目的：研究獼猴單次sc重組人胸腺肽α1（rh-Tα1）的藥動學。方法：6只獼猴單次sc rh-Tα1 350 μg/kg，采用酶聯(lián)免疫分析檢測（ELISA）法測定動物的血藥濃度，實驗數(shù)據(jù)用3P97藥代軟件擬合并計算藥動學參數(shù)。結果：rh-Tα1在獼猴體內的消除符合一房室模型，6只動物的達峰時間（t_max）均為1.5 h，平均消除半衰期（t_1/2ke）為（2.9±0.8）h；峰濃度（C_max）均值為（297.0±43.3）ng/mL；平均清除率（CL）為（0.373±0.116）mL/（h·kg）；藥時曲線下面積（AUC_0～24h）均值為（1 165±333）ng·h/mL。結論：血清樣品經(jīng) 5倍稀釋后用ELISA方法能較準確測定獼猴血清中rh-Tα1的量。6只獼猴sc rh-Tα1后達峰時間一致且較短，主要藥動學參數(shù)顯示一定個體差異，但無明顯性別差異。

Objective: To explore pharmacokinetic properties of a recombinant human Thymosin α1 (rh-Tα1) followingsc administration in monkeys. Methods: The monkeys received single sc doses of rh-Tα1 at 350 μg/kg. Serum concentration of rh-Tα1 was measured at various time-points after dosing by an enzyme-linked immunosorbent assay (ELISA). Pharmacokinetic parameters were calculated with 3P97 software. Results: The concentration-time profile of rh-Tα1 in monkeys was described by an one-compartment model. The mean time to reach peak concentration (t_max) was 1.5 h. The mean elimination half-life (t_1/2ke) was (2.9 ± 0.8) h. The average clearance rate was (0.373 ± 0.116) mL/(h·kg). The mean peak concentration (C_max) was (297.0 ± 43.3)ng/mL. The mean area under the serum concentration-time curve (AUC_{0~24 h}) was (1 165 ± 333) ng·h/mL. Conclusion: Serum concentration of rh-Tα1 is detected accurately by ELISA method when serum samples are diluted five times. The t_max of the six monkeys are the same, but the main pharmacokinetic parameters demonstrate a certain degree of individual differences without obvious sex differences.

國家高技術研究發(fā)展計劃（No.2007BAI14IB04），國家重點基礎研究發(fā)展計劃（No.2004CB518902）