Amorphous azithromycin with improved aqueous solubility and intestinal membrane permeability
Date
2015Author
Aucamp, Marique
Odendaal, Roelf
Liebenberg, Wilna
Hamman, Josias
Metadata
Show full item recordAbstract
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 (p50.05) 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
URI
http://hdl.handle.net/10394/18011https://www.tandfonline.com/doi/full/10.3109/03639045.2014.931967
https://doi.org/10.3109/03639045.2014.931967
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- Faculty of Health Sciences [2368]