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α-山竹素与锝-99m的纯度鉴定及放射性标记

The purity identification and radiolabeling of α-mangostin with technetium-99m.

作者信息

Muchtaridi Muchtaridi, Setyawati Luthfi Utami, Islamiaty Risda Rahmi, Lie Kevin Reinard, Nurhidayah Wiwit

机构信息

Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Bandung, Indonesia.

出版信息

J Adv Pharm Technol Res. 2020 Jan-Mar;11(1):6-12. doi: 10.4103/japtr.JAPTR_94_19.

Abstract

Alpha-mangostin (AM) is a natural compound that has the greatest activity in breast cancer. Radiolabeling AM with technetium-99 m (Tc-99m) has a function as breast cancer radiotracer. This study is aimed to identify the purity of Tc-99m-labeled AM. The identification method was conducted by a validated radio-high-performance liquid chromatography (HPLC) to confirm the chemical purity of the compound when the thin layer of chromatography and paper chromatography were used to find out the radiochemical purity (RCP). The validated radio-HPLC method obtained was C18 column with methanol:water (90:10) as the mobile phase and ultraviolet (243 nm) tandem radioactive detector (Gabi Star). The result showed that the RCP was 70.6% ± 2.87%. The analytical method met the validation criteria according to ICH Q2 (R1); thus, it could be applied in the identification. Unfortunately, the Tc-AM identification using radio-HPLC showed that the expected complex was not yet formed perfectly because of chemical impurities.

摘要

α-山竹黄酮(AM)是一种在乳腺癌中具有最强活性的天然化合物。用99m锝(Tc-99m)对AM进行放射性标记可作为乳腺癌放射性示踪剂。本研究旨在鉴定Tc-99m标记的AM的纯度。鉴定方法采用经过验证的放射性高效液相色谱法(HPLC)来确认化合物的化学纯度,同时使用薄层色谱法和纸色谱法来测定放射化学纯度(RCP)。所获得的经过验证的放射性HPLC方法采用C18柱,以甲醇:水(90:10)作为流动相,并配备紫外(243 nm)串联放射性检测器(Gabi Star)。结果显示,放射化学纯度为70.6%±2.87%。该分析方法符合国际人用药品注册技术协调会(ICH)Q2(R1)的验证标准,因此可应用于鉴定。遗憾的是,使用放射性HPLC对Tc-AM进行鉴定时发现,由于化学杂质的存在,预期的复合物尚未完美形成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/33cd/7034178/648620fb2f64/JAPTR-11-6-g002.jpg

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