乳糖化人生长激素在小鼠体内的组织分布和药代动力学

Biodistribution and pharmacokinetics of lactosaminated human growth hormone in mice

目的 研究乳糖化人生长激素 (hGH L)在小鼠体内的组织分布和药代动力学特征。方法 用放射性核素体内示踪技术研究体内分布 ,用放射免疫分析 (RIA)技术研究药代动力学。并对比研究人生长激素 (hGH)。结果 12 5I hGH L具有明显的趋肝性 ,肝最大摄取率为 6 8 83% ,约为12 5I hGH的 2倍。hGH L的血药时曲线下面积 (AUC为32 6 86 9)和在血清的平均驻留时间 (MRT为 2 1 37min)均小于hGH (AUC为 36 913 0 8,MRT为 2 4 98min) (P <0 0 0 5 ) ;而靶器官肝脏的hGH L分布半衰期T12 α( 1 84min)、清除半衰期T12 β( 11 0 9min)小于hGH (T12 α2 11min ,T12 β75 6 5min) (P <0 0 0 5 ) ,其AUC( 176 2 1 9) >hGH( 12 148 2 ) (P <0 0 0 5 )。结论 hGH

AIM To study the biodistribution and pharmacokinetics of lactosaminated human growth hormone (hGHL, a new drug of treating dwarfism) in mice METHODS Biodistribution was studied with in vivo radioactive tracer technique Pharmacokinetics was studied with radiommuno assay technique RESULTS 125 IhGHL had remarkable livertaxis and its most high uptake in liver was 6883% that was about two fold high than hGH The area under curve (AUC) of blood drug concentrationtime curve of hGHL was 32 6869 , the mean remain time (MRT) of hGHL in blood was 2137 minutes; but AUC of blood drug concentrationtime curve of hGH was 36 91308 , MRT of hGH in blood was 2498 minutes; P<0005 In liver, to hGHL, halftime of distribution (T 12α ) was 184 minutes, halftime of remove (T 12β ) was 1109 minutes, AUC of liver drug concentrationtime curve was 17 6219 ; to hGH, T 12α was 211 minutes; T 12β was 7565 minutes, AUC of liver drug concentrationtime curve was 12 1482 ; P<0005ONCLUSIONS hGHL will become a new drug of dwarfism therapy with enhancing curative effects of human growth hormone.