teferrol and ferric-hydroxide

The study was carried out as an open-label, laboratory-blind, single-dose, randomized, two-period crossover, isotope efficacy study. Twenty-two patients with iron-deficiency anemia were enrolled in the study. The study consisted of two treatment phases of 15 days each, including blood sample measurements for Fe-59 activity. The two treatments were given orally. Treatment A was Fe-59 labeled iron(III)-hydroxide polymaltose complex (IPC, Maltofer) equivalent to 100 mg elemental iron given orally. Treatment B consisted of Fe-59 labeled IPC complex equivalent to 100 mg elemental iron and 500 mg tetracycline HCl (CAS 64-75-5) given orally. No differences between the two treatment groups with regard to the erythrocyte iron uptake were found, and thus IPC can be used with tetracycline, if necessary.

Topics: Adult; Anemia, Iron-Deficiency; Anti-Bacterial Agents; Chemical Phenomena; Chemistry, Physical; Cross-Over Studies; Dietary Supplements; Drug Interactions; Erythrocyte Indices; Erythrocytes; Female; Ferric Compounds; Ferritins; Hemoglobins; Humans; Iron; Iron Chelating Agents; Iron Radioisotopes; Male; Middle Aged; Prospective Studies; Quality Control; Sample Size; Single-Blind Method; Tetracycline

MRI of lung parenchyma and pulmonary embolism (PE) remains challenging. "Ferrum," a ferric hydroxide sucrose complex used clinically for iron deficiency anemia for more than 40 years, was investigated as a negative MRI contrast agent in five rabbits bearing experimental PE as well as in five normal volunteers. Clots were prepared by spontaneous coagulation of 0.1 ml In-111 labeled autologous red blood cells and introduced through the jugular vein. Scintigraphic imaging permitted anatomical localization of PE in vivo and thereby served as a control for MR imaging. MRI was performed on a 1.5 T GE Signa scanner before and after induction of PE, and before and after the injection of Ferrum. T1-weighted images were obtained continuously for up to 90 min using varying doses of Ferrum. In five normal human volunteers, a single dose of 100 mg each was administered. T1- and T2-weighted spin-echo and gradient-echo images of lung parenchyma were repeatedly obtained before and after agent administration. In rabbit, Ferrum remained in circulation for several hours where it shortened both T1 and T2 of blood, improving the contrast between PE and lung parenchyma (i.e., intravascular compartment). A dose of 3 mg/kg was enough to increase the contrast-to-noise ratio (CNR) between PE and lung parenchyma by almost three fold, substantially improving lesion detectability. CNR increased up to five-fold when the dose was increased up to 20 mg/kg at which point CNR reached a plateau. In humans, T2-weighted spin-echo sequence appeared to be most sensitive to changes in signal-to-noise ratio (SNR) of normal lung parenchyma. Within 60 min after injection of 100 mg of iron, SNR dropped by 34% (p < .025). However, 24 hr later, SNR returned to almost normal. Ferrum increased the contrast between PE and lung parenchyma in the rabbit and decreased the parenchymal SNR in humans in nontoxic doses. These results suggest that Ferrum is worthy of further investigation of PE imaging in humans.

Topics: Aged; Animals; Contrast Media; Feasibility Studies; Ferric Compounds; Humans; Lung; Magnetic Resonance Imaging; Pulmonary Embolism; Rabbits; Time Factors

This paper reports a study of the pharmacokinetics of ferrous sulphate and ferric-hydroxide-polymaltose complex (Hw 6400, Ferrum Hausmann) administered orally and intravenously to anaemic and non-anaemic rats of both sexes. Radiolabelled ferrous sulphate and ferric-hydroxide-polymaltose complex was used to study iron utilization after oral administration. Measurements of radioactivity in serum, packed red cells, whole blood, liver, kidney, spleen, bone and in some cases in the gastrointestinal tract were made following a range of dosages between 0.84 and 41.9 mg Fe/kg. No significant difference in bioavailability or iron utilization was found between the two iron preparations. Pharmacokinetic measurements following i.v. administration showed different distribution volumes, iron clearance and elimination constants for the two preparations. This difference in pharmacokinetic behaviour following oral administration, particularly in the case of non-anaemic rats, was confirmed by the observation that a 10- to 20 fold smaller dose of FeSO4 than of iron-polymaltose complex was required to achieve the same rise in serum iron. It is therefore not justifiable to draw conclusions about the bioavailability of chemically different iron preparations (iron salts and iron hydroxide complexes) on the basis of AUC values for serum iron increases observed in non-anaemic animals or human subjects.

Topics: Administration, Oral; Anemia, Hypochromic; Animals; Female; Ferric Compounds; Ferrous Compounds; Injections, Intravenous; Intestinal Absorption; Iron; Kinetics; Male; Rats; Rats, Inbred Strains; Tissue Distribution