Development of taste-masking microcapsules containing azithromycin by fluid bed coating for powder for suspension and in vivo evaluation

Abstract

This research aims to develop bitter taste-masking microcapsules containing azithromycin (AZI) by a simpler and familiar method, fluid-bed coating technology, in comparison with Zithromax^®. Cores of microcapsules, AZI microparticles, were prepared by fluid-bed granulation, then taste-masking polymer was covered on by fluid-bed coating technique. Eudragit L100, Eudragit RL100, and ethyl cellulose in single and combined with Eudragit L100 and Eudragit E100 were used as taste-masking polymers. The obtained microcapsules were characterised by taste-masking ability, in vitro release, SEM, coating thickness, and coating efficiency. Combination of ethyl cellulose and Eudragit E100 (3:1) in coating thickness of 45.13 ± 2.12% w/w prevents AZI release from microcapsules below bitter taste threshold (1.78 ± 1.17 µg/ml). Bioavailability of powders containing AZI microcapsules and pH modulators (50 mg Na₃PO₄ and 35 mg Mg(OH)₂) was not significantly different from the reference product (Zithromax^®, Pfizer, New York, NY) in the rabbit model (p > 0.05). These results support the possibility of developing a generic product containing AZI.

Keywords:

• Azithromycin
• bitter taste masking
• microcapsule
• Eudragit L100
• ethyl cellulose
• pH modulator
• bioavailability

Acknowledgements

The authors would like to acknowledge Le Thanh Lam from Mediplantex National Pharmaceutical Joint Stock Company for his help with material support. This research did not receive any other specific grant from funding agencies in the public, commercial, or not-for-profit sectors.

Disclosure statement

The authors report there are no competing interest to declare.

Additional information

Funding

The author(s) reported there is no funding associated with the work featured in this article.