[Antiglaucoma ophthalmic agents with prolonged action based on macromolecular excipients. 1. In vitro studies].

Hydrogels and Hydrosols based on sodium carboxymethyl-cellulose (NaCMC), polyvinylpyrrolidone (PVP) and polyacrylic acids (PAS) Carbopol 940, Scopacryl D 339 (PAS-B) and PAS-Fluka (PAS-F) were investigated in vitro for rheological properties and pilocarpine release. The gels showed diffusion coefficients in the series Carbopol 940 1% greater than NaCMC 3% greater than PAS-F 3.5% greater than PVP K 90 23% greater than PAS-B 8% greater than PAS-F 7%. Especially PAS-F proved suitable for prolonged release, also in liquid preparations. Lyophilizated pilocarpine polymer-salts which were prepared from PAS-F and pilocarpine base, both in effect of retardation and in drug stability showed important advantages compared with aqueous solution of pilocarpine.