Objective To compare the pharmacokinetics of
pilocarpine micron emulsion with generic pilocarpine solution in the
aqueous humor Methods 60 albino rabbits were used and were divided into 20 groups, each consisting of 3 animals 10 groups received 2% generic pilocarpine 50 μl as controls; 10 groups received 50 μl of 2% pilocarpine micron emulsion in the conjunctival sac The aqueous humor was withdrawn at 5, 10, 30, 40, 60, 90, 120, 180, 240 and 360 min after instillation The drug was extracted from aqueous humor with dichloromethane The drug was analyzed by reversed phase
high pressure liquid chromatography(HPLC) Results Pilocarpine micron emulsion therapy gave higher aqueous humor concentration of the drug than
drops at all time periods tested except 5 min time point ( P =0 0003～0 042) The area under curve of micron emulsion was 3 times as much as that of drops There was a two fold increase in
ocular bioavailability of pilocarpine due to the therapy with micron emulsion Measurable amounts of drug following 2% micron emulsion were still observed at 360 min while drug levels at 180 min following 2% drop therapy were nil Conclusion Our study results demonstrated significantly increase in ocular bioavailability of pilocarpine due to the therapy with micron emulsion Our finding indicates that a novel topical preparation of pilocarpine incorporated in micron emulsion might serve as a long acting antiglaucoma agent, and less frequent applications are necessary with it than with conventional drops
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