Preparation of erythromycin microparticles with Eudragit S100 polymer using emulsion method for taste masking

Abstract

Background: Erythromycin is most effective against gram-positive bacteria such as pneumococci, streptococci, and some staphylococci. Erythromycin is generally safe in those who are allergic to penicillin. Erythromycin is the drug of choice in the treatment of neonatal respiratory chlamydia infections, eye infections bacteria and corynebacterium. Objective: Due to the bitter taste of erythromycin little acceptance among children and elderly leads to better acceptance in these cases is to modify the taste of erythromycin Method: Microspheres of erythromycin with pH-dependent polymer (such as Eudragits S100) were prepared by the emulsion solvent diffusion method (O1/O2). The effect of different polymer–drug ratios on the taste masking and the characteristics of the microspheres were investigated. In the current study formulations with different polymer/drug ratio were prepared and were characterized by drug loading, loading efficiency, yield, particle size, bitter taste threshold, x-ray diffraction (XRD), fourier transform spectroscopy (FTIR) and differential scanning calorimetry (DSC). The in vitro release studies were performed in pH 1.2 and 7.4. Results: The best polymer to drug ratio in microparticles were E1 (1:1 polymer to drug ratio) which showed 26.93%, 53.86% entrapment, loading efficiency, respectively and mean particle size of 426.62 µm. The FTIR, XRD and DSC showed the stable character of erythromycin in the drug-loaded microspheres and revealed an amorphous form. The results showed that microparticles prepared with pH-dependent polymer (Eudragit S100) were faster release than the commercial suspension (p<0.05). The results demonstrated that Eudragit S100 could for masking the unpleasant taste of erythromycin investigated. Conclusion: The results indicated that the microsphere formulation could be a promising drug carrier for masking the bitter taste of erythromycin.