Jakubiak Paulina, Schuler Franz, Alvarez-Sánchez Rubén
Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Switzerland.
Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Switzerland.
Eur J Pharm Biopharm. 2016 Dec;109:43-48. doi: 10.1016/j.ejpb.2016.08.019. Epub 2016 Sep 17.
Thorough understanding and control of the different crystal forms of a drug product is key for fine chemistry and materials science; it ultimately determines the product's physicochemical properties and performance. In this work, we extend the application of a mechanistic dissolution-precipitation model to solvent-mediated solid form transformations. To address the relevance of the model, various kinetic solvent-mediated polymorphic transition studies were retrieved from the literature. Our model succeeds in accurately describing the experimental data, shedding light on the molecular steps driving the polymorphic conversion. Given its simplicity and mechanistic character, the model can be viewed as a useful tool to monitor, predict and optimize the solvent-mediated transformations of solid forms.
深入理解和控制药品的不同晶型是精细化学和材料科学的关键；这最终决定了产品的物理化学性质和性能。在这项工作中，我们将一种机械溶解-沉淀模型的应用扩展到溶剂介导的固态形式转变。为了探讨该模型的相关性，我们从文献中检索了各种动力学溶剂介导的多晶型转变研究。我们的模型成功地准确描述了实验数据，揭示了驱动多晶型转变的分子步骤。鉴于其简单性和机械特性，该模型可被视为监测、预测和优化溶剂介导的固态形式转变的有用工具。
