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不同晶型的同一药物,由于其分子在各自晶型晶胞里的排列数目和位置及点阵形式不一样,导致药物分子之间、药物分子与溶剂分子之间的相互作用和结合方式不同,这必将影响各晶型的熔点、溶解度、溶出速率等理化性质,进而表现出稳定性、生物利用度及药效上的差异。七十年代以来,药物多晶型的问题已越来越多的引起了人们的关注,并成为控制药品生产及新药剂型研制前设计所不可缺少的重要组成部分。了解药物多晶型并熟悉其在药剂中的一些应用,将有助于我们进行新药新制剂的开发,以实现提高药物临床疗效、减轻或避免药物的毒副反应的目的。
The same drug with different crystal form, due to the different number and location of molecules in their crystal units and their lattice forms, leads to different interactions and binding modes between drug molecules, drug molecules and solvent molecules, This will inevitably affect the physical and chemical properties such as melting point, solubility and dissolution rate of each crystal form, thereby showing the differences in stability, bioavailability and pharmacodynamics. Since the 1970s, the problem of drug polymorphism has drawn more and more attention and has become an indispensable and important part in the control of drug production and the design of new drug formulations. Knowing the polymorphism of the drug and becoming familiar with some of its applications in pharmaceuticals will help us to develop new preparations of new drugs so as to achieve the purpose of improving the clinical efficacy of drugs and reducing or avoiding the side effects of drugs.