Información de la revista
Vol. 1. Núm. 3.
Páginas 155-160 (Septiembre - Octubre 2005)
Compartir
Compartir
Descargar PDF
Más opciones de artículo
Vol. 1. Núm. 3.
Páginas 155-160 (Septiembre - Octubre 2005)
Originales
Acceso a texto completo
Estudio de la biodisponibilidad en magnitud y en velocidad de comprimidos de ibuprofeno
Study of the extent and rate of bioavailability of ibuprofen tablets
Visitas
19174
M. Farréa,b,
Autor para correspondencia
mfarre@imim.es

Correspondencia: Dr. M. Farré. Unitat de Farmacologia. Institut Municipal d’Investigació Mèdica (IMIM). Doctor Aiguader, 80. 08003 Barcelona. España.
, P.N. Roseta,b,c, J.A. Pascuala,d, S. Abanadesa,b, E. Menoyoa, Y. Álvareza, A. Baenac
a Unitat de Farmacologia. Institut Municipal d’Investigació Mèdica (IMIM). Barcelona. España
b Facultat de Medicina. Universitat Autònoma de Barcelona. Barcelona. España
c Laboratorios Gelos, SL. Barcelona. España
d Facultat de Ciències de la Salut i de la Vida. Universitat Pompeu Fabra. Barcelona. España
Este artículo ha recibido
Información del artículo
Resumen
Bibliografía
Descargar PDF
Estadísticas

Se estudió la biodisponibilidad en magnitud y en velocidad de ibuprofeno en comprimidos en un ensayo clínico cruzado en 18 sujetos sanos de ambos sexos. El estudio se aprobó por el comité ético del centro y se autorizó por la Agencia Española del Medicamento. Los voluntarios firmaron el consentimiento informado y se incluyeron siguiendo los procedimientos habituales de este tipo de estudios. Los participantes recibieron en 2 sesiones distintas una dosis única de 600 mg de ibuprofeno en Gelofeno® 600 mg comprimidos, Laboratorios Gelos SL, o en la formulación de referencia, Neobrufen® 600 mg comprimidos. Se determinaron las concentraciones plasmáticas de ibuprofeno inmediatamente antes (0 h) y 0,25, 0,5, 0,75, 1, 1,5, 2, 2,5, 3, 4, 6, 8, 10, 12 y 24 h después de la administración del fármaco, y se calcularon los parámetros farmacocinéticos derivados de éstas. En todos los sujetos, Gelofeno® 600 mg comprimidos produjo concentraciones plasmáticas de ibuprofeno por encima del límite de cuantificación entre 15 y 30 min tras su administración, y en 9 (50%) de ellos en 1 h ya se alcanzaron las concentraciones máximas. La mediana del tiempo al que se alcanzó la concentración máxima (tmáx) fue de 1,25 h y la concentración máxima promedio fue de 40,7mg/l. Gelofeno® 600 mg comprimidos resultó bioequivalente, tanto en la magnitud como en la velocidad de su biodisponibilidad comparado con el fármaco de referencia. El preparado presentó una Buena tolerabilidad y no se observaron acontecimientos adversos relacionados con el fármaco administrado.

Palabras clave:
Ibuprofeno
Biodisponibilidad
Farmacocinética
Absorción
Voluntarios sanos

The extent and rate of bioavailability of ibuprofen tablets were determined in a crossover clinical trial in 18 healthy subjects of both sexes. The study was approved by the local ethical committee and was authorized by the Spanish Medicines Agency. Volunteers signed an informed consent form and were included in accordance with the standard procedures for this type of study. In two distinct sessions participants received a single 600 mg ibuprofen dose as Gelofeno® 600 mg tablets (Laboratorios Gelos S.L.), or as the reference formulation, Neobrufen® 600 mg tablets. Ibuprofen concentrations in plasma were determined immediately before (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12 and 24 h after drug administration. The pharmacokinetic parameters were then calculated. In all subjects, Gelofeno® 600 mg tablets produced plasma concentrations above the quantification limit between 15 and 30 minutes after administration, and in 9 (50%) of these subjects maximal plasma concentrations were reached at 1 h. The median tmax was 1.25 h, and the average maximal plasma concentration was 40.7 mg/l. Gelofeno® 600 mg tablets were bioequivalent both in extent and in rate of bioavailability compared with the reference drug. The formulation showed good tolerability and no medication-related adverse effects were observed.

Key words:
Ibuprofen
Bioavailability
Pharmacokinetics
Absorption
Healthy volunteers
El Texto completo está disponible en PDF
Bibliografía
[1.]
J. Flórez, J.A. Armijo, A. Mediavilla.
Farmacología humana.
4.a ed., Masson S.A, (2003),
[2.]
K.D. Rainsford, A. Ibuprofen.
critical bibliographic review.
Taylor & Francis, (1999),
[3.]
K.D. Rainsford.
Discovery, mechanisms of action and safety of ibuprofen.
Int J Clin Pract, (2003), pp. 3-8
[4.]
S.C. Sweetman.
Martindale. Guía completa de consulta farmacoterapéutica.
1.a ed., Pharma Editores, (2003),
[5.]
N.M. Davies.
Clinical pharmacokinetics of ibuprofen. The first 30 years.
Clin Pharmacokinet, 34 (1998), pp. 101-154
[6.]
W.T. Beaver.
Review of the analgesic efficacy of ibuprofen.
Int J Clin Pract, (2003), pp. 13-17
[7.]
S.L. Collins, R.A. Moore, H.J. McQuay, P.J. Wiffen.
Oral ibuprofen and diclofenac in post-operative pain: a quantitative systematic review.
Eur J Pain, 2 (1998), pp. 285-291
[8.]
M. Hyllested, S. Jones, J.L. Pedersen, H. Kehlet.
Comparative effect of paracetamol, NSAIDs or their combination in postoperative pain management: a qualitative review.
Br J Anaesth, 88 (2002), pp. 199-214
[9.]
R. Kaniecki.
Headache assessment and management.
JAMA, 289 (2003), pp. 1430-1433
[10.]
S. Schou, H. Nielsen, A. Nattestad, S. Hillerup, M. Ritzau, P.E. Branebjerg, et al.
Analgesic dose-response relationship of ibuprofen 50, 100, 200, and 400 mg after surgical removal of third molars: a singe-dose, randomized, placebo-controlled, and double-blind study of 304 patients.
J Clin Pharmacol, 38 (1998), pp. 447-454
[11.]
R.G. Wenzel, C.A. Sarvis, M.L. Krause.
Over-the-counter-drugs for acute migraine attacks: literature review and recommendations.
Pharmacotherapy, 23 (2003), pp. 494-505
[12.]
C.B. Berde, N.F. Sethna.
Analgesics for the treatment of pain in children.
New Engl J Med, 347 (2002), pp. 1094-1103
[13.]
E.A. Clark, A. Plint, R. Correl, I. Gaboury, B. Passi.
Analgesia for musculoskeletal injuries in children: a randomized, blinded, controlled trial comparing acetaminophen, ibuprofen and codeine.
Acad Emerg Med, 10 (2003), pp. 469
[14.]
C. Litalien, E. Jacqz-Aigrain.
Risks and benefits of nonsteroidal anti-inflammatory drugs in children.
Paediatr Drugs, 3 (2001), pp. 817-858
[15.]
A. Wong, A. Sibbald, F. Ferrero, M. Plager, M.E. Santolaya, A.M. Escobar, Fever Pediatric Study Group, et al.
Antipyretic effects of dipyrone versus ibuprofen versus acetaminophen in children: results of a multinational, randomized, modified double-blind study.
Clin Pediatr (Phila), 40 (2001), pp. 313-324
[16.]
Canadian Paediatric Society. Acetaminophen and ibuprofen in the management of fever and mild to moderate pain in children. Position Statements, Practice Point: Prepared by the Drug Therapy and Hazardous Substances Committee. Reaffirmed January 2002. Reference No. DT98-01 (Formerly DTP98-01). Former versions published in: Paediatrics & Child Health 1998;3(4). (Consultado 04/06/2003) Disponible en: http://www.cps.ca/english/statements/DT/dt98-01.htm
[17.]
H.M.P. Freie.
Antipyretic analgesics.
Meyler's side effects of drugs, 14th ed.,
[18.]
J.M. Le Parc, E. Van Ganse, N. Moore, R. Wall, H. Schneid, F. Verriere.
Comparative tolerability of paracetamol, aspirin and ibuprofen for shortterm analgesia in patients with misculoskeletal conditions: Results in 4291 patients.
Clin Rheumatol, 21 (2002), pp. 28-31
[19.]
S.M. Lesko, A.A. Mitchell.
An assessment of the safety of pediatric ibuprofen. A practitioner-based randomized clinical trial.
JAMA, 273 (1995), pp. 929-933
[20.]
S.M. Lesko, A.A. Mitchell.
Renal function after short-term ibuprofen use in infants and children.
Pediatrics, 100 (1997), pp. 954-957
[21.]
S.M. Lesko, A.A. Mitchell.
The safety of acetaminophen and ibuprofen among children younger than two years old.
Pediatrics, 104 (1999), pp. e39
[22.]
S.M. Lesko, C. Louik, R.M. Vezina, A.A. Mitchell.
Asthma morbidity after the short-term use of ibuprofen in children.
Pediatrics, 109 (2002), pp. e20
[23.]
S.C. Lewis, M.J. Langman, J.R. Laporte, J.N. Matthews, M.D. Rawlins, B.E. Wiholm.
Dose-response relationships between individual nonaspirin nonsteroidal anti-inflammatory drugs (NANSAIDs) and serious upper gastrointestinal bleeding: a meta-analysis based on individual patient data.
Br J Clin Pharmacol, 54 (2002), pp. 320-326
[24.]
N. Moore, C. Noblet, C. Breemeersch.
Mise au point sur la sécurité de l’ibuprofène à dose antalgique-antipyrétique.
Thérapie, 51 (1996), pp. 458-463
[25.]
N. Moore, E. Van Ganse, J.M. Le Parc, R. Wall, H. Schneid, M. Farhan, et al.
The PAIN Study: Paracetamol, Aspirin and Ibuprofen New tolerability study.
Clin Drug Invest, 18 (1999), pp. 89-98
[26.]
P. Rampal, N. Moore, E. Van Ganse, J.M. Le Parc, R. Wall, H. Schneid, et al.
Gastrointestinal tolerability of ibuprofen compared with paracetamol and aspirin at over-the-counter doses.
J Int Med Res, 30 (2002), pp. 301-308
[27.]
European Agency for the Evaluation of Medicinal Products-Committee for Proprietary Medicinal Products. Note for guidance on the investigation of bioavailability and bioequivalence. CPMP/EWP/QWP/1401/98. 2001.
[28.]
S. Bolton.
Pharmaceutical statistics.
Preclinical and clinical applications, 3rd ed., Marcel Dekker, Inc, (1997),
[29.]
E. Diletti, D. Hauschke, V.W. Steinijans.
Sample size determination for bioequivalence assessment by means of confidence intervals.
Int J Clin Pharmacol Toxicol, 30 (1992), pp. S51-S58
[30.]
E. Diletti, D. Hauschke, V.W. Steinijans.
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 Toxicol, 30 (1992), pp. S59-S62
[31.]
J.P. Liu, S.C. Chow.
Sample size determination for the two one-sided test procedure in bioequivalence.
J Pharmacokin Biopharm, 20 (1992), pp. 101-104
[32.]
P.N. Roset, M. Farré, J.A. Pascual, M. Mas, J. Segura.
PKEQ®: a program for statistical analysis in bioequivalence studies.
Thérapie, (1995), pp. 494
Copyright © 2005. Elsevier España S.L. Barcelona
Idiomas
Reumatología Clínica
Opciones de artículo
Herramientas
es en

¿Es usted profesional sanitario apto para prescribir o dispensar medicamentos?

Are you a health professional able to prescribe or dispense drugs?