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Interaction between fed gastric media (Ensure Plus®) and different hypromellose based caffeine controlled release tablets: comparison and mechanistic study of caffeine release in fed and fasted media versus water using the USP dissolution apparatus 3.
Int J Pharm. 2014 Jan 30; 461(1-2):419-26.IJ

Abstract

The aim of the study was to investigate caffeine release in fed and fasted state media from three controlled release matrix tablets containing different HPMC viscosity grades. The biorelevant in vitro dissolution methods utilize the USP 3 dissolution apparatus and biorelevant media to simulate fed and fasted gastro-intestinal dissolution conditions. The effect of tablet reciprocation rate (dip speed) in dissolution media (10 and 15 dips per minute) and media (water, fed and fasted) on caffeine release rate from - and erosion rate of - 100, 4000 and 15,000 mPa s HPMC viscosity tablets was investigated using factorial designed experiments. Furthermore, the mechanism of release in Ensure Plus(®), a nutrition drink similar in composition to the FDA standard meal, was investigated by studying tablet swelling using texture analysis. Altering dip speed has negligible effect on release and erosion rates. Using fasted media instead of water slightly decreases caffeine release from 100 and 4000 mPa s HPMC viscosity tablets as well as erosion rates, while 15,000 mPa s tablets remain unaffected. Fed compared to fasted media decreases caffeine release rate, and the food effect is greater for the 100 mPa s viscosity tablets compared to the 4000 and 15,000 mPa s viscosity tablets. The investigation using texture analysis indicates that Ensure Plus(®) becomes rate-limiting for caffeine release from HPMC tablets by forming a hydrophobic barrier around the tablets. The barrier decreases tablet water permeation, which decreases erosion rate in 100 mPa s viscosity tablets, swelling in 15,000 mPa s viscosity tablets and caffeine release from both tablets. This observed interaction between Ensure Plus(®) and the HPMC tablets may translate into decreased drug release rate in the fed stomach, which may decrease the amount of drug available for absorption in the small intestine and thus reduce systemic drug exposure and maximum plasma concentration.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Franek F
Section for Pharmaceutical Design and Drug Delivery, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 København Ø, Denmark.
Holm P
Biologics and Pharmaceutical Science, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark.
Larsen F
Clinical Pharmacology, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark.
Steffansen B
Section for Pharmaceutical Design and Drug Delivery, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 København Ø, Denmark. Electronic address: bente.steffansen@sund.ku.dk.

MeSH

CaffeineChemistry, PharmaceuticalDelayed-Action PreparationsExcipientsHydrophobic and Hydrophilic InteractionsHypromellose DerivativesSolubilityTabletsViscosityVitamin KWater

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24342711

Citation

Franek, Frans, et al. "Interaction Between Fed Gastric Media (Ensure Plus®) and Different Hypromellose Based Caffeine Controlled Release Tablets: Comparison and Mechanistic Study of Caffeine Release in Fed and Fasted Media Versus Water Using the USP Dissolution Apparatus 3." International Journal of Pharmaceutics, vol. 461, no. 1-2, 2014, pp. 419-26.
Franek F, Holm P, Larsen F, et al. Interaction between fed gastric media (Ensure Plus®) and different hypromellose based caffeine controlled release tablets: comparison and mechanistic study of caffeine release in fed and fasted media versus water using the USP dissolution apparatus 3. Int J Pharm. 2014;461(1-2):419-26.
Franek, F., Holm, P., Larsen, F., & Steffansen, B. (2014). Interaction between fed gastric media (Ensure Plus®) and different hypromellose based caffeine controlled release tablets: comparison and mechanistic study of caffeine release in fed and fasted media versus water using the USP dissolution apparatus 3. International Journal of Pharmaceutics, 461(1-2), 419-26. https://doi.org/10.1016/j.ijpharm.2013.12.003
Franek F, et al. Interaction Between Fed Gastric Media (Ensure Plus®) and Different Hypromellose Based Caffeine Controlled Release Tablets: Comparison and Mechanistic Study of Caffeine Release in Fed and Fasted Media Versus Water Using the USP Dissolution Apparatus 3. Int J Pharm. 2014 Jan 30;461(1-2):419-26. PubMed PMID: 24342711.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Interaction between fed gastric media (Ensure Plus®) and different hypromellose based caffeine controlled release tablets: comparison and mechanistic study of caffeine release in fed and fasted media versus water using the USP dissolution apparatus 3. AU - Franek,Frans, AU - Holm,Per, AU - Larsen,Frank, AU - Steffansen,Bente, Y1 - 2013/12/14/ PY - 2013/08/22/received PY - 2013/12/04/revised PY - 2013/12/06/accepted PY - 2013/12/18/entrez PY - 2013/12/18/pubmed PY - 2015/10/1/medline KW - Caffeine (PubChem CID: 2519) KW - F(i) KW - FaSSGF KW - FaSSIF KW - FeSSIF KW - Food effects KW - HPMC KW - SCoF KW - Texture analysis KW - b KW - dips per minute KW - dissolution profile shape-parameter KW - dpm KW - fasted state simulated gastric fluid KW - fasted state simulated intestinal fluid KW - fed state simulated intestinal fluid KW - maximal resistance to probe penetration into the tablet KW - simulated colonic fluid KW - t(63) KW - time when 63.2% of drug has been released SP - 419 EP - 26 JF - International journal of pharmaceutics JO - Int J Pharm VL - 461 IS - 1-2 N2 - The aim of the study was to investigate caffeine release in fed and fasted state media from three controlled release matrix tablets containing different HPMC viscosity grades. The biorelevant in vitro dissolution methods utilize the USP 3 dissolution apparatus and biorelevant media to simulate fed and fasted gastro-intestinal dissolution conditions. The effect of tablet reciprocation rate (dip speed) in dissolution media (10 and 15 dips per minute) and media (water, fed and fasted) on caffeine release rate from - and erosion rate of - 100, 4000 and 15,000 mPa s HPMC viscosity tablets was investigated using factorial designed experiments. Furthermore, the mechanism of release in Ensure Plus(®), a nutrition drink similar in composition to the FDA standard meal, was investigated by studying tablet swelling using texture analysis. Altering dip speed has negligible effect on release and erosion rates. Using fasted media instead of water slightly decreases caffeine release from 100 and 4000 mPa s HPMC viscosity tablets as well as erosion rates, while 15,000 mPa s tablets remain unaffected. Fed compared to fasted media decreases caffeine release rate, and the food effect is greater for the 100 mPa s viscosity tablets compared to the 4000 and 15,000 mPa s viscosity tablets. The investigation using texture analysis indicates that Ensure Plus(®) becomes rate-limiting for caffeine release from HPMC tablets by forming a hydrophobic barrier around the tablets. The barrier decreases tablet water permeation, which decreases erosion rate in 100 mPa s viscosity tablets, swelling in 15,000 mPa s viscosity tablets and caffeine release from both tablets. This observed interaction between Ensure Plus(®) and the HPMC tablets may translate into decreased drug release rate in the fed stomach, which may decrease the amount of drug available for absorption in the small intestine and thus reduce systemic drug exposure and maximum plasma concentration. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/24342711/Interaction_between_fed_gastric_media__Ensure_Plus®__and_different_hypromellose_based_caffeine_controlled_release_tablets:_comparison_and_mechanistic_study_of_caffeine_release_in_fed_and_fasted_media_versus_water_using_the_USP_dissolution_apparatus_3_ DB - PRIME DP - Unbound Medicine ER -