Rafferty B, Schulster D
Mol Cell Endocrinol. 1985 Jun;41(1):19-25. doi: 10.1016/0303-7207(85)90139-x.
A homologous radioimmunoassay (RIA) system was developed for human GRF 1-40 and used to measure immunoreactive (IR) concentrations of the peptide in rats to determine some of its pharmacokinetic characteristics after intravenous (i.v.) and subcutaneous (s.c.) administration. A plot of the disappearance of IR-hGRF from plasma after a single intravenous injection was fitted by a biexponential curve, analysis of which gave a half-life of 3.2 +/- 0.2 min for the initial distribution phase and 57.3 +/- 1.5 min for the elimination phase. Comparison of areas under the plasma IR-hGRF/time curves after injection of identical doses of hGRF 1-40 showed that the amount detected in the circulation after it was injected s.c. was only 14-16% of the amount detected after i.v. administration. Such results may indicate degradation of a substantial proportion of the dose of the peptide at the site of injection or during its transfer to plasma; this should be borne in mind when undertaking s.c. administration for clinical purposes or in assessing the effect of GRF analogues.
开发了一种针对人GRF 1-40的同源放射免疫分析(RIA)系统,并用于测定大鼠体内该肽的免疫反应性(IR)浓度,以确定静脉内(i.v.)和皮下(s.c.)给药后其一些药代动力学特征。单次静脉注射后血浆中IR-hGRF消失情况的曲线拟合为双指数曲线,分析得出初始分布相的半衰期为3.2±0.2分钟,消除相的半衰期为57.3±1.5分钟。注射相同剂量的hGRF 1-40后,血浆IR-hGRF/时间曲线下面积的比较表明,皮下注射后循环中检测到的量仅为静脉内给药后检测到量的14-16%。这些结果可能表明该肽剂量的很大一部分在注射部位或转移至血浆的过程中发生了降解;在进行皮下给药用于临床目的或评估GRF类似物的效果时,应牢记这一点。