Yamamoto A, Kawaratani T, Aisaka A, Hashida M, Sezaki H
Department of Basic Pharmaceutics, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
J Pharm Pharmacol. 1991 Jan;43(1):36-9. doi: 10.1111/j.2042-7158.1991.tb05444.x.
Rats were immunized with bovine gamma-globulin-sulphanilic acid conjugate and the plasma concentration of sulphanilic acid examined after an intravenous injection of this drug. There was a significant increase in plasma half-life and AUC and a significant decrease in clearance of sulphanilic acid in the immunized rats compared with the control. In the immunized rats, binding of sulphanilic acid to macromolecules in serum, determined by ultrafiltration, decreased with increase of sulphanilic acid concentration. At low concentrations, there was a significant increase in % binding of the drug in the serum of immunized rats compared with controls. There was also a significant reduction in urinary excretion of total drug in the immunized rats compared with controls. These findings suggest that sulphanilic acid-specific antibodies in the serum of immunized animals bind [14C]sulphanilic acid, giving rise to higher serum levels thereby making it unavailable for normal excretory processes.
用牛γ球蛋白 - 磺胺酸共轭物对大鼠进行免疫，静脉注射该药物后检测血浆中磺胺酸的浓度。与对照组相比，免疫大鼠体内磺胺酸的血浆半衰期和曲线下面积显著增加，清除率显著降低。在免疫大鼠中，通过超滤测定，磺胺酸与血清中大分子的结合随磺胺酸浓度的增加而降低。在低浓度时，与对照组相比，免疫大鼠血清中药物的结合百分比显著增加。与对照组相比，免疫大鼠中药物总尿排泄量也显著减少。这些发现表明，免疫动物血清中的磺胺酸特异性抗体结合[14C]磺胺酸，从而导致更高的血清水平，使其无法进行正常的排泄过程。
