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[Antiglaucoma ophthalmic agents with prolonged action based on macromolecular excipients. 2. In vivo studies]
G Pergande1, S Keipert, A Klatt
1Sektion Chemie, Augenklinik der Charité der Humboldt-Universität zu Berlin.
Abstract:
The prolonged in vitro release of pilocarpine (1) from preparations containing polyacrylic acids were represented consecutively . A preparation of polyacrylic acid-F (PAS-F; an acrylic-methacrylic acid copolymer) does not irritate the eyes. According to miotic activity tests in rabbits, the activity is prolonged by PAS-F as well as Carbopol 940 preparations. Differences between the compared preparations are not obtained. In human studies, the 1 action is prolonged and the intensity is increased by PAS-F and Carbopol containing preparations compared with aqueous 1 solution (relative bioavailability about 200%; the duration of the intraocular pressure is 4.5 times in the therapeutical relevant level). A polymeric salt of 1 and PAS-F was particular suitable in this study.