基因重组人白介素-3在小鼠中的药动学、分布和排泄的特点

Characteristics of pharmacokinetics, distribution and excretion of recombinant human interleukin 3 in mice

每只小鼠皮下注射１．８μｇ／（约相当于９０μｇ／ｋｇ）的１２５Ｉ标记基因重组人白介素－３（１２５Ｉ－ｒｈＩＬ－３）后，用反相高效液相色谱法（ＲＨＰＬＣ）测定血浆浓度，估算动力学参数和测定组织放射性分布。消除半衰期为１．７３ｈ，药物在血浆内迅速降解。组织放射性分布特点为：肾泌尿排泄系统浓度最高，胆汁、肠道系统略高于血浆，淋巴、骨髓和脾脏等浓度略低或与血浆接近，脑内含量最低。４８ｈ内经尿和粪排泄的放射性占注入量（８４．０±９．２）％，其中尿（７１．９±６．７）％，粪（１２．２±５．３）％。肾脏是降解１２５Ｉ－ｒｈＩＬ－３的重要器官之一。

Concentration time profiles of 125 I labeled recombinant human interleukin 3 ( 125 I rhIL 3 ) were determined by reverse phase high performance liquid chromatography (RHPLC) after subcutaneous administration of the drug 90 μg/kg in mice. The elimination T1/2 in plasma was 1.73 h. Rapid biodegradation was found in plasma. The distribution profiles of total radioactivity were as follows: The highest level was found in urinary system. Levels in bile enteric system, lymph nodes, bone marrow and spleen approximated that in plasma, and level in brain was the lowest. A total of (84.0±9.2)% of the injected dose was excreted through urine and feces within 48 h, of which (71.9±6.7)% through urine and (12.2±5.3)% through feces. The RHPLC analysis revealed that kidney was one of the major organ for biodegradation.