Morrison Henry G, Sun Changquan C, Neervannan Sesha
Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320, USA.
Int J Pharm. 2009 Aug 13;378(1-2):136-9. doi: 10.1016/j.ijpharm.2009.05.039. Epub 2009 May 27.
Deep eutectic solvent (DES) is a new class of solvents typically formed by mixing choline chloride with hydrogen bond donors such as amines, acids, and alcohols. Most DES's are non-reactive with water, biodegradable, and have acceptable toxicity profiles. Urea-choline chloride and malonic acid-choline chloride eutectic systems were characterized using differential scanning calorimetry (DSC) and thermal microscopy. A potential new 2:1 urea-choline chloride cocrystal with a melting point of 25 degrees C was characterized at the eutectic composition. The formation of this cocrystal suggests that DES should not be universally explained by simple eutectic melting, and may be useful in guiding the search for new DES systems. The lack of nucleation of the malonic acid-choline chloride system prohibited the construction of a phase diagram for this system using DSC. We also investigated possible uses of DES in solubilizing poorly soluble compounds for enhanced bioavailability in early drug development such as toxicology studies. For five poorly soluble model compounds, solubility in DES is 5 to 22,000 folds more than that in water. Thus, DES can be a promising vehicle for increasing exposure of poorly soluble compounds in preclinical studies.
深共熔溶剂(DES)是一类新型溶剂,通常由氯化胆碱与氢键供体(如胺、酸和醇)混合而成。大多数DES与水不发生反应,可生物降解,且具有可接受的毒性特征。采用差示扫描量热法(DSC)和热显微镜对尿素-氯化胆碱和丙二酸-氯化胆碱共晶体系进行了表征。在共晶组成下,对一种熔点为25℃的潜在新型2:1尿素-氯化胆碱共晶体进行了表征。这种共晶体的形成表明,DES不应一概而论地用简单的共晶熔化来解释,这可能有助于指导新型DES体系的探索。丙二酸-氯化胆碱体系缺乏成核作用,因此无法用DSC构建该体系的相图。我们还研究了DES在早期药物开发(如毒理学研究)中增溶难溶性化合物以提高生物利用度方面的潜在用途。对于五种难溶性模型化合物,其在DES中的溶解度比在水中高5至22000倍。因此,在临床前研究中,DES有望成为增加难溶性化合物暴露量的载体。