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dc.contributor.authorAucamp, Marique
dc.contributor.authorOdendaal, Roelf
dc.contributor.authorLiebenberg, Wilna
dc.contributor.authorHamman, Josias
dc.date.accessioned2016-07-22T06:34:32Z
dc.date.available2016-07-22T06:34:32Z
dc.date.issued2015
dc.identifier.citationAucamp, 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.issn0363-9045
dc.identifier.issn1520-5762 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/18011
dc.identifier.urihttps://www.tandfonline.com/doi/full/10.3109/03639045.2014.931967
dc.identifier.urihttps://doi.org/10.3109/03639045.2014.931967
dc.description.abstractAzithromycin (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 intestineen_US
dc.description.sponsorshipNational Research Foundation (NRF); Centre of Excellence for Pharmaceutical Sciences of the North-West University, Potchefstroom, South Africaen_US
dc.language.isoenen_US
dc.publisherTaylor & Francisen_US
dc.subjectAmorphousen_US
dc.subjectApparent permeability coefficienten_US
dc.subjectAzithromycinen_US
dc.subjectDissolutionen_US
dc.subjectSolubilityen_US
dc.subjectVapor sorptionen_US
dc.titleAmorphous azithromycin with improved aqueous solubility and intestinal membrane permeabilityen_US
dc.typeArticleen_US
dc.contributor.researchID11927860 - Aucamp, Marique Elizabeth
dc.contributor.researchID10196226 - Liebenberg, Wilna
dc.contributor.researchID10081097 - Hamman, Josias Hendrik


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