Drug Res (Stuttg)
DOI: 10.1055/s-0043-113636
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Iron Pharmacokinetics in Women with Iron Deficiency Anaemia Following A Single Oral Dose of a Novel Formulation of Tardyferon (Prolonged Release Ferrous Sulphate)

Andrew Leary1, Laurence Barthe2, Thierry Clavel2, Claudie Sanchez2, Zahida Issiakhem2, Bruno Paillard2, Jean-Marc Edmond2
  • 1Department of Pharmacology & Therapeutics, University College Cork, Ireland
  • 2Pierre Fabre Médicament, Boulogne, France
Further Information

Publication History

received 12 May 2017

accepted 10 June 2017

Publication Date:
19 July 2017 (eFirst)

Abstract

Numerous iron-containing preparations are available on the market; these vary in dosage, salt, chemical state of iron (ferric or ferrous) and in the iron delivery process (immediate or prolonged-release). Tardyferon® is a prolonged-release tablet containing 80 mg ferrous sulphate. The formulation has recently been modified; changes to the excipients which constitute the inert formulation matrix have allowed a decrease in tablet size for easier swallowing. The aim of this multicenter open-label study was to characterize the serum pharmacokinetics of iron in non-pregnant women aged 23–45 years with iron deficiency anaemia (IDA) following single oral administration of 160 mg Tardyferon® under fasting conditions. Blood samples were collected from the 29 participants before dosing and until 24 h post-dosing. Serum iron concentrations were determined using a routine colorimetric analytical method; pharmacokinetic parameters were derived using a non-compartmental approach. In these patients, median time to maximum serum concentrations (Tmax) was 4 h. Serum profiles were consistent with prolonged release; iron levels were elevated up to 12 h after dosing, with mean C12h still more than 7 times higher than baseline (CT0), and mean C2h and C8h representing 69.7% and 81.9% of the Cmax, respectively. In vitro dissolution testing performed on the clinical batch also demonstrated prolonged release of iron from this formulation. A single oral dose of 160 mg Tardyferon® administered under fasting conditions to this target population resulted in a long-lasting release of iron in the gastrointestinal tract, leading to optimal iron absorption. Moreover, Tardyferon® was well tolerated.