Legler U F, Benet L Z
Eur J Clin Pharmacol. 1986;30(1):51-5. doi: 10.1007/BF00614195.
The protein binding of prednisolone was studied in plasma obtained from healthy volunteers in the presence of added amounts of prednisone and hydrocortisone. The plasma protein binding was determined using in vitro equilibrium dialysis for 16 h at 37 degrees C against isotonic Krebs-Ringer buffer using radioactive prednisolone. Prednisone appeared to have no effect on prednisolone binding. This surprising result was observed even when prednisone concentrations were more than 35 fold greater than prednisolone concentrations. In contrast, a marked competition between hydrocortisone and prednisolone was observed. These binding data were fit using a nonlinear least squares regression computer program and the capacity and affinity constants for the binding of prednisolone to transcortin and albumin were estimated including the competition for binding sites between prednisolone and hydrocortisone. The results from these studies compare favorably with recent parameter calculations, and our previous work where differences in binding were noted between cushingoid and noncushingoid patients.
在添加了一定量泼尼松和氢化可的松的情况下，对健康志愿者的血浆中泼尼松龙的蛋白结合情况进行了研究。使用放射性泼尼松龙，在37℃下针对等渗的克雷布斯-林格缓冲液进行16小时的体外平衡透析，以测定血浆蛋白结合情况。泼尼松似乎对泼尼松龙的结合没有影响。即使泼尼松浓度比泼尼松龙浓度高出35倍以上，仍观察到这一令人惊讶的结果。相比之下，观察到氢化可的松与泼尼松龙之间存在明显的竞争。使用非线性最小二乘回归计算机程序对这些结合数据进行拟合，并估算了泼尼松龙与皮质转运蛋白和白蛋白结合的容量和亲和常数，包括泼尼松龙与氢化可的松之间对结合位点的竞争。这些研究结果与最近的参数计算结果以及我们之前的工作相比具有优势，在我们之前的工作中，注意到库欣综合征患者和非库欣综合征患者之间存在结合差异。
