Optimisation of a floating tablet containing clarithromycin 500 mg

Abstract

The purpose of the research is to optimize the formulation of a gastric floating drug delivery system of clarithromycin 500 mg (CLA). CLA is a macrolide antibiotic, indicated in the treatment of sinusitis, pharyngitis, pneumonia, acute and chronic bronchitis, especially in the treatment of Helicobacter pylori (H. pylori) infection. The formulation design is retained in the stomach for prolonging the floating time to improve bioavailability, drug absorption. The excipients include polymers such as hydroxypropyl methyl cellulose (HPMC) to control drug release. Besides, sodium bicarbonate is generally used in pharmaceuticals as a source of carbon dioxide in effervescent tablets – has been used as a gas-forming agent in floating to prolong floating time and reducing gastric irritation. Preformulating testing is not the interaction between the ingredients together. In vitro floating time and vitro dissolution studies were carried out that the results of the best formulation with HPMC K100M, HPMC K15M and NaHCO3 are 22%; 12.5% và 14.7% based on concentrate of CLA. The formulations were designed by Design - Expert and BCPharsolf OTP. The result of research showed that the floating time is approximately 8.53 – 9.34 hours and drug release for 12 hours, respectively 25% (after 2 hours), 20 – 40% (after 4 hours) and over 80% (12 hours). The analytical method for determination and quantification of CLA such as high-performance liquid chromatography (HPLC) and Fourier transform infrared FTIR.