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The influence of gastric emptying kinetics on the drug release from enteric coated pellets in fasted state: an in vitro/in vivo correlation.
Eur J Pharm Biopharm. 2012 Oct; 82(2):376-82.EJ

Abstract

The absorption and bioavailability of drugs can be substantially affected by the transit of dosage forms through the gastrointestinal (GI) tract. Gastric emptying is one of the most critical parameters contributing to this inter- and intra-individual GI transit variability. It is especially important for the delayed release dosage forms whose release depends on the local environment and begins when the dosage form passes pylorus and comes into contact with higher pH medium in small intestine. The purpose of our research work was to predict the in vivo dissolution from enteric coated pellets for population and establish a good in vitro/in vivo correlation (IVIVC) with mean in vivo absorption profiles, obtained in a pharmacokinetic study under fasting conditions. The dissolution tests were carried out on a USP 4 - flow-through cell with enteric coated pellets containing an acid-labile drug and formulated as orodispersible tablets. Using several residence times in an acidic medium, we simulated the gastric emptying of the pellets and the exposure of different fractions of the pellets to the gastric medium for different periods of time. The amount of drug released decreased with the increasing time of exposure to the acidic medium due to the drug's degradation. The mean in vivo dissolution profiles, which were predicted on the basis of experimentally determined dissolution profiles and mathematical model of pellets' gastric emptying, gave a very good IVIVC with the mean in vivo absorption profiles.

Authors+Show Affiliations

KRKA d.d., Novo mesto, Slovenia.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22884655

Citation

Stefanič, M, et al. "The Influence of Gastric Emptying Kinetics On the Drug Release From Enteric Coated Pellets in Fasted State: an in Vitro/in Vivo Correlation." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 82, no. 2, 2012, pp. 376-82.
Stefanič M, Locatelli I, Vrečer F, et al. The influence of gastric emptying kinetics on the drug release from enteric coated pellets in fasted state: an in vitro/in vivo correlation. Eur J Pharm Biopharm. 2012;82(2):376-82.
Stefanič, M., Locatelli, I., Vrečer, F., Sever, T., Mrhar, A., & Bogataj, M. (2012). The influence of gastric emptying kinetics on the drug release from enteric coated pellets in fasted state: an in vitro/in vivo correlation. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 82(2), 376-82. https://doi.org/10.1016/j.ejpb.2012.07.011
Stefanič M, et al. The Influence of Gastric Emptying Kinetics On the Drug Release From Enteric Coated Pellets in Fasted State: an in Vitro/in Vivo Correlation. Eur J Pharm Biopharm. 2012;82(2):376-82. PubMed PMID: 22884655.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The influence of gastric emptying kinetics on the drug release from enteric coated pellets in fasted state: an in vitro/in vivo correlation. AU - Stefanič,M, AU - Locatelli,I, AU - Vrečer,F, AU - Sever,T, AU - Mrhar,A, AU - Bogataj,M, Y1 - 2012/08/01/ PY - 2012/02/14/received PY - 2012/07/17/revised PY - 2012/07/19/accepted PY - 2012/8/14/entrez PY - 2012/8/14/pubmed PY - 2013/6/29/medline SP - 376 EP - 82 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 82 IS - 2 N2 - The absorption and bioavailability of drugs can be substantially affected by the transit of dosage forms through the gastrointestinal (GI) tract. Gastric emptying is one of the most critical parameters contributing to this inter- and intra-individual GI transit variability. It is especially important for the delayed release dosage forms whose release depends on the local environment and begins when the dosage form passes pylorus and comes into contact with higher pH medium in small intestine. The purpose of our research work was to predict the in vivo dissolution from enteric coated pellets for population and establish a good in vitro/in vivo correlation (IVIVC) with mean in vivo absorption profiles, obtained in a pharmacokinetic study under fasting conditions. The dissolution tests were carried out on a USP 4 - flow-through cell with enteric coated pellets containing an acid-labile drug and formulated as orodispersible tablets. Using several residence times in an acidic medium, we simulated the gastric emptying of the pellets and the exposure of different fractions of the pellets to the gastric medium for different periods of time. The amount of drug released decreased with the increasing time of exposure to the acidic medium due to the drug's degradation. The mean in vivo dissolution profiles, which were predicted on the basis of experimentally determined dissolution profiles and mathematical model of pellets' gastric emptying, gave a very good IVIVC with the mean in vivo absorption profiles. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/22884655/The_influence_of_gastric_emptying_kinetics_on_the_drug_release_from_enteric_coated_pellets_in_fasted_state:_an_in_vitro/in_vivo_correlation_ DB - PRIME DP - Unbound Medicine ER -