Tanaka K, Nagata M, Itoh S, Kumagae M, Shimizu N
Third Department of Medicine, Teikyo University School of Medicine, Ichihara, Japan.
Endocr J. 1993 Oct;40(5):591-6. doi: 10.1507/endocrj.40.591.
The pharmacokinetics, responses of plasma ACTH and cortisol, urinary excretion of steroid hormones, and safety of MCI-028, a synthetic human corticotropin-releasing hormone (hCRH), were examined in eight healthy adult male volunteers after intravenous administration of 33, 100 and 200 micrograms of the drug. The disappearance of MCI-028 from plasma could be fitted to a biexponential decay curve, the plasma half-lives (T1/2) were 0.12 to 0.15 h for alpha phase, and 0.57 to 0.67 h for beta phase. Plasma ACTH and cortisol concentrations and the urinary excretion of steroid hormones (particularly free cortisol) increased significantly in relation to the MCI-028 dose administrated. Although hot flushing and an increase in the heart rate were observed at higher doses, they were mild and transient. It is also considered that the urinary excretion of free cortisol after the administration of MCI-028 can be an index reflecting the functioning of this system.
在8名健康成年男性志愿者静脉注射33微克、100微克和200微克合成人促肾上腺皮质激素释放激素（hCRH）MCI-028后，对其药代动力学、血浆促肾上腺皮质激素（ACTH）和皮质醇反应、甾体激素的尿排泄情况以及安全性进行了研究。MCI-028在血浆中的消失情况符合双指数衰减曲线，α相的血浆半衰期（T1/2）为0.12至0.15小时，β相为0.57至0.67小时。血浆ACTH和皮质醇浓度以及甾体激素（特别是游离皮质醇）的尿排泄量随MCI-028给药剂量的增加而显著增加。尽管在较高剂量下观察到潮热和心率加快，但症状较轻且为一过性。还认为，MCI-028给药后游离皮质醇的尿排泄量可作为反映该系统功能的一个指标。
