Title:Crystal Transition and Drug-excipient Compatibility of Clarithromycin in Sustained Release Tablets
VOLUME: 16 ISSUE: 7
Author(s):Yu Li*, Xiangwen Kong and Fan Hu
Affiliation: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
Keywords:Clarithromycin, compatibility, differential scanning calorimetry, x-ray powder diffraction, infrared spectroscopy.
Abstract:
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.
Methods 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 for the incompatibility of clarithromycin with high concentration
of alcohol was crystal transition.