Borchardt W, Heinzow B, Ziegler A
Infusionsther Klin Ernahr. 1987 Apr;14 Suppl 2:28-30.
The binding of different drugs to plasma proteins as well as the binding to other structures (e.g. dialysis membranes, i.v. delivery sets) is well documented and of therapeutic importance. Colloid solutions of macromolecules are widely used as plasma substitutes and plasma expanders. A possible binding of drugs to these macromolecules was investigated by means of equilibrium dialysis. Benzodiazepines, beta-blockers, cardiac glycosides, local anesthetics, non steroidal antiinflammatory drugs, glibenclamide, phenobarbitone and phenprocoumon (10(-7) in 50 mM tris buffer, pH 7.4) were dialyzed against tris buffer diluted (1:5) commercially available plasma substitutes consisting of hydroxyethyl starch (HES), dextran, gelatine and polyvinylpyrrolidone (PVP). Binding to plasma substitutes was observed with the highest values for penbutolol and oxypolygelatine (41%), digitoxin and HES 200 (35%), phenprocoumon and PVP (43%). It is concluded that the binding of drugs to plasma substitutes is in most cases negligible and not of clinical relevance. Since some drugs seem to bind to some extent to different macromolecules this should be borne in mind and could be of some influence e.g. in perfusion experiments with isolated organs.
不同药物与血浆蛋白的结合以及与其他结构（如透析膜、静脉输液装置）的结合已有充分记录，且具有治疗重要性。大分子胶体溶液被广泛用作血浆代用品和血浆扩容剂。通过平衡透析研究了药物与这些大分子的可能结合。将苯二氮䓬类、β受体阻滞剂、强心苷、局部麻醉药、非甾体抗炎药、格列本脲、苯巴比妥和苯丙香豆素（在50 mM Tris缓冲液，pH 7.4中浓度为10⁻⁷）与用市售血浆代用品（由羟乙基淀粉（HES）、右旋糖酐、明胶和聚乙烯吡咯烷酮（PVP）组成）稀释（1:5）的Tris缓冲液进行透析。观察到药物与血浆代用品的结合情况，喷布洛尔和氧化聚明胶的结合率最高（41%），地高辛和HES 200的结合率为（35%），苯丙香豆素和PVP的结合率为（43%）。得出的结论是，在大多数情况下，药物与血浆代用品的结合可忽略不计，不具有临床相关性。由于一些药物似乎在一定程度上与不同的大分子结合，因此应予以考虑，例如在离体器官灌注实验中可能会有一定影响。
