Institute of Biomedicine (IBUB) and Department of Chemical Engineering and Analytical Chemistry, Universitat de Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain.
Unitat de Polimorfisme i Calorimetria, Centres Científics i Tecnològics, Universitat de Barcelona, Baldiri Reixac 10, 08028 Barcelona, Spain.
Eur J Pharm Sci. 2020 May 30;148:105305. doi: 10.1016/j.ejps.2020.105305. Epub 2020 Mar 14.
The solubility of three drugs (glimepiride, pioglitazone, sibutramine) with different acid/base properties and expected supersaturation behavior was examined in detail using the shake-flask (SF) and potentiometric (CheqSol) methods. Both uncharged (free) species and hydrochloride salts were used as starting materials. On the one hand, the SF method provided information about the thermodynamic solubility at any pH value, including the counterion-dependent solubility of ionic species. Additionally, this method easily allowed the identification of the solid phase in equilibrated solutions by powder X-ray diffraction, and the detection and quantification of aggregation and complexation reactions. On the other hand, CheqSol method permitted the measurement of the equilibrium solubility of neutral species, the observation of changes in solid forms, and the extent and duration of supersaturation (kinetic solubility) for "chaser" compounds. The combined information from both methods gave an accurate picture of the solubility behavior of the studied drugs.
采用摇瓶法(SF)和电位法(CheqSol)详细考察了具有不同酸碱性质和预期过饱和行为的三种药物(格列美脲、吡格列酮、西布曲明)的溶解度。使用未带电(游离)形式和盐酸盐作为起始物质。一方面,SF 法提供了有关任何 pH 值下热力学溶解度的信息,包括离子物种的反离子依赖性溶解度。此外,该方法还可以通过粉末 X 射线衍射轻松识别平衡溶液中的固相,并检测和定量聚集和络合反应。另一方面,CheqSol 法允许测量中性物质的平衡溶解度,观察固体形式的变化,以及“追赶”化合物的过饱和度(动力学溶解度)的程度和持续时间。两种方法的综合信息准确地描绘了研究药物的溶解度行为。