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Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form.
Eur J Pharm Sci. 2009 Jun 28; 37(3-4):434-41.EJ

Abstract

In vitro biorelevant dissolution tests enabling the prediction of in vivo performance of an oral modified-release (MR) dosage form were developed in this study. In vitro dissolution of MR diclofenac sodium pellets containing 100mg active ingredient was evaluated under simulated pre- and postprandial conditions using USP Apparatus 3 (reciprocating cylinder, Bio-Dis) and 4 (flow-through cell) and results compared with compendial methods using USP Apparatus 1 (basket) and 2 (paddle). In vivo, the effects of food on the absorption of diclofenac sodium from the pellet dosage form were investigated by administering the product to 16 healthy volunteers pre- and postprandially in a crossover-design study. The in vitro results were compared with the in vivo data by means of Level A in vitro-in vivo correlation (IVIVC) and Weibull distribution analysis. The compendial dissolution tests were not able to predict food effects. The biorelevant dissolution tests predicted correctly that the release (and hence absorption) of diclofenac sodium would be slower in the fed state than in the fasted state. No significant differences in extent of absorption due to changes in extent of release were predicted or observed. The results demonstrate good correlations between in vitro drug release and in vivo drug absorption in both pre- and postprandial states using the biorelevant dissolution test methods.

Authors+Show Affiliations

Institute of Pharmaceutical Technology, Johann Wolfgang Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany. jantratid@em.uni-frankfurt.deNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Journal Article

Language

eng

PubMed ID

19491035

Citation

Jantratid, Ekarat, et al. "Application of Biorelevant Dissolution Tests to the Prediction of in Vivo Performance of Diclofenac Sodium From an Oral Modified-release Pellet Dosage Form." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 37, no. 3-4, 2009, pp. 434-41.
Jantratid E, De Maio V, Ronda E, et al. Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form. Eur J Pharm Sci. 2009;37(3-4):434-41.
Jantratid, E., De Maio, V., Ronda, E., Mattavelli, V., Vertzoni, M., & Dressman, J. B. (2009). Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 37(3-4), 434-41. https://doi.org/10.1016/j.ejps.2009.03.015
Jantratid E, et al. Application of Biorelevant Dissolution Tests to the Prediction of in Vivo Performance of Diclofenac Sodium From an Oral Modified-release Pellet Dosage Form. Eur J Pharm Sci. 2009 Jun 28;37(3-4):434-41. PubMed PMID: 19491035.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form. AU - Jantratid,Ekarat, AU - De Maio,Vincenzo, AU - Ronda,Emanuela, AU - Mattavelli,Valentina, AU - Vertzoni,Maria, AU - Dressman,Jennifer B, Y1 - 2009/04/05/ PY - 2009/01/28/received PY - 2009/03/23/revised PY - 2009/03/27/accepted PY - 2009/6/4/entrez PY - 2009/6/6/pubmed PY - 2009/8/25/medline SP - 434 EP - 41 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 37 IS - 3-4 N2 - In vitro biorelevant dissolution tests enabling the prediction of in vivo performance of an oral modified-release (MR) dosage form were developed in this study. In vitro dissolution of MR diclofenac sodium pellets containing 100mg active ingredient was evaluated under simulated pre- and postprandial conditions using USP Apparatus 3 (reciprocating cylinder, Bio-Dis) and 4 (flow-through cell) and results compared with compendial methods using USP Apparatus 1 (basket) and 2 (paddle). In vivo, the effects of food on the absorption of diclofenac sodium from the pellet dosage form were investigated by administering the product to 16 healthy volunteers pre- and postprandially in a crossover-design study. The in vitro results were compared with the in vivo data by means of Level A in vitro-in vivo correlation (IVIVC) and Weibull distribution analysis. The compendial dissolution tests were not able to predict food effects. The biorelevant dissolution tests predicted correctly that the release (and hence absorption) of diclofenac sodium would be slower in the fed state than in the fasted state. No significant differences in extent of absorption due to changes in extent of release were predicted or observed. The results demonstrate good correlations between in vitro drug release and in vivo drug absorption in both pre- and postprandial states using the biorelevant dissolution test methods. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/19491035/Application_of_biorelevant_dissolution_tests_to_the_prediction_of_in_vivo_performance_of_diclofenac_sodium_from_an_oral_modified_release_pellet_dosage_form_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(09)00115-8 DB - PRIME DP - Unbound Medicine ER -