重组人胸腺肽α1在大鼠体内的药物动力学研究

Pharmacokinetics of rh-Tα_1 in Rats

研究了重组人胸腺肽α1(rh-Tα1)在大鼠体内的药物动力学,采用125I标记的rh-Tα1同位素法,观察单次皮下注射后的体内过程。125I-rh-Tα1单次皮下注射后在大鼠体内的动力学过程符合一室模型,消除半衰期(t1/2ke)为5.42～7.07h,绝对生物利用度为91.28%。125I-rh-Tα1在大鼠体内组织器官中分布广泛并能较快地消除,其在肾、胃、肺和卵巢等组织器官中有较高的积聚,而脑中则较小。125I-rh-Tα1主要经肾由尿排泄,给药后120h内,药物的82.4%由尿排出,7.6%由粪排出。

Pharmacokinetics of rh-Tα1 in rats was studied after a single dosage sc, with isotopic method labeling of ^125I. The result showed that the pharmacokinetics fit one compartment model. The pharmacokinetic parameters were as follows： t1/2ke 5.42 - 7.07h, the absolute bioavailability 91.28 %. rh-Tα1 exhibited rapid and considerable absorption and rapidly diminished in most tissues. The accumulation of rh-Tα1 in tissues appeared to be high. The kidney might play the major role in metabolism and elimination of ^125I-rh-Tα1, and the main excretion route was urinary system. Within 120h, approximately 82.4% and 7.6% of the administered dose was excreted to urine and feces, respectively.