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P.-P. Elena, C. Pollin, F. Bermon, T. Amar, T. Caillaud, H. Polzer; Snapshot Test for Investigating Gels of Anti-Glaucoma Compounds as Topical Formulations. Invest. Ophthalmol. Vis. Sci. 2009;50(13):6002. doi: https://doi.org/.
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To get predictive data on the ocular penetration of several compounds formulated as mucoadhesive polymer fluid gels in a time-sharing, money-saving test.
A single topical application of several 0.1% and 0.2% brimonidine tartrate formulations (mixture with various mixed polymers MP formulations: carbomer, polyvinylalcohol, povidone, etc...) into both eyes of pigmented rabbits, was compared to Alphagan® P 0.1%, Alphagan® P 0.15%, and Alphagan® 0.2%. The aqueous humor was sampled 15min, 30min, 40min, 60min, 120min, and 240min after treatment, and brimonidine content was evaluated by HPLC-MS.
Compared to Alphagan®, both the area under the curve (AUC15-240min) ratios and the Cmax ratios (at 40min) were within a same range, as shown in the following table:Formulation Cmax ratio vs Alphagan® AUC15-240min ratio vs Alphagan®Alphagan® 0.2% 1.00 1.00Alphagan® P 0.15% 0.64 0.95Alphagan® P 0.1% 0.73 0.82MP 701-04509-01 0.1% 1.05 0.88MP 701-04509 0.2% 1.58 2.33MP 730-0450901 0.2% 2.05 1.75MP 700-04509 0.2% 1.59 1.83Similar experiments were performed using 0.1%-timolol/2%-dorzolamide formulations vs Cosopt® and showed similar results.
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