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The role of individual gastric emptying of pellets in the prediction of diclofenac in vivo dissolution.
J Control Release. 2013 Mar 28; 166(3):286-93.JC

Abstract

The objective of the present study was to check for the possibility to successfully predict individual in vivo dissolution/absorption profiles resulting from fasted administration of a diclofenac extended release pellet formulation. For this purpose dissolution profiles were generated with different dissolution setups using a set of media reflecting pH-conditions in the different segments of the gastrointestinal tract. Since gastric emptying of pellets seemed to be a critical factor for in vivo drug release, a set of different gastric residence times was screened in in vitro studies. Subsequently, in vitro release profiles were first directly compared with the individual in vivo absorption profiles and in a second step a mathematical model, which had been developed in a previous study, was applied to calculate predicted individual in vivo release profiles based on in vitro release profiles and individual gastric emptying. The comparison of predicted individual in vivo release profiles and individual in vivo absorption profiles showed a high degree of similarity, thus confirming the suitability of a set of different gastric residence times used in in vitro drug release testing. Additionally, obtained results indicated that a substantial part of variability of diclofenac absorption profiles can be explained by the variability of pellet gastric emptying kinetics.

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Authors+Show Affiliations

Klein S
Institute of Pharmacy, Center of Drug Absorption and Transport, Ernst Moritz Arndt University Greifswald, 17487 Greifswald, Germany.
Garbacz G
No affiliation info available
Pišlar M
No affiliation info available
Locatelli I
No affiliation info available
Liu C
No affiliation info available
Weitschies W
No affiliation info available
Siegmund W
No affiliation info available
Mrhar A
No affiliation info available
Bogataj M
No affiliation info available

MeSH

AbsorptionAnti-Inflammatory Agents, Non-SteroidalBiological AvailabilityDelayed-Action PreparationsDiclofenacGastric EmptyingHumansModels, BiologicalPredictive Value of TestsSolubilityTime Factors

Pub Type(s)

Journal Article

Language

eng

PubMed ID

23306025

Citation

Klein, Sandra, et al. "The Role of Individual Gastric Emptying of Pellets in the Prediction of Diclofenac in Vivo Dissolution." Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 166, no. 3, 2013, pp. 286-93.
Klein S, Garbacz G, Pišlar M, et al. The role of individual gastric emptying of pellets in the prediction of diclofenac in vivo dissolution. J Control Release. 2013;166(3):286-93.
Klein, S., Garbacz, G., Pišlar, M., Locatelli, I., Liu, C., Weitschies, W., Siegmund, W., Mrhar, A., & Bogataj, M. (2013). The role of individual gastric emptying of pellets in the prediction of diclofenac in vivo dissolution. Journal of Controlled Release : Official Journal of the Controlled Release Society, 166(3), 286-93. https://doi.org/10.1016/j.jconrel.2012.12.032
Klein S, et al. The Role of Individual Gastric Emptying of Pellets in the Prediction of Diclofenac in Vivo Dissolution. J Control Release. 2013 Mar 28;166(3):286-93. PubMed PMID: 23306025.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The role of individual gastric emptying of pellets in the prediction of diclofenac in vivo dissolution. AU - Klein,Sandra, AU - Garbacz,Grzegorz, AU - Pišlar,Mitja, AU - Locatelli,Igor, AU - Liu,Chong, AU - Weitschies,Werner, AU - Siegmund,Werner, AU - Mrhar,Aleš, AU - Bogataj,Marija, Y1 - 2013/01/08/ PY - 2012/10/10/received PY - 2012/12/13/revised PY - 2012/12/29/accepted PY - 2013/1/12/entrez PY - 2013/1/12/pubmed PY - 2013/8/30/medline SP - 286 EP - 93 JF - Journal of controlled release : official journal of the Controlled Release Society JO - J Control Release VL - 166 IS - 3 N2 - The objective of the present study was to check for the possibility to successfully predict individual in vivo dissolution/absorption profiles resulting from fasted administration of a diclofenac extended release pellet formulation. For this purpose dissolution profiles were generated with different dissolution setups using a set of media reflecting pH-conditions in the different segments of the gastrointestinal tract. Since gastric emptying of pellets seemed to be a critical factor for in vivo drug release, a set of different gastric residence times was screened in in vitro studies. Subsequently, in vitro release profiles were first directly compared with the individual in vivo absorption profiles and in a second step a mathematical model, which had been developed in a previous study, was applied to calculate predicted individual in vivo release profiles based on in vitro release profiles and individual gastric emptying. The comparison of predicted individual in vivo release profiles and individual in vivo absorption profiles showed a high degree of similarity, thus confirming the suitability of a set of different gastric residence times used in in vitro drug release testing. Additionally, obtained results indicated that a substantial part of variability of diclofenac absorption profiles can be explained by the variability of pellet gastric emptying kinetics. SN - 1873-4995 UR - https://www.unboundmedicine.com/medline/citation/23306025/The_role_of_individual_gastric_emptying_of_pellets_in_the_prediction_of_diclofenac_in_vivo_dissolution_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0168-3659(13)00005-9 DB - PRIME DP - Unbound Medicine ER -

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