作为潜在溶石剂的偶极非质子溶剂的物理化学研究。

Physicochemical investigations of dipolar aprotic solvents as potential cholelitholytic agents.

作者信息

Kennelly P, Corrigan O I

出版信息

J Pharm Pharmacol. 1987 Jun;39(6):471-4. doi: 10.1111/j.2042-7158.1987.tb03422.x.

DOI:10.1111/j.2042-7158.1987.tb03422.x

Abstract

A number of dipolar aprotic solvents have been examined as potential co-solvents for gallstone dissolution. The power of these agents to solubilize such gallstone components as cholesterol, calcium carbonate, calcium palmitate and palmitic acid was determined and compared with that of monooctanoin (Capmul), using the synthetic solubility method. The solubilities of cholesterol and palmitic acid were greater in the N-methyl, N-ethyl and N-butylpyrrolidone derivatives than in monooctanoin. In contrast, the solubilities of the calcium salts were very low (less than 0.25% w/w) in all solvents examined. The influence of N-methylpyrrolidone (NMP) on both the in-vitro dissolution of cholesterol from gallstones and the decrease in stone weight with time was determined. NMP proved to be a better solvent than monooctanoin for human stones. NMP, which is miscible with water and monooctanoin, may have potential as a co-solvent in the design of solvent systems for gallstones.

摘要

已对多种偶极非质子溶剂作为胆结石溶解潜在助溶剂进行了研究。采用合成溶解度法测定了这些试剂溶解胆固醇、碳酸钙、棕榈酸钙和棕榈酸等胆结石成分的能力，并与单辛脂（Capmul）进行了比较。胆固醇和棕榈酸在N-甲基、N-乙基和N-丁基吡咯烷酮衍生物中的溶解度比在单辛脂中更高。相比之下，在所研究的所有溶剂中，钙盐的溶解度都非常低（小于0.25% w/w）。测定了N-甲基吡咯烷酮（NMP）对胆结石中胆固醇体外溶解以及结石重量随时间减少的影响。结果证明，对于人体结石，NMP是比单辛脂更好的溶剂。NMP可与水和单辛脂混溶，在设计胆结石溶剂体系时，它可能具有作为助溶剂的潜力。