CAJ | 학술논문

目的：对盐酸厄洛替尼A晶型、B晶型进行鉴定，了解制剂过程对晶型稳定性的影响，确定A晶型盐酸厄洛替尼片的开发工艺。方法：通过X射线粉末衍射（XRD）、红外分光光度法（IR）、电镜扫描（SEM）和差式扫描量热分析（DSC），对两种晶型进行鉴定。通过XRD技术对晶型的转化进行研究，并比较两种晶型的理化性质及片剂在溶出介质中的溶出行为差异，对片剂的工艺开发进行初步研究。结果：两种晶型具有不同的晶型特征。 A晶型溶解性好，溶出速度快，稳定性差；而B晶型具有较好的稳定性。湿法制粒中润湿剂的加入会导致A晶型转变为B晶型。结论：采用XRD、IR、SEM和DSC技术可以对药物晶型进行快速、准确的鉴定。以A晶型替代B晶型制备盐酸厄洛替尼片，采用干法制粒，但需改善包装，保证晶型的稳定性。
목적：대염산액락체니A정형、B정형진행감정，료해제제과정대정형은정성적영향，학정A정형염산액락체니편적개발공예。방법：통과X사선분말연사（XRD）、홍외분광광도법（IR）、전경소묘（SEM）화차식소묘량열분석（DSC），대량충정형진행감정。통과XRD기술대정형적전화진행연구，병비교량충정형적이화성질급편제재용출개질중적용출행위차이，대편제적공예개발진행초보연구。결과：량충정형구유불동적정형특정。 A정형용해성호，용출속도쾌，은정성차；이B정형구유교호적은정성。습법제립중윤습제적가입회도치A정형전변위B정형。결론：채용XRD、IR、SEM화DSC기술가이대약물정형진행쾌속、준학적감정。이A정형체대B정형제비염산액락체니편，채용간법제립，단수개선포장，보증정형적은정성。
Objective: To identify the polymorph crystal A and B of erlotinib hydrochloride, to learn the influence of preparation process on crystal stability and to determine the development process of er-lotinib hydrochloride tablets with polymorph A. Methods: X-ray diffraction (XRD), infrared spectrophotome-try (IR), scanning electron microscopy (SEM) and differential scanning calorimetry (DSC) were applied to study the polymorph A and B of erlotinib hydrochloride for their physicochemical properties and the crystal transformation between A and B. In addition, in vitro dissolution tests were conducted to determine the dissolution profiles of each crystal form and the development process was also studied preliminarily. Re-sults: Polymorph A and B demonstrated explicit disparity in crystal form characteristic, dissolution rate and stability, wherein polymorph A was thermodynamically unstable with better solubility and faster dissolution rate. Wetting agent added in wet granulation would transform crystal A into B. Conclusion: This study in-dicates that XRD, IR, SEM and DSC can be used to identify polymorphs rapidly and accurately. To devel-op erlotinib hydrochloride tablets of polymorph A by dry granulation process, the stability of polymorph should be ensured by improving packaging technology.