欢迎您！东篱公司
退出
-
申报数据库
-
立项数据库
-
成果数据库
-
项目获奖数据库
中文摘要：
目的制备高纯度放射性^125I标记的酪氨酸聚乙二醇化胸腺素α1（Tyr-PEG-TA1）用于动物药代动力学研究。方法改良Iodogen法进行^125I标记。Ziptip头监测标记反应进程以优化反应条件。采用Sephadex G50与Sephadex G10两步凝胶层析法对标记混合物进行纯化。利用酶免疫分析（EIA）方法鉴定PEG-TAl增加酪氨酸残基前后以及Tyr-PEG-TA1经^125I标记前后免疫学活性的变化。结果PEG-TA1增加酪氨酸残基前后以及Tyr-PEG-TA1经^125I标记前后免疫活性均无明显变化，纯化后的标记产物放化纯度为95．9％，放射性比活度为39．4Bq／ng。结论成功地制备了放化纯度和放射性比活度均满足药代动力学研究的^125I-Tyr-PEG-TA1。
英文摘要：
Objective To prepare a highly purified ^125I-pegylated thymosin al （ PEG-TA1 ） with satisfied bioaetivity for using in the distribution and excretion study in animals. Methods Tyr-PEG-TA1 was iedinated by means of Iodogen method. The ZipTip pipette tips were utilized to monitor the reaction process for the optimization of reaction conditions. A two-step gel filtration chromatography with Sephadex G50 followed by Sephadex G10 was applied to purify the labelled products. The hioactivity assay of PEG-TA1, Tyr-PEG-TA1 and ^125 I-Tyr-PEG-TA1 were performed by an enzyme immunoassay （EIA） method. Results The optimum condition of labelling reaction was： shaking for 20 min at 25℃ in 0.1 mol/L phosphate buffer （0.1mol/L NaCl） with the pH value of 7.0. Slight but no significant difference of bioactivity among the PEG-TA1, Tyr-PEG-TA1 and the ^125 I-Tyr-PEG-TA1 was observed. After the two-step purification process, a product of ^125 I-Tyr-PEG-TAI with radiochemical purity of 95 % and specific activity of 39.4 Bq/ng was obtained. Conclusion A successful preparation of ^125 I-Tyr-PEG- TA1 was achieved, and the radiochemical purity and the specific activity of the ^125I labeled molecules satisfied the requirements of non-clinical pharmacokinetic study.
同期刊论文项目
同项目期刊论文
Determination of simvastatin in human plasma by LC/MS/MS: application to the PK study in healthy Chi
Profiling of isovalertatin family aminooligosaccharides extracted from the culture of Streptomyces l
Structural revision of isovalertatin M03, M13, and M23 isolated from the culture of Streptomyces lut
Quantitation of the flavonoid wogonin and its major metabolite glucuronide in rat plasma by LC/MS/MS
Isolation and identification of the glucuronide of 4-(3H-1,2-dihydro-1- pyrrolizinone-2-methylamino)
Sensitive and specific LC/MS/MS assay for dihydroergotamine and its major metabolite in human plasma
Pharmacokinetics and partial thrombo- plastin time after intra-venous recom- binant hirudin variant-
BE study of amlodipine maleate tablet and amlodipine besylate tablet (Norvasc) in healthy Chinese su
PK of a sustained-release formulation of buflomedil after single and multiple doses in healthy Chine
Determination of ketotifen and its conjugated metabolite in human plasma by LC/MS/MS: application to
LC-MS-MS analysis of 2-pyridylacetic acid: application to a pharmacokinetic study in healthy volunte
Anti-tussive activity of benproperine enantiomers on citric acid-induced cough in conscious guinea p
Simultaneous determination of albendazol and its major active metabolite in human plasma using LC/MS
期刊信息
位置：