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Bioequivalence of two enteric coated formulations of pantoprazole in healthy volunteers under fasting and fed conditions.
Arzneimittelforschung. 2007; 57(6):309-14.A

Abstract

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.

Authors+Show Affiliations

Clinical Pharmacology and Gastroenterology Unit, São Francisco University Medical School, Bragança Paulista, SP (Brazil). cinetica04@yahoo.com.brNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17688075

Citation

de Campos, Daniel Rossi, et al. "Bioequivalence of Two Enteric Coated Formulations of Pantoprazole in Healthy Volunteers Under Fasting and Fed Conditions." Arzneimittel-Forschung, vol. 57, no. 6, 2007, pp. 309-14.
de Campos DR, Vieira NR, Bernasconi G, et al. Bioequivalence of two enteric coated formulations of pantoprazole in healthy volunteers under fasting and fed conditions. Arzneimittelforschung. 2007;57(6):309-14.
de Campos, D. R., Vieira, N. R., Bernasconi, G., Barros, F. A., Meurer, E. C., Marchioretto, M. A., Coelho, E. C., Calafatti, S. A., Sommer, C., Couto, J. M., Buranello, S., Silva, A. R., Amarante, A. R., Abib, E., & Júnior, J. P. (2007). Bioequivalence of two enteric coated formulations of pantoprazole in healthy volunteers under fasting and fed conditions. Arzneimittel-Forschung, 57(6), 309-14.
de Campos DR, et al. Bioequivalence of Two Enteric Coated Formulations of Pantoprazole in Healthy Volunteers Under Fasting and Fed Conditions. Arzneimittelforschung. 2007;57(6):309-14. PubMed PMID: 17688075.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Bioequivalence of two enteric coated formulations of pantoprazole in healthy volunteers under fasting and fed conditions. AU - de Campos,Daniel Rossi, AU - Vieira,Nelson Rogério, AU - Bernasconi,Gilberto, AU - Barros,Fabio Alessandro Proença, AU - Meurer,Eduardo César, AU - Marchioretto,Marco Antônio, AU - Coelho,Edvaldo Capobiango, AU - Calafatti,Silvana Aparecida, AU - Sommer,Carolina, AU - Couto,Jussara Moreira, AU - Buranello,Simoni, AU - Silva,Andréia Rodrigues Cristino, AU - Amarante,Antônio Ricardo, AU - Abib,Eduardo, AU - Júnior,José Pedrazzoli, PY - 2007/8/11/pubmed PY - 2007/9/12/medline PY - 2007/8/11/entrez SP - 309 EP - 14 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 57 IS - 6 N2 - 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. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/17688075/Bioequivalence_of_two_enteric_coated_formulations_of_pantoprazole_in_healthy_volunteers_under_fasting_and_fed_conditions_ DB - PRIME DP - Unbound Medicine ER -