Comparison study of oral iron preparations using a human intestinal model

Mohammed Gulrez Zariwala, Satyanarayana Somavarapu, Sebastien Farnaud, Derek Renshaw

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Iron deficiency and related iron deficiency anaemia (IDA) are the most prevalent nutritional disorders worldwide. The standard treatment involves supplementation 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 considered 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 preparations, 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.

Original languageEnglish
Pages (from-to)1123-39
Number of pages17
JournalScientia Pharmaceutica
Volume81
Issue number4
DOIs
Publication statusPublished - 21 Jun 2013
Externally publishedYes

Fingerprint

Iron
ferrous sulfate
Tablets
Nutrition Disorders
Caco-2 Cells
Iron-Deficiency Anemias
Ferritins
Capsules
Adenocarcinoma
Salts
Epithelial Cells
Cell Line

Keywords

  • Anaemia
  • Dissolution
  • Caco-2
  • Ferritin
  • Iron supplements

Cite this

Comparison study of oral iron preparations using a human intestinal model. / Zariwala, Mohammed Gulrez; Somavarapu, Satyanarayana; Farnaud, Sebastien; Renshaw, Derek.

In: Scientia Pharmaceutica, Vol. 81, No. 4, 21.06.2013, p. 1123-39.

Research output: Contribution to journalArticle

Zariwala, Mohammed Gulrez ; Somavarapu, Satyanarayana ; Farnaud, Sebastien ; Renshaw, Derek. / Comparison study of oral iron preparations using a human intestinal model. In: Scientia Pharmaceutica. 2013 ; Vol. 81, No. 4. pp. 1123-39.
@article{5a80097d169c4f59b0cba05e85ab3299,
title = "Comparison study of oral iron preparations using a human intestinal model",
abstract = "Iron deficiency and related iron deficiency anaemia (IDA) are the most prevalent nutritional disorders worldwide. The standard treatment involves supplementation 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 considered 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 preparations, 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",
author = "Zariwala, {Mohammed Gulrez} and Satyanarayana Somavarapu and Sebastien Farnaud and Derek Renshaw",
year = "2013",
month = "6",
day = "21",
doi = "10.3797/scipharm.1304-03",
language = "English",
volume = "81",
pages = "1123--39",
journal = "Scientia Pharmaceutica",
issn = "0036-8709",
publisher = "{\"O}sterreichischer Apothekerverlag",
number = "4",

}

TY - JOUR

T1 - Comparison study of oral iron preparations using a human intestinal model

AU - Zariwala, Mohammed Gulrez

AU - Somavarapu, Satyanarayana

AU - Farnaud, Sebastien

AU - Renshaw, Derek

PY - 2013/6/21

Y1 - 2013/6/21

N2 - Iron deficiency and related iron deficiency anaemia (IDA) are the most prevalent nutritional disorders worldwide. The standard treatment involves supplementation 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 considered 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 preparations, 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.

AB - Iron deficiency and related iron deficiency anaemia (IDA) are the most prevalent nutritional disorders worldwide. The standard treatment involves supplementation 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 considered 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 preparations, 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.

KW - Anaemia

KW - Dissolution

KW - Caco-2

KW - Ferritin

KW - Iron supplements

U2 - 10.3797/scipharm.1304-03

DO - 10.3797/scipharm.1304-03

M3 - Article

VL - 81

SP - 1123

EP - 1139

JO - Scientia Pharmaceutica

JF - Scientia Pharmaceutica

SN - 0036-8709

IS - 4

ER -