固体药物晶型定量分析方法  

Quantitative Analyzing Methods for Polymorphism of Pharmaceuticals

作　　者：肖燕[1,2] 王静康[1,2] 尹秋响[1,2] 王永莉[1,2] 鲍颖[1,2] 郝红勋[1,2] 

机构地区：[1]天津大学化工学院国家工业结晶工程技术研究中心,天津300072 [2]天津化学化工协同创新中心,天津300072

出　　处：《石油化工》2015年第1期11-18,10,共8页Petrochemical Technology

基　　金：国家自然科学基金项目(21376165);天津市科技支撑计划重点项目(13ZCZDNC02000)

摘　　要：药物的不同晶型会影响药效及其生物利用度,药物晶型及其含量的确定是确保药物产品的最终质量并指导药物制剂开发和生产的主要问题。针对近年来固体药物多晶型定量分析领域的研究进展进行了综述,并结合实例对3类定量分析方法(X射线粉末衍射(XRPD)法、光谱法、热分析法)的特点、适用场合进行了分析评述。目前XRPD法仍是鉴别多晶型的最主要手段,但晶体的择优取向与试样制备过程均会影响定量分析的准确度。各种光谱法对于晶体结构差异的敏感性高,且快速、无损检测,试样处理简单,在晶型定量分析中的应用具有潜力。热分析法对试样具有不可逆损害,但由于其准确度相对较高且操作方便,将来仍会得到广泛应用。Different polymorphs of a pharmaceutical will affect its bioavailability and final performance. Identification and determination of the polymorphs has become one of the main problems to be solved for the ensuring of the final quality of the product and for guiding the development and manufacturing of new formulations. The state of art of the main quantitative analytical methods for the polymorphism was reviewed and discussed. The characteristics and the extent of application of these methods （including X-ray powder diffraction（XRPD） method,spectroscopy method,thermal analysis method） were compared and analyzed by examples. Currently,XRPD is still the most frequently used method although the preferred orientation of the crystals and the samples preparation will affect the accuracy of this method. The spectroscopy method has potential applications in the quantitative analysis of the polymorphs because of its high sensitivity,simple and quick preparation of samples and nondestructive testing. The differential scanning calorimetry method will be widely used in the future because of its high accuracy and convenience,despite of the irreversible damage to the samples.

关 键 词：药物晶型定量分析 X射线粉末衍射法 红外光谱法 Raman光谱法 固体核磁共振法 示差扫描量热法 

分 类 号：TQ460.72[医药卫生—药物分析学]