Rodríguez-Spong Barbara, Price Christopher P, Jayasankar Adivaraha, Matzger Adam J, Rodríguez-Hornedo Naír
Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI 48109-1065, USA.
Adv Drug Deliv Rev. 2004 Feb 23;56(3):241-74. doi: 10.1016/j.addr.2003.10.005.
The diversity of solid-state forms that an active pharmaceutical ingredient (API) may attain relies on the repertoire of non-covalent interactions and molecular assemblies, the range of order, and the balance between entropy and enthalpy that defines the free energy landscape. It is recognized that crystallization is associated with molecular recognition events that lead to self-assembly, and that pharmaceutical function and thermodynamic stability can be altered with a slight change in the interacting molecules or their molecular network motifs. Our current understanding of pharmaceutical solids in terms of molecular recognition and complementarity provides new insights into the design and function of single and fully miscible, multiple-component solids with varying degrees of order, from amorphous to crystalline states, and in this way is leading the path to supramolecular pharmaceutics. This review describes pharmaceutical solids in terms of supramolecular chemistry and crystal engineering concepts, and discusses the events that control crystallization and solid phase transformations.
活性药物成分（API）可能呈现的固态形式的多样性取决于非共价相互作用和分子组装的种类、有序程度的范围以及定义自由能态势的熵与焓之间的平衡。人们认识到，结晶与导致自组装的分子识别事件相关，并且药物功能和热力学稳定性会因相互作用分子或其分子网络基序的微小变化而改变。我们目前从分子识别和互补性角度对药物固体的理解为设计和功能各异的单一组分和完全互溶的多组分固体提供了新的见解，这些固体具有从无定形到结晶态的不同有序程度，从而引领了超分子药物学的发展道路。本综述从超分子化学和晶体工程概念的角度描述了药物固体，并讨论了控制结晶和固相转变的事件。
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