PMID: 11604268Oct 18, 2001Paper

Citric acid as excipient in multiple-unit enteric-coated tablets for targeting drugs on the colon

International Journal of Pharmaceutics
P NykänenM Marvola

Abstract

Delivery of drugs to the large bowel has been extensively investigated during the last decade. The aim of this study was to investigate whether enteric-coated tablets could be made from enteric-coated matrix granules and drug release targeted to the colon. Whether in vitro drug release rate and in vivo absorption could be delayed by adding citric acid to the granules and/or to the tablet matrix was also studied. Ibuprofen was used as model drug because it is absorbed throughout the gastrointestinal tract. Eudragit S and Aqoat AS-HF were used as enteric polymers. Drug release rates were studied at different pH levels and drug absorption was studied in bioavailability tests. The conclusion was that citric acid retarded in vitro drug release when used in multiple-unit tablets. In vivo absorption of ibuprofen was markedly delayed when citric acid was included in both granules and tablet matrix. Further studies are needed to determine the optimal amount of citric acid in formulations.

References

Jan 1, 1995·Critical Reviews in Therapeutic Drug Carrier Systems·A Rubinstein
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Dec 10, 1998·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·M MarvolaA Autere
Jan 14, 1999·Journal of Drug Targeting·R KingetG van den Mooter
Jul 1, 1999·International Journal of Pharmaceutics·P NykänenM Marvola

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Citations

Feb 19, 2004·Advanced Drug Delivery Reviews·Tamara Minko
Jun 4, 2013·International Journal of Pharmaceutics·Alessandra MaroniAndrea Gazzaniga
Jul 25, 2003·International Journal of Pharmaceutics·Pieter van der Bijl, Armorel D van Eyk
Apr 10, 2013·Drug Design, Development and Therapy·Aleksander MendykRenata Jachowicz
Nov 1, 2012·Indian Journal of Pharmaceutical Sciences·N R KotagaleM J Umekar
Jan 11, 2011·Indian Journal of Pharmaceutical Sciences·N R KotagaleM J Umekar
Oct 30, 2013·International Journal of Pharmaceutical Investigation·Neha S RautNandkishor Ramdas Kotagale
Sep 10, 2014·Expert Opinion on Drug Delivery·Aleksandar AleksovskiOdon Planinšek
Nov 3, 2007·The Journal of Pharmacy and Pharmacology·Sandra U SchillingJames W McGinity
Dec 24, 2005·Expert Opinion on Drug Delivery·Guy Van den Mooter
May 1, 2010·Pharmaceutical Development and Technology·Ghassan Z AbdullahAzmin M Noor
Mar 20, 2010·Pharmaceutical Development and Technology·Nandkishor KotagaleChirag J Patel
Oct 15, 2013·Advanced Drug Delivery Reviews·Tamara MinkoVitaly Pozharov
Oct 16, 2002·World Journal of Gastroenterology : WJG·Yi-Nuo PangZhi-Rong Zhang
Dec 14, 2011·Chemical Society Reviews·Jayant KhandareRainer Haag
Jan 12, 2021·Pharmaceutical Development and Technology·Wipada SamprasitBenchawan Chamsai
Jun 20, 2020·Drug Discovery Today·Annemarie BroesderWouter L J Hinrichs

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