Document Detail

Bioequivalence of two enteric coated formulations of pantoprazole in healthy volunteers under fasting and fed conditions.
MedLine Citation:
PMID:  17688075     Owner:  NLM     Status:  MEDLINE    
PURPOSE: 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 formulations in fasting and fed condition was assessed considering 90% confidence intervals for the ratio of means for lnCmax 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 f2 values between 50 and 100.
RESULTS: Under fasting condition the 90% confidence interval for the ratio of means for the lnCmax, (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 lnCmax (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 f2 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. Furthermore, the fed condition study had shown a pronounced influence of food in the absorption of pantoprazole after single oral dose administration.
Daniel Rossi de Campos; Nelson Rogério Vieira; Gilberto Bernasconi; Fabio Alessandro Proença Barros; Eduardo César Meurer; Marco Antônio Marchioretto; Edvaldo Capobiango Coelho; Silvana Aparecida Calafatti; Carolina Sommer; Jussara Moreira Couto; Simoni Buranello; Andréia Rodrigues Cristino Silva; Antônio Ricardo Amarante; Eduardo Abib; José Pedrazzoli Júnior
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Publication Detail:
Type:  Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  57     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  2007  
Date Detail:
Created Date:  2007-08-10     Completed Date:  2007-09-11     Revised Date:  2013-06-04    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  309-14     Citation Subset:  IM    
Clinical Pharmacology and Gastroenterology Unit, São Francisco University Medical School, Bragança Paulista, SP (Brazil).
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MeSH Terms
2-Pyridinylmethylsulfinylbenzimidazoles / administration & dosage*,  pharmacokinetics*
Anti-Ulcer Agents / administration & dosage*,  pharmacokinetics*
Area Under Curve
Chemistry, Pharmaceutical
Cross-Over Studies
Fasting / physiology
Mass Spectrometry
Tablets, Enteric-Coated
Therapeutic Equivalency
Reg. No./Substance:
0/2-Pyridinylmethylsulfinylbenzimidazoles; 0/Anti-Ulcer Agents; 0/Excipients; 0/Tablets, Enteric-Coated; D8TST4O562/pantoprazole

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