Document Detail

Pilocarpine incorporated into a submicron emulsion vehicle causes an unexpectedly prolonged ocular hypotensive effect in rabbits.
MedLine Citation:
PMID:  7836859     Owner:  NLM     Status:  MEDLINE    
Pilocarpine, a widely used antiglaucoma drug, was incorporated into a newly developed submicron emulsion (pilocarpine emulsion) suitable for local ocular administration. Pilocarpine-Emulsion effect on the intraocular pressure (IOP) was studied following a single dose application in normotensive rabbits. Membrane filtration (steam autoclaving) was found not to affect particle size distribution, zeta potential or pH of the pilocarpine emulsion preparation. A single dose application of pilocarpine emulsion 1.7% (equivalent to 2% pilocarpine hydrochloride) induced a prolonged progressive decrease in IOP in normotensive rabbits, which started at eleven hours post instillation and reached its maximal value of 6.0 +/- 0.2 mmHg at 29 hours. The pressure decreasing effect induced by pilocarpine emulsion treatment followed a pattern different from that generated by generic pilocarpine (Pilocarpine Hydrochloride 2% eye drops); In the latter group, IOP reduction (starting at two hours) persisted during the initial five hours post-instillation, while in the former, the hypotensive effect started at a later stage, and was maintained during a twenty nine hour follow-up causing a greater IOP decrease than in the generic group (% delta IOP of 28.5% and 18%, respectively). In the contralateral eyes of Pilocarpine Emulsion treated rabbits, an ocular hypotensive effect was noted late after application (11 hours through 29 hours post-instillation), while this effect was negligible in rabbits-treated with aqueous pilocarpine. Our findings point to the possibility that the novel preparation of pilocarpine incorporated into submicron emulsion might serve as a long-acting form of pilocarpine which might require a single daily application. Further studies are required to elucidate the mechanism and action of this preparation.
N Naveh; S Muchtar; S Benita
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of ocular pharmacology     Volume:  10     ISSN:  8756-3320     ISO Abbreviation:  J Ocul Pharmacol     Publication Date:  1994  
Date Detail:
Created Date:  1995-02-27     Completed Date:  1995-02-27     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8511297     Medline TA:  J Ocul Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  509-20     Citation Subset:  IM    
Goldschleger Eye Research Institute, Tel-Aviv University, Sheba Medical Center, Tel-Hashomer, Israel.
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MeSH Terms
Administration, Topical
Double-Blind Method
Drug Delivery Systems*
Hydrogen-Ion Concentration
Intraocular Pressure / drug effects
Ocular Hypertension / drug therapy,  physiopathology
Ocular Hypotension / chemically induced*
Ophthalmic Solutions
Pilocarpine / administration & dosage*,  therapeutic use
Random Allocation
Time Factors
Reg. No./Substance:
0/Emulsions; 0/Ophthalmic Solutions; 92-13-7/Pilocarpine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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