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Rationale for ibuprofen co-administration with antacids: Potential interaction mechanisms affecting drug absorption

Authorized Users Only
2008
Authors
Parojčić, Jelena
Corrigan, Owen I.
Article (Published version)
Metadata
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Abstract
Ibuprofen is a widely used NSAID which is often co-administered with antacids because of its gastro-irritant effects. Literature data suggest that antacid interactions may increase or decrease the drug's absorption rate and onset of action and that the interaction may be formulation specific. In the present study, literature data on ibuprofen absorption were evaluated in order to gain insight into the nature of the in vivo effect. Solubility determinations in reactive media containing magnesium or aluminium and dissolution studies in the presence of antacid suspension were performed in an attempt to simulate in vitro the effects observed in vivo. The results obtained indicate that magnesium hydroxide enhances ibuprofen solubility, dissolution and bioavailability, while aluminium hydroxide has a retarding effect. Solubility studies indicated formation of a soluble solid ibuprofen phase in the presence of Mg2+, in contrast, an insoluble ibuprofen salt was formed with Al3+. The introducti...on of magnesium based antacid suspension into the dissolution media resulted in a formulation specific increase in drug dissolution rate with the most pronounced effect observed for the slowest release tablet formulation. The results obtained indicate the potential for in vitro studies to predict physicochemical interactions that are likely to influence drug absorption rate in vivo.

Keywords:
ibuprofen-antacid interaction / absorption rate / solubility / dissolution / in vitro-in vivo correlation
Source:
European Journal of Pharmaceutics and Biopharmaceutics, 2008, 69, 2, 640-647
Publisher:
  • Elsevier Science BV, Amsterdam

DOI: 10.1016/j.ejpb.2008.01.001

ISSN: 0939-6411

PubMed: 18595674

WoS: 000256710000026

Scopus: 2-s2.0-43349105478
[ Google Scholar ]
12
62
URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/1076
Collections
  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy
TY  - JOUR
AU  - Parojčić, Jelena
AU  - Corrigan, Owen I.
PY  - 2008
UR  - http://farfar.pharmacy.bg.ac.rs/handle/123456789/1076
AB  - Ibuprofen is a widely used NSAID which is often co-administered with antacids because of its gastro-irritant effects. Literature data suggest that antacid interactions may increase or decrease the drug's absorption rate and onset of action and that the interaction may be formulation specific. In the present study, literature data on ibuprofen absorption were evaluated in order to gain insight into the nature of the in vivo effect. Solubility determinations in reactive media containing magnesium or aluminium and dissolution studies in the presence of antacid suspension were performed in an attempt to simulate in vitro the effects observed in vivo. The results obtained indicate that magnesium hydroxide enhances ibuprofen solubility, dissolution and bioavailability, while aluminium hydroxide has a retarding effect. Solubility studies indicated formation of a soluble solid ibuprofen phase in the presence of Mg2+, in contrast, an insoluble ibuprofen salt was formed with Al3+. The introduction of magnesium based antacid suspension into the dissolution media resulted in a formulation specific increase in drug dissolution rate with the most pronounced effect observed for the slowest release tablet formulation. The results obtained indicate the potential for in vitro studies to predict physicochemical interactions that are likely to influence drug absorption rate in vivo.
PB  - Elsevier Science BV, Amsterdam
T2  - European Journal of Pharmaceutics and Biopharmaceutics
T1  - Rationale for ibuprofen co-administration with antacids: Potential interaction mechanisms affecting drug absorption
VL  - 69
IS  - 2
SP  - 640
EP  - 647
DO  - 10.1016/j.ejpb.2008.01.001
ER  - 
@article{
author = "Parojčić, Jelena and Corrigan, Owen I.",
year = "2008",
url = "http://farfar.pharmacy.bg.ac.rs/handle/123456789/1076",
abstract = "Ibuprofen is a widely used NSAID which is often co-administered with antacids because of its gastro-irritant effects. Literature data suggest that antacid interactions may increase or decrease the drug's absorption rate and onset of action and that the interaction may be formulation specific. In the present study, literature data on ibuprofen absorption were evaluated in order to gain insight into the nature of the in vivo effect. Solubility determinations in reactive media containing magnesium or aluminium and dissolution studies in the presence of antacid suspension were performed in an attempt to simulate in vitro the effects observed in vivo. The results obtained indicate that magnesium hydroxide enhances ibuprofen solubility, dissolution and bioavailability, while aluminium hydroxide has a retarding effect. Solubility studies indicated formation of a soluble solid ibuprofen phase in the presence of Mg2+, in contrast, an insoluble ibuprofen salt was formed with Al3+. The introduction of magnesium based antacid suspension into the dissolution media resulted in a formulation specific increase in drug dissolution rate with the most pronounced effect observed for the slowest release tablet formulation. The results obtained indicate the potential for in vitro studies to predict physicochemical interactions that are likely to influence drug absorption rate in vivo.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
title = "Rationale for ibuprofen co-administration with antacids: Potential interaction mechanisms affecting drug absorption",
volume = "69",
number = "2",
pages = "640-647",
doi = "10.1016/j.ejpb.2008.01.001"
}
Parojčić J, Corrigan OI. Rationale for ibuprofen co-administration with antacids: Potential interaction mechanisms affecting drug absorption. European Journal of Pharmaceutics and Biopharmaceutics. 2008;69(2):640-647
Parojčić, J.,& Corrigan, O. I. (2008). Rationale for ibuprofen co-administration with antacids: Potential interaction mechanisms affecting drug absorption.
European Journal of Pharmaceutics and BiopharmaceuticsElsevier Science BV, Amsterdam., 69(2), 640-647.
https://doi.org/10.1016/j.ejpb.2008.01.001
Parojčić Jelena, Corrigan Owen I., "Rationale for ibuprofen co-administration with antacids: Potential interaction mechanisms affecting drug absorption" 69, no. 2 (2008):640-647,
https://doi.org/10.1016/j.ejpb.2008.01.001 .

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