Yu Li*, Xiangwen Kong and Fan Hu Pages 1 - 9 ( 9 )
Background: Clarithromycin is widely used for infections of helicobacter pylori. Clarithromycin belongs to polymorphic drug. Crystalline state changes of clarithromycin in sustained release tablets were found.Objective: The aim of this study was to find the influential factor of the crystal transition of clarithromycin in preparation process of sustained release tablets and to investigate the possible interactions between the clarithromycin and pharmaceutical excipients. Method and Results: The crystal transition of active pharmaceuticals ingredients from form Ⅱ to form Ⅰ in portion in clarithromycin sustained release tablets were confirmed by x-ray powder diffraction. The techniques including differential scanning calorimetry and infrared spectroscopy, x-ray powder diffraction were used for assessing the compatibility between clarithromycin and several excipients as: magnesium stearate, lactose, sodium carboxymethyl cellulose, polyvinyl-pyrrolidone K-30 and microcrystalline cellulose. All of these methods showed compatibilities between clarithromycin and the selected excipients. Alcohol prescription simulation was also done, which showed incompatibility between clarithromycin and concentration alcohol. Conclusion: It was confirmed that the reason of the incompatibility of clarithromycin with high concentration of alcohol was crystal transition.
clarithromycin; compatibility; differential scanning calorimetry; x-ray powder diffraction; infrared spectroscopy.
Chemical Drug Department, Zhejiang Institute for Food and Drug Control, Hangzhou 310052,, Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd., Hangzhou 310011, , Westlake university, Westlake institute for advanced study, Hangzhou 310024