dc.contributor.author | Aucamp, Marique | |
dc.contributor.author | Odendaal, Roelf | |
dc.contributor.author | Liebenberg, Wilna | |
dc.contributor.author | Hamman, Josias | |
dc.date.accessioned | 2016-07-22T06:34:32Z | |
dc.date.available | 2016-07-22T06:34:32Z | |
dc.date.issued | 2015 | |
dc.identifier.citation | Aucamp, M. et al. 2015. Amorphous azithromycin with improved aqueous solubility and intestinal membrane permeability. Drug development and industrial pharmacy, 41(7):1100-1108. [https://doi.org/10.3109/03639045.2014.931967] | en_US |
dc.identifier.issn | 0363-9045 | |
dc.identifier.issn | 1520-5762 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/18011 | |
dc.identifier.uri | https://www.tandfonline.com/doi/full/10.3109/03639045.2014.931967 | |
dc.identifier.uri | https://doi.org/10.3109/03639045.2014.931967 | |
dc.description.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 (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 | en_US |
dc.description.sponsorship | National Research Foundation (NRF); Centre of Excellence for Pharmaceutical Sciences of the North-West
University, Potchefstroom, South Africa | en_US |
dc.language.iso | en | en_US |
dc.publisher | Taylor & Francis | en_US |
dc.subject | Amorphous | en_US |
dc.subject | Apparent permeability coefficient | en_US |
dc.subject | Azithromycin | en_US |
dc.subject | Dissolution | en_US |
dc.subject | Solubility | en_US |
dc.subject | Vapor sorption | en_US |
dc.title | Amorphous azithromycin with improved aqueous solubility and intestinal membrane permeability | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 11927860 - Aucamp, Marique Elizabeth | |
dc.contributor.researchID | 10196226 - Liebenberg, Wilna | |
dc.contributor.researchID | 10081097 - Hamman, Josias Hendrik | |