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In vitro biorelevant models for evaluating modified release mesalamine products to forecast the effect of formulation and meal intake on drug release.
Eur J Pharm Biopharm. 2015 Nov; 97(Pt A):39-50.EJ

Abstract

AIMS

Postprandial administration of solid oral dosage forms greatly changes the dissolution environment compared to fasted state administration. The aims of this study were to investigate and forecast the effect of co-administration of a meal on drug release for delayed and/or extended release mesalamine formulations as well as design of in vitro tests to distinguish among formulations in a biorelevant way.

METHODS

Five different mesalamine formulations (Asacol® 400 mg, Mezavant® 1200 mg, Pentasa® 500 mg and Salofalk® in the 250 mg and 500 mg strengths) were investigated with biorelevant dissolution methods using the USP apparatus III and USP apparatus IV (open loop mode) under both fasted and fed state conditions, as well as with the dissolution methods described in pharmacopeia for delayed and extended release mesalamine products.

RESULTS

Using the biorelevant experimental conditions proposed in this study, changes in release in the proximal gut due to meal intake are forecast to be minimal for Asacol®, Mezavant®, Pentasa® and Salofalk® 500 mg, while for Salofalk® 250 mg release was predicted to occur much earlier under fed state conditions. The USP apparatus III generally tended to result in faster dissolution rates and forecast more pronounced food effects for Salofalk® 250 mg than the USP apparatus IV. The biorelevant dissolution gradients were also able to reflect the in vivo behavior of the formulations.

CONCLUSIONS

In vitro biorelevant models can be useful in the comparison of the release behavior from different delayed and extended release mesalamine formulations as well as forecasting effects of concomitant meal intake on drug release.

Authors+Show Affiliations

Institute of Pharmaceutical Technology, Goethe University Frankfurt am Main, Max von Laue St. 9, 60438 Frankfurt am Main, Germany.Institute of Pharmaceutical Technology, Goethe University Frankfurt am Main, Max von Laue St. 9, 60438 Frankfurt am Main, Germany.Faculty of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimiopolis, 15784 Zografou, Athens, Greece.Faculty of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimiopolis, 15784 Zografou, Athens, Greece.Institute of Pharmaceutical Technology, Goethe University Frankfurt am Main, Max von Laue St. 9, 60438 Frankfurt am Main, Germany. Electronic address: Dressman@em.uni-frankfurt.de.

Pub Type(s)

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

Language

eng

PubMed ID

26391972

Citation

Andreas, Cord J., et al. "In Vitro Biorelevant Models for Evaluating Modified Release Mesalamine Products to Forecast the Effect of Formulation and Meal Intake On Drug Release." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 97, no. Pt A, 2015, pp. 39-50.
Andreas CJ, Chen YC, Markopoulos C, et al. In vitro biorelevant models for evaluating modified release mesalamine products to forecast the effect of formulation and meal intake on drug release. Eur J Pharm Biopharm. 2015;97(Pt A):39-50.
Andreas, C. J., Chen, Y. C., Markopoulos, C., Reppas, C., & Dressman, J. (2015). In vitro biorelevant models for evaluating modified release mesalamine products to forecast the effect of formulation and meal intake on drug release. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 97(Pt A), 39-50. https://doi.org/10.1016/j.ejpb.2015.09.002
Andreas CJ, et al. In Vitro Biorelevant Models for Evaluating Modified Release Mesalamine Products to Forecast the Effect of Formulation and Meal Intake On Drug Release. Eur J Pharm Biopharm. 2015;97(Pt A):39-50. PubMed PMID: 26391972.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro biorelevant models for evaluating modified release mesalamine products to forecast the effect of formulation and meal intake on drug release. AU - Andreas,Cord J, AU - Chen,Ying-Chen, AU - Markopoulos,Constantinos, AU - Reppas,Christos, AU - Dressman,Jennifer, Y1 - 2015/09/21/ PY - 2015/05/18/received PY - 2015/08/25/revised PY - 2015/09/02/accepted PY - 2015/9/23/entrez PY - 2015/9/24/pubmed PY - 2016/9/14/medline KW - Biorelevant dissolution testing KW - Dose dumping KW - Food effects KW - Mesalamine (5-ASA) KW - USP apparatus III (BioDis) KW - USP apparatus IV (flow through cell) SP - 39 EP - 50 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 97 IS - Pt A N2 - AIMS: Postprandial administration of solid oral dosage forms greatly changes the dissolution environment compared to fasted state administration. The aims of this study were to investigate and forecast the effect of co-administration of a meal on drug release for delayed and/or extended release mesalamine formulations as well as design of in vitro tests to distinguish among formulations in a biorelevant way. METHODS: Five different mesalamine formulations (Asacol® 400 mg, Mezavant® 1200 mg, Pentasa® 500 mg and Salofalk® in the 250 mg and 500 mg strengths) were investigated with biorelevant dissolution methods using the USP apparatus III and USP apparatus IV (open loop mode) under both fasted and fed state conditions, as well as with the dissolution methods described in pharmacopeia for delayed and extended release mesalamine products. RESULTS: Using the biorelevant experimental conditions proposed in this study, changes in release in the proximal gut due to meal intake are forecast to be minimal for Asacol®, Mezavant®, Pentasa® and Salofalk® 500 mg, while for Salofalk® 250 mg release was predicted to occur much earlier under fed state conditions. The USP apparatus III generally tended to result in faster dissolution rates and forecast more pronounced food effects for Salofalk® 250 mg than the USP apparatus IV. The biorelevant dissolution gradients were also able to reflect the in vivo behavior of the formulations. CONCLUSIONS: In vitro biorelevant models can be useful in the comparison of the release behavior from different delayed and extended release mesalamine formulations as well as forecasting effects of concomitant meal intake on drug release. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/26391972/In_vitro_biorelevant_models_for_evaluating_modified_release_mesalamine_products_to_forecast_the_effect_of_formulation_and_meal_intake_on_drug_release_ DB - PRIME DP - Unbound Medicine ER -