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dc.contributor.authorMuankaew, Chutimon
dc.contributor.authorJansook, Phatsawee
dc.contributor.authorStefánsson, Einar
dc.contributor.authorLoftsson, Thorsteinn
dc.date.accessioned2015-05-07T12:05:50Zen
dc.date.available2015-05-07T12:05:50Zen
dc.date.issued2014-10-20en
dc.date.submitted2015en
dc.identifier.citationInt J Pharm. 2014, 474 (1-2):80-90en
dc.identifier.issn1873-3476en
dc.identifier.pmid25128698en
dc.identifier.doi10.1016/j.ijpharm.2014.08.013en
dc.identifier.urihttp://hdl.handle.net/2336/552374en
dc.descriptionTo access publisher's full text version of this article click on the hyperlink at the bottom of the pageen
dc.description.abstractIn effort to prepare an eye drop formulation of irbesartan, the effect of γ-cyclodextrin complexation on irbesartan solubilization in aqueous solutions was investigated. The optimum cyclodextrin concentration for formation of irbesartan/cyclodextrin inclusion complex was found to be 10% (w/v) and the solubility of ionized irbesartan/γ-cyclodextrin complex (at pH 7.2) was shown to be three fold greater than that of the unionized complex (at pH 4.3). The irbesartan flux through semipermeable membranes increased with increasing γ-cyclodextrin concentration at both pH values. However, the ionized complex displayed decrease in the drug permeation coefficient with increasing cyclodextrin concentration. The effect of four pharmaceutical excipients on the cyclodextrin solubilization was investigated. EDTA, hydroxypropyl methylcellulose, and tyloxapol increased complexation efficiency of γ-cyclodextrin while benzalkonium chloride had negligible effect. The largest solubilization was observed in the eye drop vehicle that contained all four excipients in addition to γ-cyclodextrin. Dynamic light scattering measurements disclosed that excipients had impact on size of complex aggregates and consequently on the drug flux through the semipermeable membranes. Complex of irbesartan/γ-cyclodextrin was characterized by FT-IR, (1)H NMR, XRPD, and TEM techniques.
dc.description.sponsorshipIcelandic Center of Research, (RANNÍS), University of Icelanden
dc.language.isoenen
dc.publisherElsevier/North-Holland Biomedical Pressen
dc.relation.urlhttp://dx.doi.org/ 10.1016/j.ijpharm.2014.08.013en
dc.rightsArchived with thanks to International journal of pharmaceuticsen
dc.subject.meshExcipientsen
dc.subject.meshOphthalmic Solutionsen
dc.titleEffect of γ-cyclodextrin on solubilization and complexation of irbesartan: influence of pH and excipients.en
dc.typeArticleen
dc.contributor.department1Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland; Faculty of Pharmacy, Siam University, 38 Petkasem Road, Phasicharoen, Bangkae, Bangkok 10160, Thailand. 2Faculty of Pharmaceutical Sciences, Chulalongkorn University, 254 Phayathai Road, Pathumwan, Bangkok 10330, Thailand. 3Department of Ophthalmology, Faculty of Medicine, National University Hospital, Eiríksgata 37, IS-101 Reykjavík, Iceland. 4Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Icelanden
dc.identifier.journalInternational journal of pharmaceuticsen
dc.rights.accessNational Consortium - Landsaðganguren
html.description.abstractIn effort to prepare an eye drop formulation of irbesartan, the effect of γ-cyclodextrin complexation on irbesartan solubilization in aqueous solutions was investigated. The optimum cyclodextrin concentration for formation of irbesartan/cyclodextrin inclusion complex was found to be 10% (w/v) and the solubility of ionized irbesartan/γ-cyclodextrin complex (at pH 7.2) was shown to be three fold greater than that of the unionized complex (at pH 4.3). The irbesartan flux through semipermeable membranes increased with increasing γ-cyclodextrin concentration at both pH values. However, the ionized complex displayed decrease in the drug permeation coefficient with increasing cyclodextrin concentration. The effect of four pharmaceutical excipients on the cyclodextrin solubilization was investigated. EDTA, hydroxypropyl methylcellulose, and tyloxapol increased complexation efficiency of γ-cyclodextrin while benzalkonium chloride had negligible effect. The largest solubilization was observed in the eye drop vehicle that contained all four excipients in addition to γ-cyclodextrin. Dynamic light scattering measurements disclosed that excipients had impact on size of complex aggregates and consequently on the drug flux through the semipermeable membranes. Complex of irbesartan/γ-cyclodextrin was characterized by FT-IR, (1)H NMR, XRPD, and TEM techniques.


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