George S, McBurney A, Ward J
Br J Clin Pharmacol. 1984 Nov;18(5):785-90. doi: 10.1111/j.1365-2125.1984.tb02543.x.
The protein binding of timegadine to albumin, serum, plasma and plasma enriched with the acute phase reactants alpha 1-acid glycoprotein, alpha 1-anti-trypsin and C-reactive protein was determined by equilibrium dialysis. The effects of other analgesic and anti-inflammatories (indomethacin, ketoprofen, paracetamol and sodium salicylate) and other basic drugs (disopyramide, lignocaine, propranolol and quinidine) on the binding of timegadine were also determined. Timegadine binding was concentration-dependent up to 0.5 micrograms/ml, but independent above this level up to 10.0 micrograms/ml, the mean and standard error being 93.8 +/- 0.5%. Albumin accounted for only 32.4% of timegadine bound to plasma. Plasma enrichment with the acute phase reactants led to significant increases in timegadine binding. Simultaneous dialysis with other drugs caused significant decreases in timegadine binding.
采用平衡透析法测定替马加汀与白蛋白、血清、血浆以及富含急性期反应物α1-酸性糖蛋白、α1-抗胰蛋白酶和C反应蛋白的血浆的蛋白结合率。还测定了其他镇痛抗炎药(吲哚美辛、酮洛芬、对乙酰氨基酚和水杨酸钠)以及其他碱性药物(丙吡胺、利多卡因、普萘洛尔和奎尼丁)对替马加汀结合的影响。替马加汀的结合在浓度高达0.5微克/毫升时呈浓度依赖性,但在此水平以上直至10.0微克/毫升时则与浓度无关,平均值和标准误为93.8±0.5%。白蛋白仅占与血浆结合的替马加汀的32.4%。血浆中富含急性期反应物会导致替马加汀结合率显著增加。与其他药物同时透析会导致替马加汀结合率显著降低。