Phentolamine bioequivalence study
Autor(a) principal: | |
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Data de Publicação: | 2004 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://hdl.handle.net/11449/219316 |
Resumo: | Objective: To assess the bioequivalence of 2 tablet formulations of phentolamine (Regitine phentolamine 40 mg tablet formulation by Novartis, Brazil, as test formulation, and Vasomax, phentolamine 40 mg tablet formulation by Schering Plough S.A., Brazil, as reference formulation). Methods: A single 40 mg oral dose of each formulation was administered to 36 male healthy volunteers. The study was conducted after screening, using an open, randomized, 2-period crossover design, a 7-day interval between doses, and wash-out period of at least 4 weeks. Plasma samples for determination of phentolamine were obtained predose and at intervals over 720 min postdose. Plasma concentrations were quantified by reversed-phase liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using multiple reactions monitoring (MRM) method. Precision of the method was evaluated using calibration curves and plasma quality control samples. The subjects were monitored throughout the study. Systolic and diastolic blood pressure and pulse rate measurement were taken predose and at intervals up to 720 min. Tolerance of both products was good. No serious adverse reactions were reported. The pharmacokinetic parameters calculated for both compounds included: AUC(0-720 min), AUC(0-∞), Cmax, Cmax/AUC(0-720 min), tmax, t1/2 and kc. Results: The maximum concentrations reached (Cmax) were compared. Regitine 40 mg formulation Cmax geometric mean ratio was 108.29% (90% CI = 98.58 - 118.96) of Vasomax 40 mg formulation. The areas under the curve (AUC(0-720 min)) were compared. Regitine 40 formulation (AUC(0-720 min) geometric mean ratio was 102.33% (90% CI = 97.21 - 107.72) of Vasomax 40 mg formulation. Conclusion: Since the 90% CI for both Cmax and AUC ratio where inside the 80 to 125% interval proposed by the Food and Drug Administration, it is concluded that Regitine 40 mg tablet is bioequivalent to Vasomax for the rate and extent of absorption. |
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Phentolamine bioequivalence studyBioavailabilityHumanMass spectrometryPharmacokineticPhentolamineObjective: To assess the bioequivalence of 2 tablet formulations of phentolamine (Regitine phentolamine 40 mg tablet formulation by Novartis, Brazil, as test formulation, and Vasomax, phentolamine 40 mg tablet formulation by Schering Plough S.A., Brazil, as reference formulation). Methods: A single 40 mg oral dose of each formulation was administered to 36 male healthy volunteers. The study was conducted after screening, using an open, randomized, 2-period crossover design, a 7-day interval between doses, and wash-out period of at least 4 weeks. Plasma samples for determination of phentolamine were obtained predose and at intervals over 720 min postdose. Plasma concentrations were quantified by reversed-phase liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using multiple reactions monitoring (MRM) method. Precision of the method was evaluated using calibration curves and plasma quality control samples. The subjects were monitored throughout the study. Systolic and diastolic blood pressure and pulse rate measurement were taken predose and at intervals up to 720 min. Tolerance of both products was good. No serious adverse reactions were reported. The pharmacokinetic parameters calculated for both compounds included: AUC(0-720 min), AUC(0-∞), Cmax, Cmax/AUC(0-720 min), tmax, t1/2 and kc. Results: The maximum concentrations reached (Cmax) were compared. Regitine 40 mg formulation Cmax geometric mean ratio was 108.29% (90% CI = 98.58 - 118.96) of Vasomax 40 mg formulation. The areas under the curve (AUC(0-720 min)) were compared. Regitine 40 formulation (AUC(0-720 min) geometric mean ratio was 102.33% (90% CI = 97.21 - 107.72) of Vasomax 40 mg formulation. Conclusion: Since the 90% CI for both Cmax and AUC ratio where inside the 80 to 125% interval proposed by the Food and Drug Administration, it is concluded that Regitine 40 mg tablet is bioequivalent to Vasomax for the rate and extent of absorption.Department of Urology Clinical Pharmacology Unit UNIFAC Federal University of Ceara, CearaDepartment of Clinical Pharmacology Clinical Pharmacology Unit UNIFAC Federal University of Ceara, CearaClinical Pharmacology State University of Sao Paulo, Sao PauloUnidad de Farmacologia Clinica Departamento de Farmacologia, Rua Cel. Nunes de Melo 1127, Fortaleza-Ceara 60431-970Federal University of CearaUniversidade de São Paulo (USP)Unidad de Farmacologia ClinicaSilva, L. F.G.Moraes, M. O.Santana, G. S.M.Frota Bezerra, F. A.De Nucci, G.Moraes, M. E.A.2022-04-28T18:54:59Z2022-04-28T18:54:59Z2004-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article43-49International Journal of Clinical Pharmacology and Therapeutics, v. 42, n. 1, p. 43-49, 2004.0946-1965http://hdl.handle.net/11449/2193162-s2.0-0347135827Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengInternational Journal of Clinical Pharmacology and Therapeuticsinfo:eu-repo/semantics/openAccess2022-04-28T18:54:59Zoai:repositorio.unesp.br:11449/219316Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462022-04-28T18:54:59Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Phentolamine bioequivalence study |
title |
Phentolamine bioequivalence study |
spellingShingle |
Phentolamine bioequivalence study Silva, L. F.G. Bioavailability Human Mass spectrometry Pharmacokinetic Phentolamine |
title_short |
Phentolamine bioequivalence study |
title_full |
Phentolamine bioequivalence study |
title_fullStr |
Phentolamine bioequivalence study |
title_full_unstemmed |
Phentolamine bioequivalence study |
title_sort |
Phentolamine bioequivalence study |
author |
Silva, L. F.G. |
author_facet |
Silva, L. F.G. Moraes, M. O. Santana, G. S.M. Frota Bezerra, F. A. De Nucci, G. Moraes, M. E.A. |
author_role |
author |
author2 |
Moraes, M. O. Santana, G. S.M. Frota Bezerra, F. A. De Nucci, G. Moraes, M. E.A. |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
Federal University of Ceara Universidade de São Paulo (USP) Unidad de Farmacologia Clinica |
dc.contributor.author.fl_str_mv |
Silva, L. F.G. Moraes, M. O. Santana, G. S.M. Frota Bezerra, F. A. De Nucci, G. Moraes, M. E.A. |
dc.subject.por.fl_str_mv |
Bioavailability Human Mass spectrometry Pharmacokinetic Phentolamine |
topic |
Bioavailability Human Mass spectrometry Pharmacokinetic Phentolamine |
description |
Objective: To assess the bioequivalence of 2 tablet formulations of phentolamine (Regitine phentolamine 40 mg tablet formulation by Novartis, Brazil, as test formulation, and Vasomax, phentolamine 40 mg tablet formulation by Schering Plough S.A., Brazil, as reference formulation). Methods: A single 40 mg oral dose of each formulation was administered to 36 male healthy volunteers. The study was conducted after screening, using an open, randomized, 2-period crossover design, a 7-day interval between doses, and wash-out period of at least 4 weeks. Plasma samples for determination of phentolamine were obtained predose and at intervals over 720 min postdose. Plasma concentrations were quantified by reversed-phase liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using multiple reactions monitoring (MRM) method. Precision of the method was evaluated using calibration curves and plasma quality control samples. The subjects were monitored throughout the study. Systolic and diastolic blood pressure and pulse rate measurement were taken predose and at intervals up to 720 min. Tolerance of both products was good. No serious adverse reactions were reported. The pharmacokinetic parameters calculated for both compounds included: AUC(0-720 min), AUC(0-∞), Cmax, Cmax/AUC(0-720 min), tmax, t1/2 and kc. Results: The maximum concentrations reached (Cmax) were compared. Regitine 40 mg formulation Cmax geometric mean ratio was 108.29% (90% CI = 98.58 - 118.96) of Vasomax 40 mg formulation. The areas under the curve (AUC(0-720 min)) were compared. Regitine 40 formulation (AUC(0-720 min) geometric mean ratio was 102.33% (90% CI = 97.21 - 107.72) of Vasomax 40 mg formulation. Conclusion: Since the 90% CI for both Cmax and AUC ratio where inside the 80 to 125% interval proposed by the Food and Drug Administration, it is concluded that Regitine 40 mg tablet is bioequivalent to Vasomax for the rate and extent of absorption. |
publishDate |
2004 |
dc.date.none.fl_str_mv |
2004-01-01 2022-04-28T18:54:59Z 2022-04-28T18:54:59Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
International Journal of Clinical Pharmacology and Therapeutics, v. 42, n. 1, p. 43-49, 2004. 0946-1965 http://hdl.handle.net/11449/219316 2-s2.0-0347135827 |
identifier_str_mv |
International Journal of Clinical Pharmacology and Therapeutics, v. 42, n. 1, p. 43-49, 2004. 0946-1965 2-s2.0-0347135827 |
url |
http://hdl.handle.net/11449/219316 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
International Journal of Clinical Pharmacology and Therapeutics |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
43-49 |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1799964803390767104 |