环孢菌素G（NVa2环孢菌素）在血液和血浆中的分布。

Distribution of cyclosporin G (NVa2 cyclosporin) in blood and plasma.

作者信息

Yatscoff R W, Honcharik N, Lukowski M, Thliveris J, Chackowsky P, Faraci C

机构信息

Department of Laboratory Medicine and Pathology, University of Alberta, Edmonton, Canada.

出版信息

Clin Chem. 1993 Feb;39(2):213-7.

PMID:8432008

Abstract

We report here on the distribution of cyclosporin G (CsG), an analog of cyclosporin A, in whole blood. CsG has a temperature-dependent distribution between erythrocytes (RBCs) and plasma. After 30 min at 37 degrees C, the plasma/whole blood and plasma/RBC ratios were relatively constant (0.7-0.8) up to CsG at 1000 micrograms/L. At 5000 micrograms/L, this ratio increased to 1.0-1.1 for plasma/whole blood and 1.7 for plasma/RBC. The primary CsG metabolites GM1 and GM9 were sequestered within RBCs to a greater extent than was the parent drug. In whole blood, approximately 2% of CsG was bound to granulocytes, 6% to lymphocytes, and 50-55% to RBC, and 35-40% was found in the plasma fraction. The free fraction of the drug as determined by ultracentrifugation was 5-6% and 13-17% of total drug at 37 and 4 degrees C, respectively. In plasma the drug was primarily associated with high-density lipoprotein (50-60%) and to a lesser degree with low-density (20-30%) and very-low-density (10%) lipoproteins.

摘要

我们在此报告环孢素A类似物环孢素G（CsG）在全血中的分布情况。CsG在红细胞（RBC）和血浆之间的分布与温度有关。在37℃下放置30分钟后，在CsG浓度达1000微克/升之前，血浆/全血和血浆/红细胞的比例相对恒定（0.7 - 0.8）。在5000微克/升时，血浆/全血的这一比例增至1.0 - 1.1，血浆/红细胞的比例增至1.7。主要的CsG代谢产物GM1和GM9比母体药物更易被隔离在红细胞内。在全血中，约2%的CsG与粒细胞结合，6%与淋巴细胞结合，50 - 55%与红细胞结合，35 - 40%存在于血浆部分。通过超速离心测定，在37℃和4℃时，药物的游离部分分别占总药物的5 - 6%和13 - 17%。在血浆中，药物主要与高密度脂蛋白相关（50 - 60%），与低密度脂蛋白（20 - 30%）和极低密度脂蛋白（10%）的相关性较低。