Crystal Transition and Drug-excipient Compatibility of Clarithromycin in Sustained Release Tablets
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Published:2020-08-17
Issue:7
Volume:16
Page:950-959
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ISSN:1573-4129
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Container-title:Current Pharmaceutical Analysis
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language:en
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Short-container-title:CPA
Author:
Li Yu1, Kong Xiangwen2, Hu Fan3
Affiliation:
1. Chemical Drug Department, Zhejiang Institute for Food and Drug Control, Hangzhou 310052, China 2. Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd., Hangzhou 310011, China 3. Westlake university, Westlake institute for advanced study, Hangzhou 310024, China
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.
Funder
Zhejiang Food and Drug Administration
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmaceutical Science,Molecular Medicine,Biochemistry,Biophysics
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