Preparation of Erythromycin microparticles with alginate sodium and carbomer 934p polymers for taste masking

Abstract

Background: Clarithromycin (CLA), a semi-synthetic mac¬rolide, is a broad-spectrum antibiotic with excel¬lent activity against gram positive, some gram negative and anaerobic bacteria. It is very bitter and as yet no mouth dissolving taste-masked preparation that might be useful in pediatric and geriatric patients is available in the market. Objective: Due to the bitter taste of clarithromycin little acceptance among children and elderly leads to better acceptance in these cases is to modify the taste of clarithromycin. Method: Microspheres of clarithromycin with polymers (such as sodium alginate and/carbomer 934p) were prepared by gelation ionotropic method by using calcium chloride. In the current study formulations with different polymer/s drug ratio were prepared and were characterized by drug loading, loading efficiency, yield, particle size, bitter taste threshold and differential scanning calorimetry (DSC). The in vitro release studies were performed in phosphate buffer (pH 6.8). Results: The best polymer/s to drug ratio in microparticles were Cl3 (3.84:1, alginate to Cl ratio) and Cl6 (1:9.6:2.5 carbomer to alginate to Cl ratio) which showed 19.43%, 17.1% entrapment, 94.06%, 89.65% loading efficiency and mean particle size of 1006, 2162.70 µm, respectively. The DSC showed the stable character of chlarithromycin in the drug-loaded microspheres and revealed crystal form. The results showed that microparticles prepared with polymer/s were faster release than the caplet® (p<0.05). The results demonstrated that microparticles-loaded could for masking the unpleasant taste of clarithromycin investigated. Conclusion: The results indicated that the prepared formulations could be a promising drug carrier for masking the bitter taste of clarithromycin.