Inlfuence of high-viscosity vehicles on miotic effect of pilocarpine. 1978

R D Schoenwald, and R L Ward, and L M DeSantis, and R E Roehrs

Gel formulations containing 2% pilocarpine hydrochloride were prepared from ethylene maleic anhydride, carbomer, hydroxyethylcellulose, polyacrylamide, ethylhydroxyethylcellulose, hydroxypropylcellulose, and poly(methylvinyl ether--maleic anhydride). The viscosity characteristics of each formulation were evaluated from rheograms developed at 37 degrees using a cone and plate viscometer. Single-point viscosities were determined at room temperature using a single-point rotational viscometer. Plastic viscosity parameters correlated to miosis durations in the rabbit following ophthalmic dosing of 50 microliters. Carbomer formulations varying in concentration between 0.9 and 5.0% (w/w) showed a discontinuous relationship when either yield value or plastic viscosity was plotted against miosis durations. At carbomer concentrations above 3%, miosis durations increased 1.5-fold. Above and below this range, plastic parameters did not correlate to miosis duration. It was reasoned that the increased duration was a consequence of the gel's increased yield value such that appreciable in vivo thinning of the gel does not take place with eyelid and/or eyeball movements. As a result, the residence time of the drug in the eye would be expected to increase, thus promoting an increased duration.

UI MeSH Term Description Entries
D008297 Male Males
D010862 Pilocarpine A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. Isopilocarpine,Isoptocarpine,Ocusert,Pilocarpine Hydrochloride,Pilocarpine Mononitrate, (3S-cis)-Isomer,Pilocarpine Nitrate,Pilocarpine, Monohydrochloride, (3S-cis)-Isomer,Salagen,Hydrochloride, Pilocarpine,Nitrate, Pilocarpine
D011108 Polymers Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS). Polymer
D011680 Pupil The aperture in the iris through which light passes. Pupils
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D005260 Female Females
D005782 Gels Colloids with a solid continuous phase and liquid as the dispersed phase; gels may be unstable when, due to temperature or other cause, the solid phase liquefies; the resulting colloid is called a sol.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor
D014677 Pharmaceutical Vehicles A carrier or inert medium used as a solvent (or diluent) in which the medicinally active agent is formulated and or administered. (Dictionary of Pharmacy, 1986) Pharmaceutical Vehicle,Vehicle, Pharmaceutical,Vehicles, Pharmaceutical

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