Bioequivalence of two enteric coated formulations of pantoprazole in healthy volunteers under fasting and fed conditions

dc.creatorde Campos, DR
dc.creatorVieira, NR
dc.creatorBernasconi, G
dc.creatorBarros, FAP
dc.creatorMeurer, EC
dc.creatorMarchioretto, MA
dc.creatorCoelho, EC
dc.creatorCalafatti, SA
dc.creatorSommer, C
dc.creatorCouto, JM
dc.creatorBuranello, S
dc.creatorSilva, ARC
dc.creatorAmarante, AR
dc.date2007
dc.date2014-07-30T13:52:06Z
dc.date2015-11-26T17:12:26Z
dc.date2014-07-30T13:52:06Z
dc.date2015-11-26T17:12:26Z
dc.date.accessioned2018-03-29T00:00:50Z
dc.date.available2018-03-29T00:00:50Z
dc.identifierArzneimittel-forschung-drug Research. Ecv-editio Cantor Verlag Medizin Naturwissenschaften, v. 57, n. 6, n. 309, n. 314, 2007.
dc.identifier0004-4172
dc.identifierWOS:000248389700003
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/55567
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/55567
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1281328
dc.descriptionPurpose: To compare the bioavailability of two pantoprazole (CAS 102625-70-7) formulations (40 mg pantoprazole enteric coated tablets) under fasted and fed conditions as well as to evaluate the dissolution profile in biorelevant media. Methods: The subjects received either 40 mg of the reference or of test formulation in fasting (n = 28) and fed (n = 70) condition. The studies were conducted according to a single dose and randomized crossover design. Blood samples were collected up to 12 h after drug administration in fasting condition and up to 48 h in fed condition. Plasma concentrations of pantoprazole were determined by LC-MS/MS. Pharmacokinetic parameters were calculated from the observed plasma concentration-time profiles. Bioequivalence between the for mulations in fasting and fed condition was assessed considering 90% confidence intervals for the ratio of means for lnC(max) and lnAUC(0-t), within 0.8-1.25. Dissolution profiles were evaluated in biorelevant media [Fasting State Simulating Intestinal Fluid (FaSSIF) and Fed State Simulating Intestinal Fluid (FeSSIF)]. The sameness of the dissolution curves was assessed by f(2) values between 50 and 100. Results: Under fasting condition the 90% confidence interval for the ratio of means for the lnC(max) (0.94-1.03) and lnAUC(0-t) (0.89-0.99) was within the guideline range of bioequivalence (0.80-1.25). However, the data for lnC(max) (0.51-0.76) and lnAUC(0-t) (0.68-0.90) under fed condition were not within the bioequivalence range. The postprandial study demonstrated a high intra-subject variability and in some subjects pantoprazole could not be detected for up to 24 h, although the dissolution profile of reference and test formulations presented a similar disposition in FaSSIF and FeSSIF as confirmed by the values of f(2) higher than 50. Conclusion: The results demonstrated that the test formulation was bioequivalent to the reference in fasting condition but not in postprandial state. The dissolution profile in FaSSIF indicates that this biorelevant medium was more adequate to discriminate the in vivo disposition of pantoprazole than FeSSIF. Futhermore, the fed condition study had shown a pronounced influence of food in the absorption of pantoprazole after single oral dose administration.
dc.description57
dc.description6
dc.description309
dc.description314
dc.languageen
dc.publisherEcv-editio Cantor Verlag Medizin Naturwissenschaften
dc.publisherAulendorf
dc.publisherAlemanha
dc.relationArzneimittel-forschung-drug Research
dc.relationArzneimittelforschung
dc.rightsaberto
dc.sourceWeb of Science
dc.subjectantiulceratives
dc.subjectCAS 102625-70-7
dc.subjectpantoprazole, bioequivalence, biorelevant dissolution testing
dc.subjectproton pump inhibitors
dc.subjectPharmacokinetics
dc.subjectOmeprazole
dc.subjectDrug
dc.subjectDissolution
dc.subjectAbsorption
dc.titleBioequivalence of two enteric coated formulations of pantoprazole in healthy volunteers under fasting and fed conditions
dc.typeArtículos de revistas


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