Parsons D L, Vallner J J
J Pharm Sci. 1979 May;68(5):546-51. doi: 10.1002/jps.2600680507.
Application of dynamic dialysis to drug binding to erythrocytes was found to be more complex than previously described. Drug molecules located intracellularly in erythrocytes must diffuse through erythrocytes membranes before diffusing through the dialysis membrane to the external sink in dynamic dialysis. One must consider drug within the dialysis sack and within the erythrocyte and their corresponding volumes. When binding occurs in these internal compartments, different equations result for computing Dt, the total drug within the dialysis bag. With these equations and theoretically generated data, the results of "double dialysis" on the data produced in dynamic dialysis studies of drug-erythrocyte interactions were examined. The intracellular binding of drug by the erythrocyte to a single class of preexisting noninteracting sites could be misinterpreted as cooperative binding, or binding to at least two classes of sites, when the data of dynamic dialysis are treated in the Scatchard format.
动态透析在药物与红细胞结合中的应用比之前描述的更为复杂。红细胞内的药物分子在动态透析中必须先穿过红细胞膜,然后才能穿过透析膜扩散到外部接收器。必须考虑透析袋内和红细胞内的药物及其相应体积。当在这些内部隔室中发生结合时,计算透析袋内总药物量Dt会得到不同的方程。利用这些方程和理论生成的数据,对药物 - 红细胞相互作用动态透析研究中产生的数据进行“双重透析”的结果进行了检验。当以Scatchard格式处理动态透析数据时,红细胞对单一类预先存在的非相互作用位点的药物细胞内结合可能会被误解为协同结合,或与至少两类位点的结合。