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Nuklearmedizin 2018; 57(06): 242-246
DOI: 10.3413/Nukmed-0933-18-08
Original Article
Georg Thieme Verlag KG Stuttgart · New York

Examination of the complexation ability of different calixarene derivatives towards [223Ra]RaCl2 in a hospital radiopharmaceutical laboratory

Untersuchung der Komplexierungsfähigkeit verschiedener Calixarenderivate gegenüber [223Ra] RaCl2 in einem radiopharmazeutischen Labor eines Krankenhauses
Martin Freesmeyer
1   Klinik für Nuklearmedizin, Universitätsklinikum Jena, Am Klinikum 1, 07747 Jena, Germany
,
Wolfgang Weigand
2   Institut für Anorganische und Analytische Chemie, Friedrich-Schiller Universität Jena, Humboldt-Straße 8, 07743 Jena, Germany
,
Thomas Weisheit
1   Klinik für Nuklearmedizin, Universitätsklinikum Jena, Am Klinikum 1, 07747 Jena, Germany
› Author Affiliations
Further Information

Publication History

received: 21 August 2018

accepted: 28 September 2018

Publication Date:
14 December 2018 (online)

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Summary

Aim: In this contribution we investigated the potential transfer of an established method for the synthesis of 223Ra-labelled calixarene complexes to a hospital radiopharmaceutical environment. For this purpose, commercially available [223Ra]RaCl2 solution in pharmaceutical grade (Xofigo®) was reacted with three calixarene derivatives. Methods: A wellestablished two-phase extraction method using a two-phase solvent system was performed for complexation of the radium ions with calixarenes under slightly basic conditions. Moreover, the complexation reaction was conducted in homogenous medium (water / THF) as well as under elevated temperature. Results: The investigated reaction conditions did not allow the isolation of the desired products. Analytical evidence for the presence of radium-calixarene species by means of activity measurement, TLC as well as HPLC could not been proven unambiguously. Conclusion: We address the non-conversion of the educts to the large excess of sodium ions in the used Xofigo® solution, what may explain the hampered reaction for all conducted experiments. Finally the transfer of the published complexation concept into a radiopharmaceutical routine environment was not successful.

Zusammenfassung

Ziel: Ziel der vorliegenden Arbeit ist es, eine bekannte Methode zur Synthese von 223Ramarkierten Calixaren-Komplexen zunächst auf ihre Reproduzierbarkeit zu prüfen und gegebenenfalls für die Anwendung in einem radiopharmazeutischen Arbeitsbereich einer Klinik zu adaptieren. Als Ausgangsnuklid wurde kommerziell verfügbares [223Ra]RaCl2 in pharmazeutischer Qualität (Xofigo®) eingesetzt. Dieses wurde mit verschiedenen Calixarenderivaten umgesetzt. Methoden: Die Komplexierungsreaktion wurde sowohl mittels einer in der Literatur beschriebenen Zwei-Phasen-Extraktion als auch in einem homogenen Lösungsmittelgemisch (THF/Wasser) bei schwach basischen Bedingungen durchgeführt. Weiterhin wurde die Reaktionstemperatur variiert. Resultate: Bei keiner der durchgeführten Umsetzungen konnte die Bildung des postulierten Produkts durch spezifische Analysenmethoden wie Aktivitätsmessung, Radio-Dünnschichtchromatographie-Scans sowie Hochleistungsflüssigkeitschromatographie (HPLC) nachgewiesen werden. Schlussfolgerungen: Das Ausbleiben der Komplexierung ist wahrscheinlich auf den extrem hohen Überschuss an Natriumionen in der verwendeten Xofigo®-Lösung zurückzuführen. Die Anwendung der publizierten Komplexierungsmethode in einem radiopharmazeutischen Kliniklabor ist nicht möglich.

Keywords

Radium dichloride - Calixarene

Schlüsselwörter

Radiumdichlorid - Calixaren
 

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