In vitro release - In vivo microbiological and toxicological studies on ketoconazole lipid granules

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dc.contributor.authorOzyazici, Mine
dc.contributor.authorGokce, Evren Homan
dc.contributor.authorOzer, Ozgen
dc.contributor.authorAy, Zeynep
dc.contributor.authorGuneri, Tamer
dc.contributor.authorErtan, Gokhan
dc.contributor.authorGokce, Goksel
dc.contributor.authorMetin, Dilek Yesim
dc.contributor.authorHilmioglu, Suleyha
dc.contributor.authorDurmaz, Guliz
dc.contributor.authorYalcin, Ayfer
dc.contributor.authorPekeetin, Cetin
dc.contributor.authorOzyurt, Dogan
dc.date.accessioned2019-10-27T19:38:55Z
dc.date.available2019-10-27T19:38:55Z
dc.date.issued2007
dc.departmentEge Üniversitesien_US
dc.description.abstractIn some multidrug therapy programs, ketoconazole (KTZ) may be administered with some antacids that could modify its dissolution rate and reduce its absorption, thus leading to therapeutic failures. The primary aim of this study was to evaluate the influence of Compritol HD5 ATO and Compritol 888 ATO on this interaction in comparison with commercial KTZ tablets. The second aim was to prepare lipid granules of KTZ that could be an alternative to the commercial formulation. Therefore, six KTZ sustained-release granules were prepared with different lipid concentrations, because they were found to be more suitable than tablets that are dissolved only in gastric medium. The results confirmed that the dissolution rate of KTZ granules was significantly reduced in the presence of antacids. The ideal formulation was selected as granules including 5% of Compritol lipids in relation to the suitability of the target profile. Therapeutic effects of orally administered, ideal KTZ granule formulations, and commercial tablets were evaluated in vivo by the experimental model of murine vulvo-vaginal candidiasis (VVC) with and without antacids. It was found that formulations were very effective on VVC, and the therapeutic effect decreased significantly in the presence of antacids. Histopathological studies were carried out for vagina, stomach, and liver tissues and hepatoxicity was also examined. The levels of reduced glutathione (GSH) were measured to assess the oxidative stress induced by KTZ and function of the liver. It was observed that orally administered formulations of KTZ were successful in treating candidiasis in mice without irritancy in stomach. However, liver tissues were damaged. The decreased GSH levels indicated toxicity in our study. This study suggested that in vitro release and in vivo microbiological-toxicological properties of KTZ were affected by antacids and drug-excipient interactions. Lipid granules of KTZ prepared with Compritol 888 ATO could be proposed as a new KTZ solid dosage form with optimum dissolution and therapeutic characteristics.en_US
dc.identifier.doi10.1080/10837450701560968en_US
dc.identifier.endpage590en_US
dc.identifier.issn1083-7450
dc.identifier.issue6en_US
dc.identifier.pmid18161631en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage581en_US
dc.identifier.urihttps://doi.org/10.1080/10837450701560968
dc.identifier.urihttps://hdl.handle.net/11454/40128
dc.identifier.volume12en_US
dc.identifier.wosWOS:000252090500005en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Incen_US
dc.relation.ispartofPharmaceutical Development and Technologyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectketoconazoleen_US
dc.subjectvulvo-vaginal candidiasisen_US
dc.subjectantaciden_US
dc.subjectdrug releaseen_US
dc.subjectPEGen_US
dc.subjecthepatotoxicityen_US
dc.titleIn vitro release - In vivo microbiological and toxicological studies on ketoconazole lipid granulesen_US
dc.typeArticleen_US

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