摘要
介绍一种新放射性药物即钐［（１５３）￣Ｓｍ］－柠檬酸－羟基磷灰石（（１５３）￣Ｓｍ－Ｃｉｔｒａｔｅ－Ｈｙｄｒｏｘｙａｐａｔｉｔｅ），采用转换络合法进行标记。先将钐［（１５３）￣Ｓｍ］与柠檬酸络合，然后转换络合为羟基磷灰石（ＨＡ）的标记物。ＨＡ的络合容量约５ｍｇ（以Ｓｍ＿２Ｏ＿３计），标记物粒度主要为２—１０μｍ，标记率高达９８％。体外稳定性研究表明：标记物在生理盐水和人血浆蛋白溶液中放置三个半衰期，（１５３）￣Ｓｍ的总游离量小于２％。正常兔左后膝关节注射１４．８ＭＢｑ（４００μＣｉ）（１５３）￣Ｓｍ－Ｃｉｔｒａｔｅ－ＨＡ，于４８ｈ、７２ｈ、１２０ｈ处死，经各脏器取样测量没发现有明显的放射性计数，９９％的注射量滞留在关节内。本标记药物可望用作风湿性关节滑膜切除。
A new kind of labelled radiopharmaceutical hydroxyapatite(HA ) by means of transfer complexing for the treatment of rheumatoid arthritis is described. HA with particals of 2 10μmis labelledwith(153)￣Sm by a citrate transfer ligand.(153)￣Sm-citrate-HA is obtained in high yield and is extremly sta-ble in vitro.The complexing capability of HA is about 5 mg Sm_2O_3/ g HA , the decomposition ratesof(153)￣Sm-citrate-HA both in saline of 0.9%and in human plasma(37±0.5℃)are less than 2.0%for a period of 3 half lives. Biodistribution studies in rabbits demonstrated long term retention of near-ly 99%of injected(153)￣Sm-Citrate-HA in arthritis joint. Extra-articular leakage of radioactivity in bothblood and urine accounted for 0.5%of injected dose,and few retained in other major tissues afterabout 14. 8 MBq of(153)￣Sm-Citrate-HA has injected into the left knee joint of normal rabbits.(153)￣Sm-cit-rate-HA could be potentially useful in radio-synovectomy treatment of rheumatism arthritis.
出处
《同位素》
CAS
北大核心
1994年第2期92-97,共6页
Journal of Isotopes
关键词
滑膜切除
放射性药物
钫153
m- citrate- HA transfer complexing extraarthritis leakage radioactivesynovectom y
