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通过平衡透析法测定替马加汀的蛋白质结合率。

The protein binding of timegadine determined by equilibrium dialysis.

作者信息

George S, McBurney A, Ward J

出版信息

Br J Clin Pharmacol. 1984 Nov;18(5):785-90. doi: 10.1111/j.1365-2125.1984.tb02543.x.

Abstract

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.

摘要

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。

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本文引用的文献

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Clinical Pharmacokinetics of indomethacin.吲哚美辛的临床药代动力学
Clin Pharmacokinet. 1981 Jul-Aug;6(4):245-58. doi: 10.2165/00003088-198106040-00001.
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Intravenous propranolol in patients with inflammation.炎症患者静脉注射普萘洛尔
Br J Clin Pharmacol. 1982 Apr;13(4):577-8. doi: 10.1111/j.1365-2125.1982.tb01426.x.
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Determinants of the plasma protein binding of theophylline in health.健康状态下茶碱血浆蛋白结合的决定因素。
Br J Clin Pharmacol. 1983 Apr;15(4):399-405. doi: 10.1111/j.1365-2125.1983.tb01521.x.
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Characterization of chloroquine plasma protein binding in man.氯喹与人血浆蛋白结合的特性研究。
Br J Clin Pharmacol. 1983 Mar;15(3):375-7. doi: 10.1111/j.1365-2125.1983.tb01513.x.

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