Radiopharmaceutical development of a freeze-dried kit formulation for the preparation of [99mTc-EDDA-HYNIC-D-Phe1, Tyr3]-octreotide, a somatostatin analog for tumor diagnosis

Journal of Pharmaceutical Sciences
Elisabeth Von GuggenbergC Decristoforo

Abstract

[(99m)Tc-EDDA-HYNIC-D-Phe(1),Tyr(3)]-Octreotide ((99m)Tc-EDDA/HYNIC-TOC) is a promising new radiopharmaceutical with the potential to replace [(111)In-DTPA-D-Phe(1)]-Octreotide ((111)In-DTPA-OCT) as the radiopharmaceutical for somatostatin receptor scintigraphy due to the advantage of improved image quality, lower radiation dose for the patient, and daily availability. Here we describe the development of a freeze-dried kit formulation based on the Tricine/EDDA exchange labeling approach for the preparation of this radiopharmaceutical in a clinical setting. Three parameters were of major importance to achieve a suitable formulation with a radiochemical purity (RCP) >90%: addition of bulking agent, the pH of the freeze-drying solution, and the content of stannous chloride. The final formulation consisted of 20 mg Tricine, 10 mg EDDA, 50 mg Mannitol, 20 microg SnCl(2). 2H(2)O, and 20 microg [HYNIC-D-Phe(1), Tyr(3)]-Octreotide (HYNIC-TOC). Radiolabeling was performed by addition of 0.2 M Na(2)HPO(4) to adjust the pH to 6-7, followed by 0.5-2 GBq (99m)Tc sodium pertechnetate, in a total volume of 2 mL and incubation for 10 min in a boiling water bath. Mean RCP values of 10 batches showed values >90% over a storage period of up to 1 ...Continue Reading

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Citations

Mar 15, 2006·Nuclear Medicine Communications·Guillermina Ferro-FloresMaría Teresa Ramírez-Iglesias
Dec 18, 2013·Nuclear Medicine Communications·Zareth Ortiz-ArzateVanessa Izquierdo-Sánchez
Nov 20, 2013·Indian Journal of Nuclear Medicine : IJNM : the Official Journal of the Society of Nuclear Medicine, India·Koramadai Karuppusamy KamaleshwaranAjit Sugunan Shinto
Jun 29, 2010·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·G Ferro-FloresD Ordaz-Rosado
May 1, 2007·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·M GandomkarS E S Ebrahimi
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Mar 18, 2006·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Armando González-VázquezZohar Gutiérrez-García
Mar 21, 2006·Nuclear Medicine and Biology·Kjerstin Bruus-JensenHans-Jürgen Wester
Sep 6, 2005·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Elisabeth von GuggenbergClemens Decristoforo
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Apr 17, 2015·BioMed Research International·Caiyun Xu, Hong Zhang
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