盐酸乐卡地平Ⅰ、Ⅱ晶型及无定型对制剂制备的影响
发布时间：2018-11-08 20:29
【摘要】：目的:研究盐酸乐卡地平Ⅰ、Ⅱ晶型及无定型对制剂制备的影响,为其制剂开发及一致性评价提供理论基础。方法:采用X-射线粉末衍射(XRD)、红外分光光度(IR)和差式扫描量热(DSC)法鉴定盐酸乐卡地平的3种晶型;采用XRD法比较粉粹、研磨、加压工艺,湿法制粒中黏合剂溶剂(水、乙醇)和干燥温度(50、60、70℃)对盐酸乐卡地平3种晶型稳定性的影响;比较3种晶型盐酸乐卡地平片在水、盐酸、p H 4.5醋酸盐缓冲液、p H 6.8磷酸盐缓冲液4种介质中的体外溶出度。结果:XRD显示,Ⅰ、Ⅱ晶型均有特征衍射峰,且2θ值不一致,无定型无特征衍射峰;IR显示,3种晶型具有不同的吸收强度和吸收峰数目;DSC显示,Ⅰ、Ⅱ晶型分别在194.6、207.3℃有明显吸热峰,无定型在86.1℃有明显吸热峰、299.8℃有放热峰。粉粹、研磨、加压及干燥温度对3种晶型转变均无影响;湿法制粒时水对晶型转变无影响,乙醇会引起Ⅰ晶型的晶型转变。除在盐酸中Ⅰ晶型与Ⅱ晶型片比较f_2=68外,4种介质中3种晶型盐酸乐卡地平片溶出度两两比较的f_2均小于50。结论:XRD、IR、DSC法均能鉴定盐酸乐卡地平的3种晶型。用Ⅰ晶型制备盐酸乐卡地平片时,湿法制粒应避免使用乙醇作为黏合剂溶剂,建议使用水。不同晶型会影响所制盐酸乐卡地平片的体外溶出度。
[Abstract]:Aim: to study the effect of the crystal form and amorphous form of Lecardipine hydrochloride on the preparation of the preparation, and to provide a theoretical basis for the development and consistency evaluation of the preparation. Methods: X-ray powder diffraction (XRD),) infrared spectrophotometry (IR) and differential scanning calorimetry (DSC) were used to identify the three crystal forms of Lecardipine hydrochloride. The effects of binder solvent (water, ethanol) in wet granulation and drying temperature (50 鈩，
本文编号：2319607
[Abstract]:Aim: to study the effect of the crystal form and amorphous form of Lecardipine hydrochloride on the preparation of the preparation, and to provide a theoretical basis for the development and consistency evaluation of the preparation. Methods: X-ray powder diffraction (XRD),) infrared spectrophotometry (IR) and differential scanning calorimetry (DSC) were used to identify the three crystal forms of Lecardipine hydrochloride. The effects of binder solvent (water, ethanol) in wet granulation and drying temperature (50 鈩，
本文编号：2319607
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