【摘要】：目的:研究鹽酸樂卡地平Ⅰ、Ⅱ晶型及無定型對制劑制備的影響,為其制劑開發(fā)及一致性評價提供理論基礎。方法:采用X-射線粉末衍射(XRD)、紅外分光光度(IR)和差式掃描量熱(DSC)法鑒定鹽酸樂卡地平的3種晶型;采用XRD法比較粉粹、研磨、加壓工藝,濕法制粒中黏合劑溶劑(水、乙醇)和干燥溫度(50、60、70℃)對鹽酸樂卡地平3種晶型穩(wěn)定性的影響;比較3種晶型鹽酸樂卡地平片在水、鹽酸、p H 4.5醋酸鹽緩沖液、p H 6.8磷酸鹽緩沖液4種介質中的體外溶出度。結果:XRD顯示,Ⅰ、Ⅱ晶型均有特征衍射峰,且2θ值不一致,無定型無特征衍射峰;IR顯示,3種晶型具有不同的吸收強度和吸收峰數(shù)目;DSC顯示,Ⅰ、Ⅱ晶型分別在194.6、207.3℃有明顯吸熱峰,無定型在86.1℃有明顯吸熱峰、299.8℃有放熱峰。粉粹、研磨、加壓及干燥溫度對3種晶型轉變均無影響;濕法制粒時水對晶型轉變無影響,乙醇會引起Ⅰ晶型的晶型轉變。除在鹽酸中Ⅰ晶型與Ⅱ晶型片比較f_2=68外,4種介質中3種晶型鹽酸樂卡地平片溶出度兩兩比較的f_2均小于50。結論:XRD、IR、DSC法均能鑒定鹽酸樂卡地平的3種晶型。用Ⅰ晶型制備鹽酸樂卡地平片時,濕法制粒應避免使用乙醇作為黏合劑溶劑,建議使用水。不同晶型會影響所制鹽酸樂卡地平片的體外溶出度。
[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，

本文編號：2319607