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Sci. Pharm. 2013, 81(4), 1123-1140; doi:10.3797/scipharm.1304-03

Comparison Study of Oral Iron Preparations Using a Human Intestinal Model

1
Department of Human & Health Sciences, School of Life Sciences, University of Westminster, 115 New Cavendish Street, London, W1W 6UW, UK
2
Department of Pharmaceutics, UCL School of Pharmacy, 29–39 Brunswick Square, London, WC1N 1AX, UK
3
Department of Life Sciences, University of Bedfordshire, Park Square, Luton, LU1 3JU, UK
§
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 4 April 2013 / Accepted: 21 June 2013 / Published: 21 June 2013
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Abstract

Iron deficiency and related iron deficiency anaemia (IDA) are the most prevalent nutritional disorders worldwide. The standard treatment involves supple-mentation with solid or liquid iron supplement preparations, usually based on a ferrous salt such as ferrous sulphate, ferrous fumarate, or ferrous gluconate. In the present study, we compared iron uptake and absorption from various solid and liquid iron supplement preparations currently available in the United Kingdom using the well-characterised human epithelial adenocarcinoma cell line Caco-2. Intracellular ferritin protein formation by the Caco-2 cell was con-sidered an indicator of cellular iron uptake and absorption. We investigated the effects of formulation ingredients at a defined pH on iron uptake and absorption, and designed a novel two-stage dissolution-absorption protocol that mimicked physiological conditions. Our experiments revealed wide variations in the rate of dissolution between the various solid iron preparations. Conventional-release ferrous iron tablets dissolved rapidly (48 ± 4 mins to 64 ± 4 mins), whereas modified-released tablets and capsules took significantly longer to undergo complete dissolution (274 ± 8 to 256 ± 8 mins). Among the solid iron prepa-rations, ferrous sulphate conventional-release tablets demonstrated the highest iron absorption, whereas modified-release ferrous preparations demonstrated uniformly low iron absorption, as compared to the control (P < 0.05). Taken together, our results demonstrate that there are wide-ranging variations in dissolution times and iron uptake from oral iron preparations, with the physical characteristics of the preparation as well as the form of iron playing a key role.
Keywords: Anaemia; Dissolution; Caco-2; Ferritin; Iron Supplements Anaemia; Dissolution; Caco-2; Ferritin; Iron Supplements
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

ZARIWALA, M.G.; SOMAVARAPU, S.; FARNAUD, S.; RENSHAW, D. Comparison Study of Oral Iron Preparations Using a Human Intestinal Model. Sci. Pharm. 2013, 81, 1123-1140.

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