Vine W, Flye M W, Jatlow P
Clin Chem. 1986 Oct;32(10):1828-31.
"Trough" (minimum inter-dose) cyclosporine concentrations were measured by liquid chromatography in samples of serum and whole blood or bile obtained from renal- and hepatic-transplant patients. Overall, concentrations in whole blood correlated poorly with concentrations in concurrently obtained serum. The poor correlation also held for individual patients over time. The degree of variability observed for individuals is especially disconcerting. Although cyclosporine measurements in whole blood may mitigate time- and temperature-dependent changes in the drug's distribution after collection, concentrations in serum separated after distribution are less dependent on the cellular mass in blood, and may better reflect the amount of drug available to receptor sites. This consideration may be particularly important in the postoperative period, when fluctuations in the cellular mass of blood are frequent. Concentrations of cyclosporine were also determined in concurrently collected bile and serum samples after liver transplantation. Concentrations of unchanged drug in bile were variably higher than those in serum. Bile/serum concentration ratios ranged from 65/1 to 4.6/1. It is postulated that bile/blood concentration ratios may reflect liver function.
通过液相色谱法对肾移植和肝移植患者的血清、全血或胆汁样本进行“谷值”（最低给药间期）环孢素浓度测定。总体而言，全血中的浓度与同时采集的血清中的浓度相关性较差。随着时间推移，这种较差的相关性在个体患者中也依然存在。个体所观察到的变异性程度尤其令人不安。尽管全血中环孢素的测定可能会减轻采集后药物分布中时间和温度依赖性的变化，但分布后分离的血清中的浓度较少依赖于血液中的细胞量，并且可能更好地反映可用于受体部位的药物量。在术后期间，当血液细胞量频繁波动时，这一考虑可能尤为重要。肝移植后，还对同时采集的胆汁和血清样本中的环孢素浓度进行了测定。胆汁中未变化药物的浓度变化不定地高于血清中的浓度。胆汁/血清浓度比范围为65/1至4.6/1。据推测，胆汁/血液浓度比可能反映肝功能。
