Kwan K H, Higuchi W I, Molokhia A M, Hofmann A F
J Pharm Sci. 1977 Aug;66(8):1105-8. doi: 10.1002/jps.2600660813.
Various compounds that might function as cholesterol gallstone dissolution accelerators were studied. The dissolution rates of cholesterol monohydrate pellets in synthetic bile (116 mM sodium cholate-32 mM lecithin) containing the agent at various concentration levels were determined. In the absence of any dissolution rate accelerator, the dissolution kinetics for cholesterol previously were found to be interfacial resistance controlled, and the rates were around 20 times less than the diffusion-controlled rates in the present experiments. Primary, secondary, and tertiary amines and quaternary ammonium compounds were effective accelerators. When the alkyl chain lengths were long enough and/or when the agent concentrations were high enough, the dissolution rates generally approached diffusion-controlled rates. Steroidal amines generally had good activity. Anionic and nonionic surfactants had little or negative activity.
对各种可能作为胆固醇胆结石溶解促进剂的化合物进行了研究。测定了一水合胆固醇颗粒在含有不同浓度该试剂的合成胆汁（116 mM胆酸钠 - 32 mM卵磷脂）中的溶解速率。在没有任何溶解速率促进剂的情况下，先前发现胆固醇的溶解动力学受界面阻力控制，其速率比本实验中扩散控制的速率低约20倍。伯胺、仲胺、叔胺和季铵化合物是有效的促进剂。当烷基链长度足够长和/或试剂浓度足够高时，溶解速率通常接近扩散控制的速率。甾体胺通常具有良好的活性。阴离子和非离子表面活性剂的活性很小或呈负活性。
