Gramaglia Daniela, Conway Barbara R, Kett Vicky L, Malcolm R Karl, Batchelor Hannah K
Department of Pharmaceutical Chemistry, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy.
Int J Pharm. 2005 Sep 14;301(1-2):1-5. doi: 10.1016/j.ijpharm.2005.04.038.
Conventional differential scanning calorimetry (DSC) techniques are commonly used to quantify the solubility of drugs within polymeric-controlled delivery systems. However, the nature of the DSC experiment, and in particular the relatively slow heating rates employed, limit its use to the measurement of drug solubility at the drug's melting temperature. Here, we describe the application of hyper-DSC (HDSC), a variant of DSC involving extremely rapid heating rates, to the calculation of the solubility of a model drug, metronidazole, in silicone elastomer, and demonstrate that the faster heating rates permit the solubility to be calculated under non-equilibrium conditions such that the solubility better approximates that at the temperature of use. At a heating rate of 400 degrees C/min (HDSC), metronidazole solubility was calculated to be 2.16 mg/g compared with 6.16 mg/g at 20 degrees C/min.
传统的差示扫描量热法（DSC）技术通常用于量化药物在聚合物控释系统中的溶解度。然而，DSC实验的性质，特别是所采用的相对较慢的升温速率，限制了其仅用于测量药物在熔点温度时的溶解度。在此，我们描述了超DSC（HDSC）的应用，HDSC是DSC的一种变体，涉及极快的升温速率，用于计算模型药物甲硝唑在硅橡胶中的溶解度，并证明更快的升温速率允许在非平衡条件下计算溶解度，从而使溶解度更接近使用温度下的溶解度。在400℃/min的升温速率（HDSC）下，计算得出甲硝唑的溶解度为2.16mg/g，而在20℃/min时为6.16mg/g。
