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

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. Objectives: 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.This randomized clinical trial recruited 60 rural women at higher risk of breast cancer in Babol, Iran in 2016. Thirty women from two randomly selected villages were assigned to the MI group. Two other villages were also randomly selected and 30 of their female residents were allocated to the control group. Eligible people were first identified by referring to the villages’ health centers. The participants were recruited using a table of random numbers and their informed consent was obtained. In the MIgroup, five 90-minute weekly sessions of MI were held. Conventional training was conducted in the control group. All subjects completed a researcher-made questionnaire at baseline (before the intervention), at the end of the study, and three months later. Data were analyzed using repeated measures analysis of variance, and Bonferroni, Friedman, Wilcoxon, and chi-square tests. Conclusion: It was confirmed that the reason of the incompatibility of clarithromycin with high concentration of alcohol was crystal transition.

Investigation of Drug-Excipient Compatibility Studies Using Validated RP-HPLC Method for Azelnidipine and Telmisartan Tablets

“…[5][6] During these studies bulk drug and excipients comes into contact with each other as physical admixtures in a fixed ratio, or as a preliminary dosage form; subject to several stress conditions. The physico-chemical and performance attributes of the bulk drug and excipients are then estimated using one or more analytical techniques [7][8][9][10][11].…”