Experimental Pharmacodynamics Research Of Levofloxaein Hydroehlorid In Situ Forming Eye Gel

ObjectiveTo observe the single-dose and multiple-dose of eye irritation and experimentalpharmacodynamics of levofloxaein hydroehlorid in situ forming eye gel.MethodsSingle-dose eye irritation experiment:chose6new zealand white rabbits as experimentalanimals, left eyes were levofloxaein hydroehlorid in situ forming eye gel group and the righteyes were PBS control group, observe the eye irritation in the1h,6h,12h,24h,48h and72hafter the treatment. Multiple-dose of eye irritation experiment:chose6new zealand whiterabbits as experimental animals, left eyes were levofloxaein hydroehlorid in situ forming eyegel group and the right eyes were PBS control group, rabbits were treated twice a day.observe the eye irritation before every treated and in the24h,48h,72h after the lasttreated.10ul staphylococcus aureu （ATCC25923） suspension contain105CFUstaphylococcus aureus were injected directly within the left eye of50new zealand whiterabbits cornea.Rabbits with bacterial keratitis were randomly divided into four groups:24hbaseline group,PBS control group, levofloxacin hydrochloride eye drops group,levofloxaeinhydroehlorid in situ forming eye gel group.For24h baseline group,slit-lamp examinationsand clinical scores were performed, rabbits were killed and corneas were harvested forbacterial quantitation and histopathology. The remaining three groups were treated accordingto the scheduled treatment,three groups were treated in the same way with24h baselinegroup2h after the last treated.ResultsLevofloxaein hydroehlorid in situ forming eye gel with single-dose,the scores ofconjunctival,corneal and iris were zero. The scores of conjunctival,corneal and iris withmultiple-dose were not more than1minute. Staphylococcus aureus keratitis animal modelswere successfully made in50new zealand white rabbits,48among this the clinical scoreswere between6-10,every eye present photophobia tears, blepharospasm, a small amount ofsecretions,conjunctival edema,congestion, corneal surface formation, limitations of about4mm grey cloudy focal keratitis infiltration stage performance,etc.The rest2rabbits clinicalscores were15,inflammation, photophobia tears,severe symptoms of blepharospasm,a largenumber of secretion cause eyelid adhesions, height of conjunctival edema, congestion, corneal surface to form a6mm white muddy stove and accompanied by1mm anterior chamberempyema.The SLE scores from PBS group, levofloxaein hydroehlorid eye drops and levofloxaeinhydroehlorid in situ forming eye gel was7.831.39,4.211.1and3.630.86respectively,Compared with PBS group,levofloxaein hydroehlorid eye drops and levofloxaeinhydroehlorid in situ forming eye gel P=0.00,has significantly statistical differences. But therewas no significantly statistical differences between levofloxaein hydroehlorid eye drops andlevofloxaein hydroehlorid in situ forming eye gel(P=0.217). The effectiveness of two drugs isalso reflected in the cornea bacterial quantitation, staphylococcus aureus recovered fromcorneas PBS group was5.65±0.09,while levofloxaein hydroehlorid in situ forming eye gelgroup and levofloxaein hydroehlorid eye drops was4.640.10and4.870.05respectively at7D PI,a significantly statistical differences was revealed between levofloxaein hydroehlorid insitu forming eye gel and levofloxaein hydroehlorid eye drops (P=0.00).ConclusionLevofloxaein hydroehlorid in situ forming eye gel had no eye irritation. Treatment ofstaphylococcus aureus keratitis,it can reduce corneal bacterial more significantly comparedwith levofloxacin hydrochloride eye drops and relieve clinical symptoms,it is a kind of safeand effective new eye ophthalmic agent.