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Objective:To produce the solid target nuclide 89Zr , and prepare the probe 89Zr-desferrioxamine (DFO)-Trastuzumab. Methods:The 89Y(p, n) 89Zr nuclear reaction was used for 89Zr production. 89Y target was irradiated by 20 μA proton in a medical cyclotron ( E=12.5 MeV) for about 1-2 h. 89Zr was purified from hydroxamate resin using 1 mol/L oxalic acid solution. The characteristic peak, radionuclide purity and radiochemical purity of 89Zr were determined by γ-ray spectroscopy. 89Zr-DFO-Trastuzumab probe was synthesized by the reaction of 89Zr-oxalate and DFO-Trastuzumab at room temperature, and the radiochemical purity was measured. Results:89Zr was prepared successfully for 11 times, and the production of 89Zr was 555-1 506 MBq, with production rate of (34.8±5.2) MBq·μA -1·h -1. After the purification (purification rate: 42%-87%), 227.2-991.6 MBq 89Zr was obtained, with the concentration of 1.0×10 6 MBq/L. The γ spectrum showed that the characteristic peak of 89Zr were 511 and 909 keV, and no impurities were found. The radionuclide purity and radiochemical purity were both close to 100%. 89Zr-DFO-Trastuzumab was successfully labeled with radiochemical purity more than 95%, and it was above 90% within 72 h in human serum albumin (HSA) solution. Conclusion:Through the self-designed target assembling, the solid target PET nuclide 89Zr with high quality and labeling are successfully achieved, which provides guarantee for the clinical application of the 89Zr drug.
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Immunosuppressant targeting programmed death protein-1 and its ligand (PD-1/PD-L1) is a hot topic in solid tumor immunotherapy.Detection of PD-1/PD-L1 expression in solid tumor patients by molecular imaging can predict whether tumor patients can benefit from immunotherapy.Small molecular polypeptide inhibitors have the advantages of low molecular weight,fast diffusion in tumor microenvironment,uniform distribution and easy access to the deep part of solid tumor.Non-invasive,real-time and quantitative detection of PD-1/PD-L1 expression in tumor patients can be performed by radionuclide labeled small molecular polypeptide inhibitor molecular probe PET imaging.It is expected to provide new detection methods for patient screening,efficacy monitoring,treatment plan optimization and prognosis evaluation.
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Objective@#To optimize the radiolabeling of prostate specific membrane antigen (PSMA)-targeted probe Al18F-PSMA-BCH (Beijing Cancer Hospital) and to evaluate its potential for clinical trial and translation.@*Methods@#The mixture of PSMA-BCH, AlCl3, potassium biphthalate and no-carrier loaded 18F- was reacted at 110 ℃ for 15 min, then purified by Sep-Pak Light C18 column and filtered through 0.22 μm sterile filter to obtain Al18F-PSMA-BCH. The radiolabeled yield and radiochemical purity were determined. Al18F-PSMA-BCH PET/CT imaging was performed on 5 healthy volunteers (age: (68±7) years) for biodistribution and radiation dosimetry estimate and on 1 patient (65 years) with recurrent prostate cancer.@*Results@#The non-decay-corrected radiochemical yield of Al18F-PSMA-BCH was (38.0±3.5)% with the radiochemical purity >99% and the specific activity of (16.4±4.4) MBq/nmol. Al18F-PSMA-BCH was stable in saline at room temperature. In healthy volunteers, radioactivity was mainly accumulated in the bladder, kidneys, lacrimal glands, parotid glands and submandibular glands, of which kidneys were the most critical organs with the dosimetry of (152.89±33.43) μGy/MBq, while bones showed lower uptake ((11.10±1.23) μGy/MBq) than most organs. The effective dose of whole body was (0.013 5 ±0.002 5) mSv/MBq. Multiple bone metastases were observed by Al18F-PSMA-BCH PET/CT imaging in a patient with recurrent prostate cancer.@*Conclusions@#Al18F-PSMA-BCH prepared with the pH controller of potassium biphthalate holds the potential for the diagnosis, staging and monitoring recurrence of prostate cancer.
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Objective To optimize the radiolabeling of prostate specific membrane antigen (PSMA)-targeted probe Al18 F-PSMA-BCH (Beijing Cancer Hospital) and to evaluate its potential for clinical trial and translation. Methods The mixture of PSMA-BCH, AlCl3 , potassium biphthalate and no-carrier loaded 18F- was reacted at 110 ℃ for 15 min, then purified by Sep-Pak Light C18 column and filtered through 0.22 μm sterile filter to obtain Al18 F-PSMA-BCH. The radiolabeled yield and radiochemical purity were determined. Al18 F-PSMA-BCH PET/ CT imaging was performed on 5 healthy volunteers (age: (68±7) years) for bio-distribution and radiation dosimetry estimate and on 1 patient (65 years) with recurrent prostate cancer. Re-sults The non-decay-corrected radiochemical yield of Al18F-PSMA-BCH was (38. 0±3.5)％ with the radiochem-ical purity >99％ and the specific activity of (16.4±4.4) MBq/ nmol. Al18 F-PSMA-BCH was stable in saline at room temperature. In healthy volunteers, radioactivity was mainly accumulated in the bladder, kidneys, lacrimal glands, parotid glands and submandibular glands, of which kidneys were the most critical organs with the dosim-etry of (152.89±33.43) μGy/ MBq, while bones showed lower uptake ((11.10±1.23) μGy/ MBq) than most or-gans. The effective dose of whole body was (0.0135 ±0.0025) mSv/ MBq. Multiple bone metastases were ob-served by Al18F-PSMA-BCH PET/ CT imaging in a patient with recurrent prostate cancer. Conclusions Al18 F-PSMA-BCH prepared with the pH controller of potassium biphthalate holds the potential for the diagnosis, staging and monitoring recurrence of prostate cancer.
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Objective To investigate the association between morniing blood pressure surge (MBPS) and carotid atherosclerosis in elder patients with essential hypertension. Methods According to the results of24h ambulatory blood pressure monitoring, 106 patients were classified as the morning BP surge group (MBPS group,n = 58) ,and nonsurge group (NMBPS group, n = 48). Patients underwent carotid ultrasound and the intima-medial thickness (CCA-IMT) and plaques were examined. Results The CCA-IMT of the MBPS group was significantly thicker than that the NMBPS group[(1.27 ± 0. 12)mm vs (0.92 ± 0.33 )mm], P ＜ 0. 05 ) ;②Compared with the NMBPS group,the severity of carotid arteries plaque of the MBPS group was significantly higher (72. 15% vs 54.21% ), ( P ＜0. 01 ) ;③Pearson relation analysis showed CCA-IMT level positively correlated with age (r = 0.288, P ＜ 0.001 ) ,the average of 24h SBP ( r = 0. 768 ,P ＜ 0. 001 ), and MBPS ( r = 0. 768, P ＜ 0.001 ). Conclusion The study showed that MBPS was closely related with carotid atherosclerosis in elder patients with essential hypertension and was an important risk factor in the process of atheresclerosis.