CAJ | 학술논문

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。
약물적불동정형회영향약효급기생물이용도，약물정형급기함량적학정시학보약물산품적최종질량병지도약물제제개발화생산적주요문제。침대근년래고체약물다정형정량분석영역적연구진전진행료종술，병결합실례대3류정량분석방법（X사선분말연사（XRPD）법、광보법、열분석법）적특점、괄용장합진행료분석평술。목전XRPD법잉시감별다정형적최주요수단，단정체적택우취향여시양제비과정균회영향정량분석적준학도。각충광보법대우정체결구차이적민감성고，차쾌속、무손검측，시양처리간단，재정형정량분석중적응용구유잠력。열분석법대시양구유불가역손해，단유우기준학도상대교고차조작방편，장래잉회득도엄범응용。
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.