Cyclodextrin formulation of dorzolamide and its distribution in the eye after topical administration

2.50
Hdl Handle:
http://hdl.handle.net/2336/69193
Title:
Cyclodextrin formulation of dorzolamide and its distribution in the eye after topical administration
Authors:
Sigurdsson, Hakon H; Stefansson, Einar; Gudmundsdottir, Elinborg; Eysteinsson, Thor; Thorsteinsdottir, Margret; Loftsson, Thorsteinn
Citation:
J Control Release. 2005, 102(1):255-62
Issue Date:
20-Jan-2005
Abstract:
Due to limited aqueous solubility of dorzolamide at physiologic pH, the pH of Trusopt eye drops (cont. 2% dorzolamide) has to be kept at about 5.65, and to increase the topical bioavailability of the drug from Trusopt the contact time of the drug with the eye surface is increased by increasing the viscosity of the eye drops to 100 cps. This low pH and high viscosity can lead to local irritation. In this study, dorzolamide hydrochloride was formulated as 2% and 4% low viscosity solutions (viscosity 3 to 5 cps) containing randomly methylated beta-cyclodextrin at pH 7.45. These formulations were evaluated in rabbits. The animals were sacrificed at various time points after topical administration of the drug and the dorzolamide concentration determined in the different parts of the eye. Trusopt was used as a reference standard. The topical availability of dorzolamide from the cyclodextrin-containing eye drops appeared to be comparable to that from Trusopt and the drug reached retina and optic nerve to give measurable concentrations for at least 8 h after administration of the eye drops.
Description:
To access publisher full text version of this article. Please click on the hyperlink in Additional Links field
Additional Links:
http://www.sciencedirect.com/science/article/B6T3D-4DTP391-5/2/ac5c577b34945a211592ff09cb68d879

Full metadata record

DC FieldValue Language
dc.contributor.authorSigurdsson, Hakon H-
dc.contributor.authorStefansson, Einar-
dc.contributor.authorGudmundsdottir, Elinborg-
dc.contributor.authorEysteinsson, Thor-
dc.contributor.authorThorsteinsdottir, Margret-
dc.contributor.authorLoftsson, Thorsteinn-
dc.date.accessioned2009-05-27T15:04:19Z-
dc.date.available2009-05-27T15:04:19Z-
dc.date.issued2005-01-20-
dc.date.submitted2009-05-27-
dc.identifier.citationJ Control Release. 2005, 102(1):255-62en
dc.identifier.issn0168-3659-
dc.identifier.pmid15653150-
dc.identifier.doi10.1016/j.jconrel.2004.10.004-
dc.identifier.urihttp://hdl.handle.net/2336/69193-
dc.descriptionTo access publisher full text version of this article. Please click on the hyperlink in Additional Links fielden
dc.description.abstractDue to limited aqueous solubility of dorzolamide at physiologic pH, the pH of Trusopt eye drops (cont. 2% dorzolamide) has to be kept at about 5.65, and to increase the topical bioavailability of the drug from Trusopt the contact time of the drug with the eye surface is increased by increasing the viscosity of the eye drops to 100 cps. This low pH and high viscosity can lead to local irritation. In this study, dorzolamide hydrochloride was formulated as 2% and 4% low viscosity solutions (viscosity 3 to 5 cps) containing randomly methylated beta-cyclodextrin at pH 7.45. These formulations were evaluated in rabbits. The animals were sacrificed at various time points after topical administration of the drug and the dorzolamide concentration determined in the different parts of the eye. Trusopt was used as a reference standard. The topical availability of dorzolamide from the cyclodextrin-containing eye drops appeared to be comparable to that from Trusopt and the drug reached retina and optic nerve to give measurable concentrations for at least 8 h after administration of the eye drops.en
dc.language.isoenen
dc.publisherElsevier Science Publishersen
dc.relation.urlhttp://www.sciencedirect.com/science/article/B6T3D-4DTP391-5/2/ac5c577b34945a211592ff09cb68d879en
dc.subject.meshAdministration, Topicalen
dc.subject.meshAnimalsen
dc.subject.meshChemistry, Pharmaceuticalen
dc.subject.meshCyclodextrinsen
dc.subject.meshEyeen
dc.subject.meshRabbitsen
dc.subject.meshSulfonamidesen
dc.subject.meshThiophenesen
dc.titleCyclodextrin formulation of dorzolamide and its distribution in the eye after topical administrationen
dc.typeArticleen
dc.contributor.departmentFaculty of Pharmacy, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland.en
dc.identifier.journalJournal of controlled release : official journal of the Controlled Release Societyen

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