The influence of gastric emptying kinetics on the drug release from enteric coated pellets in fasted state: An in vitro/in vivo correlation

Štefanič, Marko (author), Locatelli, Igor (author), Vrečer, Franc (author), Sever, Tanja (author), Mrhar, Aleš (author), Bogataj, Marija (author)

The absorption and bioavailability of drugs can be substantially affected by the transit of dosage forms 25 through the gastrointestinal (GI) tract. Gastric emptying is one of the most critical parameters contribut- 26 ing to this inter- and intra-individual GI transit variability. It is especially important for the delayed 27 release dosage forms whose release depends on thelocal environment and begins when the dosage form 28 passes pylorus and comes into contact with higher pH medium in small intestine. The purpose of our 29 research work was to predict the in vivo dissolution from enteric coated pellets for population and 30 establish a good in vitro/in vivo correlation (IVIVC) with mean in vivo absorption profiles, obtained in a 31 pharmacokinetic study under fasting conditions. The dissolution tests were carried out on a USP 4 - 32 flow-through cell with enteric coated pellets containing an acid-labile drug and formulated as orodispers- 33 ible tablets. Using several residence times in an acidic medium, we simulated the gastric emptying of the 34 pellets and the exposure of different fractions of the pellets to the gastric medium for different periods of 35 time. The amount of drug released decreased with the increasing time of exposure to the acidic medium 36 due to the drugʼs degradation. The mean in vivo dissolution profiles, which were predicted on the basis of 37 experimentally determined dissolution profiles and mathematical model of pelletsʼ gastric emptying, 38 gave a very good IVIVC with the mean in vivo absorption profiles.

• Language: English
• Keywords: In vitro dissolution, gastric emptying, In vivo dissolution, multiparticulate systems
• Work type: Not categorized (r6)
• Tipology: 1.01 - Original Scientific Article
• Organization: FFA - Faculty of Pharmacy
• Year: 2012
• Number of pages: str. 376-382
• Numbering: Vol. 82, issue 2
• UDC: 542.9:615.015
• ISSN on article: 0939-6411
• DOI: 10.1016/j.ejpb.2012.07.011
• COBISS.SI-ID: 3286385
• Average score: (0 votes)
• Your score: Voting is allowed only to logged in users.

Record is a part of a journal

• Title: European journal of pharmaceutics and biopharmaceutics
• Shortened title: Eur. j. pharm. biopharm.
• Publisher: Wiss. Verl.-Ges.
• ISSN: 0939-6411
• COBISS.SI-ID: 13176839