法莫替丁共晶提高溶出度的研究

基金项目: 国家“重大新药创制”科技重大专项资助项目(No.2011ZX09201-101-02)；江苏省六大高峰人才资助（A类）；中央高校基本科研业务费专项资金资助项目（No.JKP2011006）

Enhanced dissolution of famotidine by cocrystal formation with tartaric acid and maleic acid

摘要: 采用溶液结晶法制备了法莫替丁酒石酸共晶和法莫替丁-马来酸共晶,通过差示扫描量热法（DSC），红外光谱法（IR）和粉末X线衍射法（PXRD）对所制备的共晶进行了表征，利用PXRD数据建立了两种共晶的晶体结构。考察了共晶的溶出度，并与市售法莫替丁晶型B进行比较，结果表明在水及pH 4.5磷酸盐缓冲液中，共晶的溶出度有明显提高。
- 法莫替丁 /
- 共晶 /
- 溶出度 /
- 晶型 /
- 酒石酸 /
- 马来酸
Abstract: Famotidine-tartaric acid cocrystal and famotidine-maleic acid cocrystal were prepared by solution method and confirmed by differential scanning calorimetry (DSC),Fourier transform infrared spectroscopy (FTIR) and X-ray powder diffraction (PXRD) analysis.Crystal structures were determined from PXRD data.Cocrystal dissolution was assessed and compared with commercial available famotidine (form B).It was demonstrated that the cocrystal had significantly greater dissolution rate than famotidine and physical mixture in distilled water and phosphate buffer (pH 4.5).
- famotidine /
- cocrystal /
- dissolution /
- crystal form /
- tartaric acid /
- maleic acid