Ángeles UJ, Benjamín Nájera IB

Language: Spanish
References: 24
Page: 51-56
PDF size: 82.82 Kb.

ABSTRACT

The Bioavailability of two oral preparations of Lisinopril, Alfaken® and Prinivil®, was assessed and compared in 24 healthy male volunteers, being the latter product the one designated by Mexican Health Authorities as the Reference Drug Product. Both products successfully met the requirements of the Norma Oficial Mexicana (Mexican Official Standards) NOM-177-SSA-1-1998. Based on a single dose, randomized, two-way crossover design, volunteers received a 20-mg dose (two 10-mg tablets) of each study drug for two periods with a washout of two weeks (14 days) between each period in order to eliminate the drug taken in the previous period. Aimed at withdrawing blood samples in order to assess the pharmacokinetic profile for the study and reference drug products, a catheter was introduced in the forearm vein. Blood samples were obtained before the drug product administration (time zero) and at 0.5, 1, 2, 4, 6, 7, 8, 12, 24, 36, 72, 96, 120, and 144 hours after the dose. Lisinopril plasma concentration was determined by means of a validated reliable LC-MS analytical method. Results showed that the method successfully met the accuracy and linearity requirements for lisinopril within a concentration range between 3 and 280 ng/mL. The Bioavailability parameters were calculated for both products plasma profile data with noncompartimental methods by using statistical software WinNonlin v 3.3. Results obtained for Alfaken® and Prinivil® respectively are the following: AUC_0-t (1,087.4 ± 428.3 and 1,120.2 ± 433.1 ng h/mL), AUC_0-∞ (1,136.8 ± 423.6 and 1,169.0 ± 433.4 ng h/mL), C_max (90.0 ± 43.3 and 90.8 ± 36.3 ng/mL), T_max (7.1 ± 0.63 and 6.6 ± 1.4 h), t½ (6.9 ± 1.8 and 6.9 ± 1.7 h), Ke (0.11 ± 0.02 and 0.11 ± 0.02 h-1), MRT (11.9 ± 1.6 and 11.8 ± 1.7 h). Bioequivalent statistics showed that AUC and Cmax log parameters met the bioequivalence criteria of Two one-sided t-test: p ‹ 80% (p ≤ 0.05); p › 125% (p ≤ 0.05), 90% Confidence Interval (80-125%) and Power (p › 0.80). The comparison of the above results permitted to attain the conclusion that both products are bioequivalent.

REFERENCES

1. Wong YC, Charles BG. Determination of the Angiotensin-Converting Enzyme Inhibitor Lisinopril in Urine Using Solid-Phase Extraction and Reversed-Phase High-Performance Liquid Chromatography. J Chromatogr B Biomed Appl 1995; 673(2): 306-10.

2. Rosenstein E. Diccionario de Especialidades Farmacéuticas. Edición 46. PLM 2001: 1681-84.

3. Noble TA, Murray KM. Lisinopril: a Nonsulfhydry Angiotensin-Coverting Enzyme Inhibitor. Clin Pharm 1988; 7(9): 659-69.

4. Monografía de Lisinopril. 02-05-2001 disponible en www.rxlist. com

5. Monografía de Lisinopril. Drugdex evaluations 02-05-2001 disponible en www.micromedex.com Drugdex

6. Monografía de Lisinopril Zestoretic R (Lisinopril Zeneca) disponible en URL: http://www.rxmed. com

7. Goodman-Gilman. Las Bases Farmacológicas de la Terapéutica. Editorial McGraw-Hill. Interamericana, Novena edición. 1996; Vol. I y II: 798, 831 y 1869.

8. Thomson AH, Kelly JG, Whiting B. Lisinopril Population Pharmacokinetics in Elderly and Renal Disease Patients with Hypertension. Br J Clin Pharmac 1989: 27, 57-65.

9. Beermann B, Till AE, Gomez HJ, Hichens M, Bolognese JA, Junggren I. Pharmacokinetics of Lisinopril (IV/PO) in Healthy Volunteers. Biopharmaceutics & Drug Disposition, 1989; 10: 397-409.

10. Norma Oficial Mexicana NOM-177-SSA1-1998. Diario Oficial de la Federación 7 de mayo de 1999.

11. Analytical methods for an in vivo Bioavailability study. 21 CFR parte 320.29

12. Montgomery D. Introducción al Control Estadístico de la Calidad. Grupo Editorial Iberoamericana. 442.

13. Reglamento de la Ley General de Salud en Materia de Investigación para la Salud. DOF del 6 de enero de 1987.

14. <1090> In vivo bioequivalence guidance. USP 25 General chapters page 2165.

15. Saenz-Campos D, Bayes MC, Masana E, Martin S, Barbanoj M, Jane F. Sex related pharmacokinetic and pharmacodynamic variations of lisinopril. Methods Find Exp Clin Pharmacol 1996; 18(8): 533-8.

16. Laher MS, Mullkerrins E, Hosie J, Conell PA, Smith RP, Swaisland AJ. The effects of age and renal impairment on the pharmacokinetics of coadministered lisinopril and hydrochlorothiazide. J Hum Hypertens 1991; (Suppl. 2); 77-84.

17. Bellisant E, Nquyen PC, Giudicelli JF. Pharmacokinetic-Pharmacodynamic model relating lisinopril plasma concentrations to regional hemodynamic effects in healthy volunteers. J Cardiovasc Pharmacol 1996; 28(3): 470-8.

18. Mc Lean AJ, Drummer OH, Smith HJ, Froomes P, McNeil JJ. Comparative pharmacokinetics of enalapril and lisinopril, alone and with hydralazine. J Hum Hypertens 1989; 3(Suppl. 1): 147-51.

19. Vanderburg MJ, Morris F, Marks C, Kelly JG, Dews IM, Stephens JD. A study of the potential pharmacokinetic interaction of lisinopril and digoxin in normal volunteers. Xenobiotica 1988; 18(10): 1179-84.

20. Lancaster SG, Todd PA Lisinopril. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension and congestive heart failure. Drug 1988; 35(6): 646-69.

21. Sathe P, Venitz J, Lesko L. Evaluation of Truncated Areas in the Assessment of Bioequivalence of Immediate Release Formulations of Drugs with Long Half-Lives and of Cmax with Different Dissolution Rates.

22. Guidance for Industry BA and BE Studies for orally Administered Drug Product-General Considerations. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research. October 2000.

23. Postmarketing reporting of adverse drug experiences. Definitions 21 CFR parte 314.80

24. Fortuño CV, Llorens TF, Garibay VM, Valenzuela GGF, Cárdenas LM, Luján EM. Asociación de Médicos en la Industria Farmacéutica AC (AMEIFAC), Asociación Mexicana de Farmacología AC (AMEFAR) 23-6.