[Antiglaucoma ophthalmic agents with prolonged action based on macromolecular excipients. 2. In vivo studies].
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.
Pergande
G
G
Sektion Chemie, Augenklinik der Charité der Humboldt-Universität zu Berlin.
Keipert
S
S
Klatt
A
A
D000180:Acrylic Resins; D000818:Animals; D001682:Biological Availability; D003692:Delayed-Action Preparations; D005079:Excipients; D005260:Female; D005901:Glaucoma / Q000188:drug therapy*; D006168:Guinea Pigs; D006801:Humans; D007429:Intraocular Pressure / Q000187:drug effects; D015877:Miosis; D010862:Pilocarpine / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D011817:Rabbits
D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D005079:Excipients; D010862:Pilocarpine; C006903:carbopol 940
Antiglaukomatosahltige Ophthalmika mit prolongierter Wirkung auf Basis makromolekularer Hilfsstoffe. Teil 2: In vivo-Untersuchungen.