Report an error   


Submitted: 24 May 2008 Modified: 06 September 2012
HERDIN Record #: PCHRD052408030525

The relative bioavailability of a generic felodipine 5mg tablet with the innovator brand 5mg tablet.

See More

OBJECTIVES: The study was conducted to compare the bioavailability of a local generic felodipine formulation with the innovator felodipine in healthy Filipino males aged 18 to 45 years. In addition, the Study also determined and compared the safety profile of each drug as evidenced by adverse events.

METHODS: This study had a randomized, open-labeled treatment, blind-endpoint analysis, two-formulation, two-period, two-sequence, non-replicated, crossover design with single drug dose administrations In the fasting condition and 1 week wash-out period.

RESULTS: The Cra>x of the innovator brand (5.77 nmol/L i 3.19) was" greater than the Cmail of the generic felodipine (3.27 nmol/L +/- 1.70). The Tmax of the innovator brand (5.47 hours +/- 3.70) was longer than the TmlJ of the generic felodipine (4.80 hours +/- 2.55). A(IC024 and ACIC0.]>st showed that plasma levels of felodipine were consistently higher for the innovator brand compared to generic felodipine. The 90 percent confidence limits of the ratios of the AGC's of the generic felodipine to innovator brand were not completely outside the prescribed limits of 80 to 125 percent needed to establish bioequivalence. Similarly, the 90 percent confidence limits of the ratio of the Cmax of the generic felopdipine to the innovator brand were outside the 80 to 125 percent window.

CONCLUSION: The study showed that the bioavailability of the generic felodipine is statistically different from the bioavailability of the innovator brand. The adverse events reported were minor and were known adverse effects of the drug. (Author)

Objectives

The study was conducted to compare the bioavailability of a local generic felodipine formulation with the innovator felodipine in healthy Filipino males aged 18 to 45 years. In addition, the Study also determined and compared the safety profile of each drug as evidenced by adverse events.

LocationLocation CodeAvailable FormatAvailability
Philippine Council for Health Research and Development Library Box No 48 Fulltext Print Format (Request Document)
1. Saltiel, E , Ellrodt, A G, Monk, J P, Langley, M S. "Felodipine: A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension" Drugs 36, 387, 1988
2. Todd, P A, Faulds, D . "Felodipine: A review od the pharmacology and therapeutic use of the extended release formulation in cardiovascular disorders" Drugs 44(2): 251, 1992
3. Welin, L , Elvelin, L , Niklasson, A , et al, . "Overview of the safety of felodipine based on clinical trials in patients with hypertension" American Journal Cardiology 79(7): 996, April 1997
4. Faulds, D , Sorkin, E M. "Felodipine. A review of the pharmacology and therapeutic use of the extended release formulation in older patients" Drugs Aging 2(5): 374, October 1992
5. Trachtman, H , Frank, R , Mahan, J D, et al, . "Clinical trial of extended-release felodipine in pediatric essential hypertension" Pediatric Nephrology 18(6): 548, June 2003
6. Woo, B Y, Yeoh, T K, Tan, A T. "Felodipine as monotherapy in Asian patients with mild to moderate hypertension" Annals Academy of Medicine Singapore 19(1): 64, January 1990
7. Kon, S P, Tan, H W, Chua, C T, et al, . "Once daily felodipine monotherapy in mild to moderate hypertension" Medical Journal Malaysia 47(4): 290, December 1992
8. Cheung, B M, Lau, C P, Wu, B Z. "Amlodipine, felodipine, and isradipine in the treatment of Chinese patients with mild-to-moderate hypertension" Clinical Therapeutics 20(6): 1159, December 1998
9. Gradman, A H. "Treatment of hypertension with felodipine in patients with concomitant diseases" Clinical Cardiology 16(4): 294, April 1993
10. Reuter, M K, Lorenz, H , Verho, P , et al, . "Effects of felodipine ER. a dihydropyridine calcium antagonist, on blood pressure and serum lipids" Current Medical Research and Opinion 14(2): 97, 1998
11. Weber, M A, Goldberg, A L, Faison, E P, et al, . "Extended-release felodipine in patients with mild to moderate hypertension" Clinical Pharmacology Therapeutics 55, 346, March 1994
12. Blychert, E , Edgar, B , Elmfeldt, D , Hedner, T . "Plasma concentration- effect relationship for felodipine: A meta analysis" Clinical Pharmacology Therapeutics 52(1): 80, July 1992
13. Ekelund, L G, Ulvenstam, G , Walldius, G , Aberg, A . "Effects of felodipine versus nifedipine on exercise tolerance in stable angina pectoris" American Journal Cardiology 73(9): 658, April 1994
14. Gradman, A H. "The evolving role of calcium channel blockers in the treatment of angina pectoris: Focus on felodipine" Canadian Journal Cardiology 11(Suppl. B): 14B - 21B, April 1995
15. Brun, J , Froberg, L , Kronmann, P , et al, . "Optimal felodipine dose when combined with metoprolol in arterial hypertension: A Swedish multicenter study within primary health care. Swedish General Practitioner Felodipine study Group" Journal Cardiovascular Pharmacology 15(Suppl 4): S60 , 1990
16. Bailey, D G, Bend, J R, Arnold, J M, et al, . "Erythromycin-felodipine interactiond: Magnitude, mechanism, and comparison with grapefruit juice" Clinical Pharmacology Therapeutics 60(1): 25, July 1996
17. Bailey, D G, Dresser, G K, Kreeft, J H, et al, . "Grapefruit-felodipine interaction: Effect of unprocessed fruit and probable active ingredients" Clinical Pharmacology Therapeutics 68(5): 468, November 2000
18. Capewell, S , Freestone, S , Critchley, J A, et al, . "Reduced felodipine bioavailability in patients taking anticonvulsants" Lancet 2(8609): 480, August 1988
19. Food and Drug Administration (FDA): Guidance for Industry Statistical Approaches to Establishing Bioequivalence 2001.
20. Guidance for Industry: Bioavailability and Bioequivalence Studies for Orally Administered Drug Products-General Considerations 2003.