J Korean Soc Magn Reson Med.  2013 Dec;17(4):259-266. 10.13104/jksmrm.2013.17.4.259.

Pharmacokinetics and Bio-distribution of New Gd-complexes of DTPA-bis (amide) (L3) in a Rat Model

Affiliations
  • 1Department of Radiology, the Second Affiliated Hospital, Shantou University Medical College, Shantou 515041, PR China.
  • 2Department of Radiology & Molecular Medicine, Kyungpook National University, Daegu, Korea. ychang@knu.ac.kr
  • 3Department of Radiology, Bogang Hospital, Daegu, Korea.

Abstract

PURPOSE
To investigate the blood pharmacokinetics and bio-distribution of DTPA-bis-amide (L3) Gd(III) complexes.
MATERIALS AND METHODS
The pharmacokinetics and bio-distribution of Gd (L3)(H2O).nH2O were investigated in Sprague-Dawley rats after intravenous administration at a dose of 0.1 mmol Gd/kg. The Gd content in the blood, various tissues, and organs was determined by ICP-AES. Blood pharmacokinetic parameters were calculated using a two-compartment model.
RESULTS
The half-lives of alphaphase and betaphase Gd (L3)(H2O).nH2O were 2.286+/-0.11 min and 146.1+/-7.5 min, respectively. The bio-distribution properties reveal that the complex is mainly excreted by the renal pathway, and possibly excreted by the hepatobiliary route. The concentration ratio of Gd (III) was significantly higher in the liver and spleen than in other organs, and small amounts of Gd (III) ion were detected in the blood or other tissues of rats only after 7 days of intravenous administration.
CONCLUSION
The MRI contrast agent Gd (L3)(H2O).nH2O provides prolonged blood pool retention in the circulation and then clears rapidly with minimal accumulation of Gd(III) ions. The synthesis of gadolinium complexes with well-balanced lipophilicity and hydrophilicity shows promise for their further development as blood pool MRI contrast agents.

Keyword

Pharmacokinetics; MRI contrast agent; DTPA-bis (amide) (L3); Magnetic resonance imaging (MRI)

MeSH Terms

Administration, Intravenous
Animals
Contrast Media
Gadolinium
Hydrophobic and Hydrophilic Interactions
Ions
Liver
Magnetic Resonance Imaging
Models, Animal*
Pharmacokinetics*
Rats*
Rats, Sprague-Dawley
Spleen
Contrast Media
Gadolinium
Ions
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