^(153)Sm-EDTMP体内外的竞争结合分析

IN VIVO AND IN VITRO BINDING ASSAY OF ^(153)Sm EDTMP

采用Ｗａｔｅｒｓ ＨＰＬＣｃｏｌｕｍ ｎ ｕｌｔｒａｈｙｄｒｏｇｅｌＴＭ１２０ μｍ （７．８ ｍ ｍ ×３００ ｍ ｍ ）ＨＰＬＣ凝胶色层柱，对１５３Ｓｍ Ｃｌ３、１５３Ｓｍ －ＥＤＴＭＰ分别与半胱胺酸、牛血清蛋白（ＢＳＡ）、小鼠血清进行了体外竞争结合分析；１５３Ｓｍ Ｃｌ３、１５３Ｓｍ －ＥＤＴＭＰ小鼠尾静脉注射后，对肝匀浆提取液和尿样进行了ＨＰＬＣ分析。ＨＰＬＣ分析条件：流动相０．８５ ｍ ｏｌ／ｍ ＬＰＢＳ，流速０．５ ｍ Ｌ／ｍ ｉｎ，进样量１５ μＬ。结果表明：游离的１５３Ｓｍ Ｃｌ３ 既可在体外与鼠血清相结合，又可在体内与肝蛋白结合；１５３Ｓｍ －ＥＤＴＭＰ在体内体外竞争结合分析中，它不与鼠血清、半胱胺酸、ＢＳＡ结合，当ｎ（ＥＤＴＭＰ）∶ｎ（Ｓｍ ）＝ １∶１ 时在体内的肝匀浆提取液中有滞留，比值≥５∶１ 未观测到任何滞留，说明１５３Ｓｍ －ＥＤＴＭＰ在体内是稳定的。１５３Ｓｍ －ＥＤＴＭＰ在有效使用期６ ｄ 内外观颜色变深，但ＨＰＬＣ分离分析未观测到辐射分解产物，大剂量包装放置２ 个月后ＨＰＬＣ紫外图中出现降解小峰，２ 种情况下的放射化学纯度都大于９８ ％ 。

With the waters ultrahydrogel TM 120 μm HPLC column(7.8 mm×300 mm),several experiments have been finished, including the in vitro binding assay of 153 Sm EDTMP, 153 SmCl 3 with the Cys, BSA, mouse plasma; HPLC analysis of the urine and the extracting solution of liver homogenate after having injected the 153 Sm EDTMP and 153 SmCl 3 2 h; HPLC analysis of the production ( 153 Sm EDTMP)radiation self decomposition with large dose. For the HPLC analysis, the condition is the mobile phase of 0.85 mol/mL PBS (pH=7.5), flow rate of 0.5 mL/min, sampling of 15 μL. The results are following: (1) The 153 SmCl 3 not only is able to bind with the mouse plasma in vitro, but also is able to be absorbed by liver in vivo; (2) 153 Sm EDTMP is not bind with the mouse plasma, the Cys and BSA in vitro & vivo; 153 Sm EDTMP is not found in the extracted solution of liver homogenate at n (EDTMP)∶ n (Sm)≥5∶1; 153 Sm EDTMP is not decomposed in the urine, 153 Sm EDTMP is stable in vivo; (3) 153 Sm EDTMP radiation self decomposition is not detected with large dose in the term of validity (6 d), but two small degradation peaks have been found in the production solution after 60 d, the radiochemistry purity of production is always great than 98 % during the period.