Abstract
Introduction: The use of germanium-68 (68Ge)/gallium-68 (68Ga) generators is still limited when compared with the 99Mo/99mTc counterpart, mainly because of the absence of commercial kits and a kit-based method for preparing 68Ga-labelled radiopharmaceuticals in a reliable way. The present study aimed to develop and optimize a reliable direct labelling of DOTATOC with 68Ga through a kit-based approach. Materials and methods: A fraction of the eluate of two different 68Ge/68Ga generators was directly injected into a vial prefilled with precursor, buffer and scavenger (the prototype of a potential lyophilized kit). The vial was directly warmed to 100°C and then buffered with a 1.5 mol/l sodium ascorbate solution. The parameters influencing the reaction were studied and optimized. The efficacy of the method in terms of incorporation yield and quality of the final radiotracer was compared with preparations performed with two commercial automatic synthesizers by applying the tests prescribed in the European Pharmacopeia monograph for 68Ga-DOTATOC. Results: Under optimal conditions, the overall radiochemical yields of the kit-based process were 73 ± 4 and 69 ± 3% not decay-corrected for the IGG100 and itG generator, respectively. The radiochemical purity was 95 ±3% and the preparations were compliant with all specifications given in the pharmacopoeia monograph. Conclusion: The feasibility of a kit-based approach for the preparation of 68Ga-DOTATOC was proved and a first homemade version of a putative lyophilized kit was proposed.
| Original language | English |
|---|---|
| Pages (from-to) | 502-510 |
| Number of pages | 9 |
| Journal | Nuclear Medicine Communications |
| Volume | 36 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - Apr 14 2015 |
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Keywords
- DOTATOC
- Gallium-68
- Kit-based synthesis
- PET
- Somatostatin analogues
ASJC Scopus subject areas
- Radiology Nuclear Medicine and imaging
- Medicine(all)
Cite this
Development of a simple kit-based method for preparation of pharmaceutical-grade 68Ga-DOTATOC. / Asti, Mattia; Iori, Michele; Capponi, Pier Cesare; Rubagotti, Sara; Fraternali, Alessandro; Versari, Annibale.
In: Nuclear Medicine Communications, Vol. 36, No. 5, 14.04.2015, p. 502-510.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Development of a simple kit-based method for preparation of pharmaceutical-grade 68Ga-DOTATOC
AU - Asti, Mattia
AU - Iori, Michele
AU - Capponi, Pier Cesare
AU - Rubagotti, Sara
AU - Fraternali, Alessandro
AU - Versari, Annibale
PY - 2015/4/14
Y1 - 2015/4/14
N2 - Introduction: The use of germanium-68 (68Ge)/gallium-68 (68Ga) generators is still limited when compared with the 99Mo/99mTc counterpart, mainly because of the absence of commercial kits and a kit-based method for preparing 68Ga-labelled radiopharmaceuticals in a reliable way. The present study aimed to develop and optimize a reliable direct labelling of DOTATOC with 68Ga through a kit-based approach. Materials and methods: A fraction of the eluate of two different 68Ge/68Ga generators was directly injected into a vial prefilled with precursor, buffer and scavenger (the prototype of a potential lyophilized kit). The vial was directly warmed to 100°C and then buffered with a 1.5 mol/l sodium ascorbate solution. The parameters influencing the reaction were studied and optimized. The efficacy of the method in terms of incorporation yield and quality of the final radiotracer was compared with preparations performed with two commercial automatic synthesizers by applying the tests prescribed in the European Pharmacopeia monograph for 68Ga-DOTATOC. Results: Under optimal conditions, the overall radiochemical yields of the kit-based process were 73 ± 4 and 69 ± 3% not decay-corrected for the IGG100 and itG generator, respectively. The radiochemical purity was 95 ±3% and the preparations were compliant with all specifications given in the pharmacopoeia monograph. Conclusion: The feasibility of a kit-based approach for the preparation of 68Ga-DOTATOC was proved and a first homemade version of a putative lyophilized kit was proposed.
AB - Introduction: The use of germanium-68 (68Ge)/gallium-68 (68Ga) generators is still limited when compared with the 99Mo/99mTc counterpart, mainly because of the absence of commercial kits and a kit-based method for preparing 68Ga-labelled radiopharmaceuticals in a reliable way. The present study aimed to develop and optimize a reliable direct labelling of DOTATOC with 68Ga through a kit-based approach. Materials and methods: A fraction of the eluate of two different 68Ge/68Ga generators was directly injected into a vial prefilled with precursor, buffer and scavenger (the prototype of a potential lyophilized kit). The vial was directly warmed to 100°C and then buffered with a 1.5 mol/l sodium ascorbate solution. The parameters influencing the reaction were studied and optimized. The efficacy of the method in terms of incorporation yield and quality of the final radiotracer was compared with preparations performed with two commercial automatic synthesizers by applying the tests prescribed in the European Pharmacopeia monograph for 68Ga-DOTATOC. Results: Under optimal conditions, the overall radiochemical yields of the kit-based process were 73 ± 4 and 69 ± 3% not decay-corrected for the IGG100 and itG generator, respectively. The radiochemical purity was 95 ±3% and the preparations were compliant with all specifications given in the pharmacopoeia monograph. Conclusion: The feasibility of a kit-based approach for the preparation of 68Ga-DOTATOC was proved and a first homemade version of a putative lyophilized kit was proposed.
KW - DOTATOC
KW - Gallium-68
KW - Kit-based synthesis
KW - PET
KW - Somatostatin analogues
UR - http://www.scopus.com/inward/record.url?scp=84927519613&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84927519613&partnerID=8YFLogxK
U2 - 10.1097/MNM.0000000000000275
DO - 10.1097/MNM.0000000000000275
M3 - Article
C2 - 25695611
AN - SCOPUS:84927519613
VL - 36
SP - 502
EP - 510
JO - Nuclear Medicine Communications
JF - Nuclear Medicine Communications
SN - 0143-3636
IS - 5
ER -