Frömming K H, Ditter W, Horn D
J Pharm Sci. 1981 Jul;70(7):738-43. doi: 10.1002/jps.2600700707.
The interaction of 32 drugs of diverse chemical structure with cross-linked insoluble polyvinylpyrrolidone (crospovidone) was studied. By using a polymer to drug ratio of 10:1, the sorbed amount for 20 compounds was found to be less than 5%. After a 10-fold decrease of the polymer concentration, the sorbed amount of eight other compounds fell to or below the 5% level. Only tannic acid and hexylresorcinol exhibited a significantly stronger sorption tendency. The interaction appeared to be controlled by phenolic groups in the active ingredient. The binding can be quantified by an interaction constant Ks, whose definition is based on a bulk phase model of interaction via independent binding sites. The exceptionally strong binding of hexylresorcinol, however, apparently was caused by cooperative interacting of the hexyl groups in the bound state. Desorption studies revealed that the binding was fully reversible in all cases. Therefore, the presence of cross-linked polyvinylpyrrolidone as a disintegrant in pharmaceutical preparations is not expected to interfere with GI drug absorption.
研究了32种化学结构各异的药物与交联不溶性聚乙烯吡咯烷酮（交联聚维酮）的相互作用。当聚合物与药物的比例为10:1时，发现20种化合物的吸附量小于5%。聚合物浓度降低10倍后，其他8种化合物的吸附量降至或低于5%的水平。只有单宁酸和己基间苯二酚表现出明显更强的吸附倾向。这种相互作用似乎受活性成分中酚羟基的控制。结合作用可以用相互作用常数Ks来定量，其定义基于通过独立结合位点的体相相互作用模型。然而，己基间苯二酚异常强烈的结合显然是由结合态己基的协同相互作用引起的。解吸研究表明，在所有情况下结合都是完全可逆的。因此，预计在药物制剂中作为崩解剂的交联聚乙烯吡咯烷酮的存在不会干扰胃肠道药物吸收。
