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Abstract
Azithromycin (AZM) is a poorly soluble macrolide antibacterial agent. Its low solubility is considered as the major contributing factor to its relatively low oral bioavailability. The aim of this study was to improve the solubility of this active pharmaceutical ingredient (API) by preparing an amorphous form by quench cooling of the melt and to study the influence of the improved solubility on membrane permeability. The amorphous azithromycin (AZM-A) exhibited a significant increase in water solubility when compared to the crystalline azithromycin dihydrate (AZM-DH). The influence that the improved solubility could have on membrane permeability was also studied. The apparent permeability coefficient (Papp) values of AZM-A were statistically significantly higher (p < 0.05) than crystalline AZM-DH at pH values of 6.8 and 7.2. The results therefore indicated that the improved solubility of AZM in the amorphous form also produced improved permeability across excised intestinal tissue at physiological pH values found in the small intestine.
Acknowledgements
The financial support of the National Research Foundation (NRF) and the Centre of Excellence for Pharmaceutical Sciences of the North-West University, Potchefstroom, South Africa is acknowledged.
Declaration of interest
The authors declare no conflict of interest. This study was financially support by the National Research Foundation (NRF) and the Centre of Excellence for Pharmaceutical Sciences of the North-West University, Potchefstroom, South Africa. Any opinion, findings and conclusions or recommendations expressed in this material are those of the authors and therefore the NRF do not accept any liability in regard thereto.