Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Drug Dev Ind Pharm. 2011 Jan;37(1):62-71. doi: 10.3109/03639045.2010.491831. Epub 2010 Jun 14.
Basic physicochemical properties including their apparent solubility in aqueous buffer and vegetable oils of a series of 11 peptidomimetics varying with respect to chain length and degree of N-methylation were estimated. It was observed that the compounds in contact with water transformed into sticky, slowly dissolving semisolid materials. Based on these observations, the in vitro release behavior of selected peptide derivatives from oil solutions and in situ formed precipitates was investigated using a validated in vitro release model.
The results of this investigation suggest that both types of oil-based drug delivery systems might constitute alternative sustained release formulation principles of such amorphous peptide derivatives for the intra-articular route of administration.
研究了一系列 11 种肽类似物的基本物理化学性质，包括其在水缓冲液和植物油中的表观溶解度，这些肽类似物在链长和 N-甲基化程度上有所不同。结果发现，与水接触的化合物会变成粘性的、缓慢溶解的半固体物质。基于这些观察结果，使用经过验证的体外释放模型研究了选定的肽衍生物从油溶液和原位形成的沉淀物中的体外释放行为。
这项研究的结果表明，这两种类型的油基药物传递系统都可能构成此类无定形肽衍生物用于关节内给药途径的替代持续释放制剂原则。
