Vallner J J, Speir W A, Kolbeck R C, Harrison G N, Bransome E D
Am Rev Respir Dis. 1979 Jul;120(1):83-6. doi: 10.1164/arrd.1979.120.1.83.
The binding of theophylline to serum protein within the pH range of 7.0 to 7.8 was determined by equilibrium dialysis using serum from 8 healthy adult volunteers. The percentage of theophylline bound was independent of the total concentration of the drug, but was directly related to pH. Because changes in the free fraction of theophylline may alter the therapeutic response, toxic effects, and pharmacokinetics, any future studies of the pharmacology of theophylline should include assessment of the acid-base status of the patients and measurements of free as well as total theophylline concentrations.
使用8名健康成年志愿者的血清,通过平衡透析法测定了在pH值7.0至7.8范围内茶碱与血清蛋白的结合情况。结合的茶碱百分比与药物总浓度无关,但与pH值直接相关。由于茶碱游离部分的变化可能会改变治疗反应、毒性作用和药代动力学,因此未来任何关于茶碱药理学的研究都应包括对患者酸碱状态的评估以及游离和总茶碱浓度的测量。