Convenient and Efficient Method for Quality Control Analysis of 18F-Fluorocholine: For a Small Scale GMP-based Radiopharmaceuticals Laboratory Set-up

Title:Convenient and Efficient Method for Quality Control Analysis of 18F-Fluorocholine: For a Small Scale GMP-based Radiopharmaceuticals Laboratory Set-up

Volume: 9 Issue: 2

Author(s): Hishar Hassan, Suharzelim Abu Bakar, Khairul Najah Che A Halim, Jaleezah Idris and Abdul Jalil Nordin

Affiliation:

Keywords: ¹⁸F-Fluorocholine, ¹⁸F-Fluorodeoxyglucose, GE TracerLabMx, PET, Prostate cancer, quality control.

Abstract: Background and Objective: Prostate cancer continues to be the most prevalent cancer in men in Malaysia. As time progresses, the prospect of PET imaging modality in diagnosis of prostate cancer is promising, with on-going improvement on novel tracers. Among all tracers, ¹⁸F-Fluorocholine is reported to be a reputable tracer and reliable diagnostic technique for prostate imaging. Nonetheless, only ¹⁸F-Fluorodeoxyglucose (¹⁸F-FDG) is available and used in most oncology cases in Malaysia. With a small scale GMP-based radiopharmaceuticals laboratory set-up, initial efforts have been taken to put Malaysia on¹⁸F-Fluorocholine map. This article presents a convenient, efficient and reliable method for quality control analysis of ¹⁸F-Fluorocholine. Besides, the aim of this research work is to assist local GMP radiopharmaceuticals laboratories and local authority in Malaysia for quality control analysis of ¹⁸F-Fluorocholine guideline.

Methods: In this study, prior to synthesis, quality control analysis method for 18F-Fluorocholine was developed and validated, by adapting the equipment set-up used in ¹⁸F-Fluorodeoxyglucose (¹⁸FFDG) routine production. Quality control on the ¹⁸F-Fluorocholine was performed by means of pH, radionuclidic identity, radio-high performance liquid chromatography equipped with ultraviolet, radio- thin layer chromatography, gas chromatography and filter integrity test.

Results: Post-synthesis; the pH of ¹⁸F-Fluorocholine was 6.42 ± 0.04, with half-life of 109.5 minutes (n = 12). The radiochemical purity was consistently higher than 99%, both in radio-high performance liquid chromatography equipped with ultraviolet (r-HPLC; SCX column, 0.25 M NaH2PO4: acetonitrile) and radio-thin layer chromatography method (r-TLC). The calculated relative retention time (RRT) in r-HPLC was 1.02, whereas the retention factor (Rf) in r-TLC was 0.64. Potential impurities from ¹⁸F-Fluorocholine synthesis such as ethanol, acetonitrile, dimethylethanolamine and dibromomethane were determined in gas chromatography. Using our parameters, (capillary column: DB-200, 30 m x 0.53 mm x 1 um) and oven temperature of 35°C (isothermal), all compounds were well resolved and eluted within 3 minutes. Level of ethanol and acetonitrile in ¹⁸F-Fluorocholine were detected below threshold limit; less than 5 mg/ml and 0.41 mg/ml respectively. Meanwhile, dimethylethanolamine and dibromomethane were undetectable.

Conclusion: A convenient, efficient and reliable quality control analysis work-up procedure for ¹⁸FFluorocholine has been established and validated to comply all the release criteria. The convenient method of quality control analysis may provide a guideline to local GMP radiopharmaceutical laboratories to start producing ¹⁸F-Fluorocholine as a tracer for prostate cancer imaging.

Cite this article as:

Hassan Hishar, Bakar Abu Suharzelim, Halim Najah Che A Khairul, Idris Jaleezah and Nordin Jalil Abdul, Convenient and Efficient Method for Quality Control Analysis of 18F-Fluorocholine: For a Small Scale GMP-based Radiopharmaceuticals Laboratory Set-up, Current Radiopharmaceuticals 2016; 9 (2) . https://dx.doi.org/10.2174/1874471008666150527091956