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Prediction of the in vivo performance of enteric coated pellets in the fasted state under selected biorelevant dissolution conditions.
Eur J Pharm Sci. 2014 Oct 01; 62:8-15.EJ

Abstract

The purpose of this research was to predict the in vivo dissolution of lansoprazole from enteric coated pellets in the fasted state using a biorelevant flow-through dissolution method with low flow rates and volumes close to those in vivo. Additionally, a novel rotating stirring element, composed from magnet inserted in a silicone tube, was used to produce the movement of the pellets and expose them to slightly increased physical stress. Obtained dissolution results were compared to the dissolution results of our previous work using the USP IV with higher flow rate (11 ml/min). As drug release from enteric coated pellets usually starts in the small intestine, the influence of pellets' residence time in the gastric medium and additionally the effect of different media on drug release was studied. Prolongation of residence time in an acidic medium had only minor effect on the release rate after initial lag time, but significantly reduced the total amount of the drug released from both tested formulations, which was attributed to the drug's degradation in an acidic medium. The increased physical load on the pellets induced by the rotating stirring element compensated for the decrease of flow rate from 11 ml/min using the USP IV to 3 ml/min using the non-compendial system. Considering also gastric emptying kinetics good prediction of the in vivo release was achieved compared to in vivo absorption data obtained from a pharmacokinetic study under fasting conditions. Thus, using more physiologically relevant dissolution conditions, expressed through low volume and lower flow rate, and in combination with increased mechanical stress we obtained equally good in vitro/in vivo correlation as using USP IV and higher flow rates. Comparison of the dissolution results obtained with two different systems provided additional insight into product behaviour and improved prediction of in vivo performance.

Authors+Show Affiliations

KRKA d.d., Novo mesto, Šmarješka cesta 6, 8501 Novo Mesto, Slovenia.KRKA d.d., Novo mesto, Šmarješka cesta 6, 8501 Novo Mesto, Slovenia; Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia. Electronic address: marija.bogataj@ffa.uni-lj.si.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

24844699

Citation

Stefanič, M, et al. "Prediction of the in Vivo Performance of Enteric Coated Pellets in the Fasted State Under Selected Biorelevant Dissolution Conditions." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 62, 2014, pp. 8-15.
Stefanič M, Vrečer F, Rizmal P, et al. Prediction of the in vivo performance of enteric coated pellets in the fasted state under selected biorelevant dissolution conditions. Eur J Pharm Sci. 2014;62:8-15.
Stefanič, M., Vrečer, F., Rizmal, P., Mrhar, A., & Bogataj, M. (2014). Prediction of the in vivo performance of enteric coated pellets in the fasted state under selected biorelevant dissolution conditions. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 62, 8-15. https://doi.org/10.1016/j.ejps.2014.05.007
Stefanič M, et al. Prediction of the in Vivo Performance of Enteric Coated Pellets in the Fasted State Under Selected Biorelevant Dissolution Conditions. Eur J Pharm Sci. 2014 Oct 1;62:8-15. PubMed PMID: 24844699.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Prediction of the in vivo performance of enteric coated pellets in the fasted state under selected biorelevant dissolution conditions. AU - Stefanič,M, AU - Vrečer,F, AU - Rizmal,P, AU - Mrhar,A, AU - Bogataj,M, Y1 - 2014/05/15/ PY - 2014/01/30/received PY - 2014/04/29/revised PY - 2014/05/09/accepted PY - 2014/5/22/entrez PY - 2014/5/23/pubmed PY - 2015/3/31/medline KW - Biorelevant dissolution KW - Enteric coated pellets KW - Gastric emptying KW - IVIVC KW - Non-compendial system SP - 8 EP - 15 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 62 N2 - The purpose of this research was to predict the in vivo dissolution of lansoprazole from enteric coated pellets in the fasted state using a biorelevant flow-through dissolution method with low flow rates and volumes close to those in vivo. Additionally, a novel rotating stirring element, composed from magnet inserted in a silicone tube, was used to produce the movement of the pellets and expose them to slightly increased physical stress. Obtained dissolution results were compared to the dissolution results of our previous work using the USP IV with higher flow rate (11 ml/min). As drug release from enteric coated pellets usually starts in the small intestine, the influence of pellets' residence time in the gastric medium and additionally the effect of different media on drug release was studied. Prolongation of residence time in an acidic medium had only minor effect on the release rate after initial lag time, but significantly reduced the total amount of the drug released from both tested formulations, which was attributed to the drug's degradation in an acidic medium. The increased physical load on the pellets induced by the rotating stirring element compensated for the decrease of flow rate from 11 ml/min using the USP IV to 3 ml/min using the non-compendial system. Considering also gastric emptying kinetics good prediction of the in vivo release was achieved compared to in vivo absorption data obtained from a pharmacokinetic study under fasting conditions. Thus, using more physiologically relevant dissolution conditions, expressed through low volume and lower flow rate, and in combination with increased mechanical stress we obtained equally good in vitro/in vivo correlation as using USP IV and higher flow rates. Comparison of the dissolution results obtained with two different systems provided additional insight into product behaviour and improved prediction of in vivo performance. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/24844699/Prediction_of_the_in_vivo_performance_of_enteric_coated_pellets_in_the_fasted_state_under_selected_biorelevant_dissolution_conditions_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(14)00191-2 DB - PRIME DP - Unbound Medicine ER -