Crystal Transition and Drug-excipient Compatibility of Clarithromycin in Sustained Release Tablets

Author(s): Yu Li*, Xiangwen Kong, Fan Hu

Journal Name: Current Pharmaceutical Analysis

Volume 16 , Issue 7 , 2020

DOI : 10.2174/1573412915666190328234326

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Graphical Abstract:


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.

Keywords: Clarithromycin, compatibility, differential scanning calorimetry, x-ray powder diffraction, infrared spectroscopy.

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Article Details

VOLUME: 16
ISSUE: 7
Year: 2020
Published on: 17 August, 2020
Page: [950 - 959]
Pages: 10
DOI: 10.2174/1573412915666190328234326
Price: $65

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