کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10613542 | 986893 | 2005 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Cyclodextrin formulation of dorzolamide and its distribution in the eye after topical administration
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
مهندسی مواد
بیومتریال
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چکیده انگلیسی
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 β-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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Controlled Release - Volume 102, Issue 1, 20 January 2005, Pages 255-262
Journal: Journal of Controlled Release - Volume 102, Issue 1, 20 January 2005, Pages 255-262
نویسندگان
Hakon H. Sigurdsson, Einar Stefánsson, ElÃnborg Gudmundsdóttir, Thór Eysteinsson, Margrét Thorsteinsdóttir, Thorsteinn Loftsson,