来昔决南钐［153Sm］注射液质量控制标准

建立了来昔决南钐［¹⁵³Sm］注射液的质量控制指标及方法,主要包括pH检查、细菌内毒素检查、无菌检查、性状鉴别、含游离依地四膦酸量、来昔决南钐含量、放射性核纯度、放化纯度、放射性浓度。分析方法适用于来昔决南钐［¹⁵³Sm］注射液的常规检验,为该药的质量控制提供了可靠的分析手段。     

Biodistribution study of [^61Cu]pyruvaldehyde-bis （N-4-methylthiosemicarbazone） in normal rats as a PET tracer

[61Cu]-labeled pyruvaldehyde-bis (N-4-methylthiosemicarbazone) (61Cu-PTSM), a promising agent made for imaging blood perfusion, was produced via the natZn(p,x)61Cu nuclear reaction in a 30 MeV cyclotron, and separated by a two-step column chromatography method developed in our laboratory using a cation and an anion exchange resin. After 150μA irradiation for 76 min, about 6.006 Ci of 61Cu2 was obtained with a radiochemical separation yield of 95% and a radionuclidic purity of 99%. 61Cu-PTSM was prepared using an optimized method with in-house synthesized PTSM ligand for radiolabeling following quality control procedures using RTLC and HPLC. The tracer is mostly incorporated in heart, kidneys and brain compared to free copper cation as a control. These are in agreement with former reports. In conclusion, [61Cu]-PTSM was prepared at the radiopharmaceutical scales with high quality and is a potential PET tracer in the perfusion study of the heart, kidney, brain and tumors.     

亲和素-生物素系统的153Sm标记及其生物学分布动力学的研究

选用＾１５３Ｓｍ对生物素进行放射性标记,然后利用亲和素和链霉亲和素与生物素的高亲合力特性,再对亲和素和链霉亲和素进行＾１５３Ｓｍ的标记,观察到大鼠和小鼠体内的血清除率和生物学分布,并与＾１５３ＳｍＣｌ３和＾１５３Ｓｍ－ＤＴＰＡ的生物学分布进行比较。结果表明,＾１５３Ｓｍ标记的亲和素血素除迅速,肝肾放射性摄取高;＾１５３Ｓｍ标记的链霉亲和素血清除缓慢,肝、脾、肾等脏器和血液中滞留量高;而＾１５３Ｓｍ     

Preparation and bio-distribution of bone tumor therapeutic radiopharmaceutical ~(153)Sm-TTHMP

TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was labeled with 153Sm. The labeling condition, stability, mole ratio of 153Sm to TTHMP, rabbit bone imaging and bio-distribution of 153Sm-TTHMP in mice were investigated. The results showed that weak basie media and high concentration ligands were favorable to form 153Sm-TTHMP; labeling compounds were stable at pH 7 in 7 days. The results also indicated that the chemical mole ratio of 153Sm-TTHMP is n(153Sm) : n(TTHMP) = 1 : 1 and skeleton uptake of 153Sm-TTHMP is high((13.96±3.51)%/g at 1h post injection and (13.54±2.98)%/g at 48h post injection), while the non-target tissue uptake is relatively low, so 153Sm-TTHMP is a promising bone tumor therapeutic agent.     

Preparation and bio-distribution of 153Sm-HEDTMP as a radiopharmaceutical for bone metastases

1 Introduction Metastases to skeleton from prostate, breast, andlung cancer are frequent in clinical practice. The pal-liation of patients with extreme pain of bone metasta-ses was of primary importance in clinical managementof patients with advanced cancer. Based on concentra-tion at sites of increased bone turnover, ra-dio-therapeutics was an effective alternative to con-ventional therapies. 153Sm-EDTMP (ethylene diaminetetramethylene phosphonate) has been developed topalliate su…     

Preparation, quality control and biodistribution of [^61Cu]-doxorubicin for PET imaging

This work was conducted for radiolabeling of an anticancer antibiotic, i.e. doxorubicin with 61Cu for pro-duction of possible tracer used in PET oncology. 61Cu was prepared with natural zinc target and 22 MeV150 mA pro-tons via natZn(p, xn)61Cu reaction with a yield of 123.2 MBq·μA-1·h-1. Optimization reactions were performed for pH, temperature and concentration. Biodistribution of the tracer was studied in normal and fibrosarcoma bearing mice. At the optimized conditions, ITLC showed that radiochemical purity was over 97% with a specific activity of 2.22×103MBq ·mmol-1·L-1. This was kept unchanged even with presence of human serum as well as room temperature for 5 h. Biodistribution of the tracer in fibrosarcoma bearing mice demonstrated significant tumor uptake after 2 h. This tracer can be used in the detection of various tumors responding to doxorubicin chemotherapy using PET scan and/or determination of tumor therapy response to doxorubicin chemotherapy.     

高活度^153Gd源芯体的研制

~(153)Gd骨密度计源芯体的烧结工艺为:将加有4%石蜡的~(153)Gd_2O_3粉末于专用模具中压制成形,再于1400℃氢气气氛中烧结成直径3mm、厚度1mm及放射性活度大于3.7×10~(10)Bq的骨密度计源陶瓷芯体。     

153Sm-葡庚糖酸钠的制备

研究了制备条件对153Sm标记GH的影响及标记物的体外稳定性,建立了有效的153Sm标记葡萄糖酸钠(GH)方法。结果表明:用通氮敞开体系、沸水浴加热的标记方法,反应时间不低于30min,GH浓度不低于2.4×10-2mol/L时,可获得标记率大于98%的153Sm-GH;用高比活度153Sm(～4.5TBq/g(Sm))标记,其比活度可达14GBq/g(GH)。该标记物在室温下具有较好的稳定性,放置40h内,其放化纯度>96%。     

Preparation and preliminary evaluation of [55Co](Ⅱ)vancomycin

Co-55 (t1/2=17.53 h) was produced by 150 μA irradiation of a natural nickel target using 15 MeV protons. It was separated from the irradiated target material by two ion exchange chromatography steps with a radiochemical yield of>95% and was used for the preparation of [55Co]vancomycin ([55Co]VAN). Optimization studies were per-formed using Co-57 due to its longer half-life. Cobalt-57 (t1/2=271.79 d) was produced by irradiation of a natural nickel target with 150 μA current of 22 MeV protons. The 57Co was separated from the irradiated target material using a no-carrier-added method with a radiochemical yield of>97%. Both products were controlled for radionuelide and chemical purity. The solutions of [55Co]VAN were prepared (radiochemical yield>80%) starting with 55Co acetate and vancomycin at room temperature after 30 min. A precise solid phrase extraction (SPE) method was developed using Si Sep-Pak in order to purify/reconstitute the final formulation for animal studies. [55Co]VAN showed a radiochemical purity of more than 99%. The resultant specific activity was about 1.15 TBq/mmol. It is proved that the tracer is stable in the final product and in presence of human serum at 37℃ up to 24 h. Biodistribution study of [55Co]VAN in normal rats was undertaken for up to 72 h.     

^153Gd骨密度计源的研制

本文介绍了生产~(153)Gd骨密度计源的原理、工艺和结果。采用天然Eu_2O_3作靶材料,汞阴极电解法分离得的~(153)Gd,经压制、烧结法制成源芯体。源的活度>3.7×10~10Bq,放射性核纯度>99.99%。     

Preparation and preliminary evaluation of [^55Co]（II）vancomycin

Co-55 (t1/2=17.53 h) was produced by 150 μA irradiation of a natural nickel target using 15 MeV protons. It was separated from the irradiated target material by two ion exchange chromatography steps with a radiochemical yield of >95% and was used for the preparation of [55Co]vancomycin ([55Co]VAN). Optimization studies were per- formed using Co-57 due to its longer half-life. Cobalt-57 (t1/2=271.79 d) was produced by irradiation of a natural nickel target with 150 μA current of 22 MeV protons. The 57Co was ...     

153Sm-DTPA-PNIPAAm的制备及其在荷瘤鼠体内的分布

合成了带双功能偶联剂二乙三胺五醋酸(DTPA)的热敏高分子DTPA-PNIPAAm,它保持了聚(N-异丙基丙烯酰胺)(PNIPAAm)的热敏性.探讨了153Sm-DTPA-PNIPAAm的制备条件和体外稳定性,经皮下瘤内注入后标记物在荷瘤鼠体内的分布.结果表明,室温下153Sm-DTPA-PNIPAAm的最佳标记条件为,pH=7～9,配体质量为20～25 mg,反应时间大于20 min;最高标记率为93.4%;标记物的体外稳定性较高,76 h内标记物的放化纯度保持在96.5%以上;皮下瘤内注入后,标记物主要滞留在注入点肿瘤组织内,3 d时其滞留率为(83.2±9.7)%.     

羟基磷灰石对153Sm-HEDTMP的吸附性能研究

研究了各种因素对153Sm-HEDTMP(羟乙基乙二胺三甲撑膦酸)在羟基磷灰石(HA)上吸附的影响。结果表明,室温下153Sm-HEDTMP在HA上吸附20 min即可达到平衡,温度对吸附量影响不明显;过量配体会使配合物吸附量降低;吸附量在酸性条件下较高,153Sm3 在HA上的吸附能力最强,饱和吸附容量可达720μmol.g-1;153Sm-HEDTMP饱和吸附容量为61μmol.g-1;Ca2 对吸附有强烈的促进作用。EDTMP和HEDTMP对配合物的解吸率较高;生理盐水的解吸作用不明显。     

Radiosynthesis and biodistribution of [^18F]-tetracosactide using a semi-automated [^18F]SFB production module

In order to prepare a specific melanocortin type 2 receptor (MC2R) ligand, b1-24-corticotrophin was pre-pared in one-step reaction with [18F] SFB and b-1-24-corticotrophin pharmaceutical solution (1 mg/mL, pH=6.5). [18F]SFB was prepared in a semi-automated module in two steps with an overall radiochemical yield of 47% to EOB (not-decay corrected) in 90 min. The 18F-labeled intermediates and 18F-labeled peptide was checked by RTLC and HPLC. The results show that the radiochemical purity is >95% and the yield to EOB (not-decay corrected) is 29% for final 18F-labeled peptide at optimized conditions. Preliminary in vivo studies in normal mice were performed to deter-mine biodistribution of the 18F-labeled peptide for 150 min. The results show that the major tracer uptake is consistent with the natural distribution of MC2R receptors in mammals. Testes/blood and testes/muscle ratios for 18F-labeled peptide at 150 min were 184 and 1.56, respectively, and adipocyte/blood and adipocyte/muscle ratios at 120 min were 221 and 142, respectively. The data support the specific receptor binding of the radiolabeled peptide as reported for MC2R receptor accumulation in adipocytes and testes and demonstrates the retention of biological activity of the pep-tide. This tracer can be used in detection of MC2R distribution in malignancies and sex organ diseases.     

生长抑素及其类似物的标记技术的发展

生长抑素受体显像剂是临床上应用最为普遍的放射性多肽类受体显像剂。用多种放射性同位素^111In、^90Y、^6Ga、^68Ga、^64Cu或是用^99Tc^m、^188Re以及卤族同位素^123I、^18F等对奥曲肽及其类似物进行标记得到的放射性多肽药物，已广泛用于临床显像。介绍了生长抑素类似物及标记技术的发展，对目前临床上比较成熟的生长抑素类显像剂做了综述和比较。同时介绍了目前在SST类似物开发领域及生物行为研究领域中的最新发展动态。     

153Sm─EDTMP注射液活度测量标准化研究

治疗用放射性药品活度与其用药安全性和有效直接相关。为了确保153Sm─EDTMP注射液用药安全有效,本工作对使用活度计测量Na188ReO4 溶液活度的方法进行了标准化研究。利用4π液闪、4πβ-γ符合方法,通过四家单位6套装置测量,确定153Sm─EDTMP注射液标准源的活度量值;再利用已知活度的标准源,对使用活度计测量153Sm─EDTMP注射液活度的方法进行了标准化研究,确定测量条件。     

Measurement of 153Sm-EDTMP bone uptake by whole-body scintigraphy and its application to individualized treatment dosimetry of bone metastasis

1 INTRODUCTIONSamarium-153 ethylenedialninetetramethylene phosphonic acid ("'Sin-EDTMP) iselective in the palation of painful bony metastases[1]. Pain relief is seen in 60%~90%of patients treated with "'Sin-EDTMP, and the onset Of pain relief generally beginswithin 1 week of administration. The critical organ in 153Sin-EDTMP therapy is thered bone marrow and myelotoalcity can be a significant side effect of the administrationof therapeutic activities of 153Sin-EDTMP[2]. There is…     

153Sm-EDTMP与云克联合治疗转移性骨肿瘤疼痛的临床价值

为探讨^153Sm-EDTMP（^153钐－乙二胺四亚甲基膦酸）与云克（^99Tc-MDP，即^99锝－亚甲基二膦酸盐）联合治疗转移性骨肿瘤疼痛的临床价值。对210例癌骨转移患者分别为^153Sm-EDTMP单独治疗或与云克联合治疗，观察其疗效。结果显示，^153Sm-EDTMP单独治疗组，止痛有效率为83．7％，转移灶消失或缩小的总有效率为21．6％；^153Sm-EDTMP与云克静脉滴注联合治疗组，止痛有效率为94．7％，转移灶消失或缩小的总有效率为35．1％。后者明显高于单独治疗组。表明^153Sm-EDTMP联合云克静脉滴注对恶性肿瘤多发性骨转移所致疼痛有明显疗效，且安全无副作用。联合治疗组疗效优于单独治疗组。     

~(153)Sm-纳米羟基磷灰石的合成及生物行为初探

合成了纳米羟基磷灰石,制备的153Sm-EDTMP-nanoHA和153Sm-citrate-nanoHA体外稳定性良好。153Sm-EDTMP-nanoHA新西兰兔显像对比度较好,骨骼系统显示清晰,肝脾显影清晰,肾脏显影,血清除快;153Sm-citrate-nanoHA新西兰兔显像,肝脾显影清晰,血清除快,肾脏几乎不显影,说明主要通过肝胆排泄。153Sm-EDTMP-nanoHA对肝癌SMMC-7721和乳腺癌MCF-7细胞的半抑制率浓度分别是1.98g/L和0.075g/L,153Sm-citrate-nanoHA则分别是1.89g/L和0.094g/L。153Sm-EDTMP-nanoHA和153Sm-citrate-na-noHA较同等浓度下的单一nanoHA的半抑制率浓度低得多,具有很高的深入研究价值。     

Synthesis,radiolabeling and biological evaluation of butene amine oxime containing nitrotriazole as a tumor hypoxia marker

~(99m)Tc-BnAO, as a nonnitroaromatic hypoxia marker, is the subject of intensive research in recent years. In this study, a butene amine oxime–nitrotriazole(Bn AO–NT)was synthesized and radiolabeled with ~(99m)Tc in high yield.Cellular uptakes of~(99m)Tc-Bn AO–NT and ~(99m)Tc-Bn AO were tested using murine sarcoma S180 and hepatoma H22 cell lines. The highest hypoxic cellular uptake of~(99m)TcBn AO–NT was 27.11 ± 0.73 and 14.85 ± 0.83 % for the S180 and H22 cell lines, respectively, whereas the normoxic cellular uptake of the complex was about 4–8 % for both cell lines. For~(99m)Tc-Bn AO, the highest hypoxic cellular uptake was 30.79 ± 0.44 and 9.66 ± 1.20 % for the S180 and H22 cell lines, respectively, while the normoxic cellular uptake was about 5 % for both cell lines. Both~(99m)Tc-Bn AO–NT and~(99m)Tc-Bn AO complexes showed hypoxic/normoxic differentials in the two cell lines, but the results were more significant for the S180 cell line. The in vitro results suggested that S180 may be better than H22 cell line in hypoxic biological evaluation of Bn AO complexes. The biodistribution study was tested using a S180 tumor model. The complex~(99m)Tc-Bn AO–NT showed a selective enrichment in tumor tissues: At 4 h, the tumor-to-muscle ratio was 3.79 ± 0.98 and the tumor-to-blood ratio was 2.31 ± 0.34.Compared with the results of ~(99m)Tc-Bn AO, the latter was at the same level. In vitro and in vivo studies demonstrated that ~(99m)Tc-Bn AO–NT could be a hypoxia-sensitive radiotracer for monitoring hypoxic regions in a sarcoma S180 tumor.