugui E.M. Mycophenolate mofetil and its mechanisms of action. Immunopharmacology 2000, 47:85-118.
4. Staatz C.E., Tett S.E. Clinical pharmacokinetics and pharmacodynamics of mycophenolate in solid organ transplant recipients. Clin Pharmacokinet 2007, 46:13-58.
5. Villarroel M.C., Hidalgo M., Jimeno A. Mycophenolate mofetil: an update. Drugs Today (Barc) 2009, 45:521-532.
6. Golshayan D., Pascual M., Vogt B. Mycophenolic acid formulations in adult renal transplantation-update on efficacy and tolerability. Ther Clin Risk Manag 2009, 5:341-351.
7. ® SmPC Roche Products Ltd, Accessed November 25, 2010. http://www.medicines.org.uk/EMC/medicine/1680/SPC/Cellcept+500mg+Tablets/.
8. CellCept: EPAR-Product Information European Medicines Agency, Accessed December 21, 2010. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000082/WC500021864.pdf.
9. European Public Assessment Report: Mycophenolate Mofetil, Cellcept European Medicines Agency, Accessed November 20, 2010. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/000882/WC500031271.pdf.
10. CHMP Assessment report: Myclausen European Medicines Agency, Accessed November 25, 2010. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/001218/WC500097856.pdf.
11. European Public Assessment Report: Mycophenolate Mofetil, Teva European Medicines Agency, Accessed November 25, 2010. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/000882/WC500031271.pdf.
12. CHMP Guideline on the Investigation of Bioequivalence European Medicines Agency, Accessed December 21, 2010. http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/01/WC500070039.pdf.
13. Public Assessment Report: Mycophenolate Mofetil Sandoz 250mg Capsules, Hard-UK/H/0886/001/DC; PL 04416/0712. October 15, 2007 Medicines and Healthcare Products Regulatory Agency, Accessed April 4, 2011. http://www.mhra.gov.uk/home/groups/l-unit1/documents/websiteresources/con2032733.pdf.
14. Public Assessment Report: Mycophenolate Lek 250mg Capsules (Mycophenolate mofetil)-UK/H/1037/001/DC; PL 16220/0005. October 8, 2008 Medicines and Healthcare Products Regulatory Agency, Accessed April 4, 2011. http://www.mhra.gov.uk/home/groups/l-unit1/documents/websiteresources/con028288.pdf.
15. Public Assessment Report: Mycophenolate Mofetil 500mg Film Coated Tablets-UK/H/1055/001/DC; PL 20075/0001. Feb 4, 2009 Medicines and Healthcare Products Regulatory Agency, Accessed April 4, 2011. http://www.mhra.gov.uk/home/groups/pl-p/documents/websiteresources/con038637.pdf.
16. Public Assessment Report: Mycophenolate mofetil 500mg Film-Coated Tablets - UK/H/1922/001/DC; PL 08553/0359 Medicines and Healthcare Products Regulatory Agency, Accessed January 20, 2011. http://www.mhra.gov.uk/home/groups/par/documents/websiteresources/con065527.pdf.
17. ICH Topic E 6 (R1) Guideline for Good Clinical Practice European Medicines Agency, Accessed November 25, 2010. http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002874.pdf.
18. Guidance for Industry: Bioanalytical Method Validation US Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER), and Center for Veterinary Medicine (CVM), Accessed November 25, 2010. http://www.fda.gov/downloads/Drugs/Guidance%20ComplianceRegulatoryInformation/Guidances/UCM070107.pdf.
19. US Pharmacopeia (USP), Accessed November 26, 2010. http://www.usp.org/aboutUSP/.
20. Yu L.X., Amidon G.L., Polli J.E., et al. Biopharmaceutics classification system: the scientific basis for biowaiver extensions. Pharm Res 2002, 19:921-925.
21. Emami J. In vitro-in vivo correlation: from theory to applications. J Pharm Pharm Sci 2006, 9:169-189.
22. Schuebel E, Adamy L. In vitro dissolution of mycophenolate mofetil: comparison between innovator and generic formulations. Proceedings of the British Pharmacological Society 2008. 2008. http://www.pa2online.org/abstracts/Vol6Issue4abst118P.pdf.
23. Almeida S., Filipe A., Neves R., et al. Mycophenolate mofetil 500-mg tablet under fasting conditions: single-dose, randomized-sequence, open-label, four-way replicate crossover, bioequivalence study in healthy subjects. Clin Ther 2010, 32:556-574.
24. Estevez-Carrizo F.E., Parrillo S., Cedres M., et al. Comparative bioavailability of two oral formulations of mycophenolate mofetil in healthy adult Uruguayan subjects: a case of highly variable rate of drug absorption. Int J Clin Pharmacol Ther 2010, 48:621-627.
25. Masri M.A., Rizk S., Attia M.L., et al. Bioavailability of a new generic formulation of mycophenolate mofetil MMF 500 versus CellCept in healthy adult volunteers. Transplant Proc 2007, 39:1233-1236.
26. Zhang Q., Tao Y., Zhu Y., Zhu D. Bioequivalence and pharmacokinetic comparison of two mycophenolate mofetil formulations in healthy Chinese male volunteers: an open-label, randomized-sequence, single-dose, two-way crossover study. Clin Ther 2010, 32:171-178.
27. Spínola AC, Almeida S, Filipe A, et al. Highly variable drugs and highly variable drug products. Briefing on regulatory and scientific perspectives. EUFEPS BABP Network Open Discussion: Revised European Guidelines on Bioequivalence. Bonn, Germany. January 14-15, 2009.
28. Mueller E.A., Kovarik J.M., van Bree J.B., et al. Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharm Res 1994, 11:301-304.
29. Cooney G.F., Fiel S.B., Shaw L.M., Cavarrochi N.C. Cyclosporine bioavailability in heart-lung transplant candidates with cystic fibrosis. Transplantation 1990, 49:821-823.
30. Kovarik J.M., Mueller E.A., van Bree J.B., et al. Cyclosporine pharmacokinetics and variability from a microemulsion formulation-a multicenter investigation in kidney transplant patients. Transplantation 1994, 58:658-663.
31. Dunn S., Cooney G., Sommerauer J., et al. Pharmacokinetics of an oral solution of the microemulsion formulation of cyclosporine in maintenance pediatric liver transplant recipients. Transplantation 1997, 63:1762-1767.
32. Lindholm A., Welsh M., Rutzky L., Kahan B.D. The adverse impact of high cyclosporine. Clearance rates on the incidences of acute rejection and graft loss. Transplantation 1993, 55:985-993.
33. Schroeder T.J., Hariharan S., First M.R. Variations in bioavailability of cyclosporine and relationship to clinical outcome in renal transplant subpopulations. Transplant Proc 1995, 27:837-839.
34. Tan K.K., Hue K.L., Strickland S.E., et al. Altered pharmacokinetics of cyclosporin in heart-lung transplant recipients with cystic fibrosis. Ther Drug Monit 1990, 12:520-524.
35. Armstrong V.W., Tenderich G., Shipkova M., et al. Pharmacokinetics and bioavailability of mycophenolic acid after intravenous administration and oral administration of mycophenolate mofetil to heart transplant recipients. Ther Drug Monit 2005, 27:315-321.
36. Brunet M., Martorell J., Oppenheimer F., et al. Pharmacokinetics and pharmacodynamics of mycophenolic acid in stable renal transplant recipients treated with low doses of mycophenolate mofetil. Transpl Int 2000, 13(Suppl 1):S301-S305.
37. Bullingham R., Monroe S., Nicholls A., Hale M. Pharmacokinetics and bioavailability of mycophenolate mofetil in healthy subjects after single-dose oral and intravenous administration. J Clin Pharmacol 1996, 36:315-324.