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NDA019921/S-021
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OCUFLOX
(ofloxacinophthalmicsolution)0.3%
sterile
DESCRIPTION
OCUFLOX?(ofloxacinophthalmicsolution)0.3%isasterileophthalmicsolution.Itisafluorinated
carboxyquinoloneanti-infectivefortopicalophthalmicuse.
ChemicalName:
(±)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-
carboxylicacid.
Contains:Active:ofloxacin0.3%(3mg/mL).Preservative:benzalkoniumchloride(0.005%).
Inactives:sodiumchlorideandpurifiedwater.Mayalsocontainhydrochloricacidand/orsodiumhydroxideto
adjustpH.
OCUFLOX?solutionisunbufferedandformulatedwithapHof6.4(range-6.0to6.8).Ithasanosmolalityof
300mOsm/kg.Ofloxacinisafluorinated4-quinolonewhichdiffersfromotherfluorinated4-quinolonesinthat
thereisasixmember(pyridobenzoxazine)ringfrompositions1to8ofthebasicringstructure.
CLINICALPHARMACOLOGY
Pharmacokinetics
Serum,urineandtearconcentrationsofofloxacinweremeasuredin30healthywomenatvarioustimepoints
duringaten-daycourseoftreatmentwithOCUFLOX?solution.Themeanserumofloxacinconcentration
rangedfrom0.4ng/mLto1.9ng/mL.Maximumofloxacinconcentrationincreasedfrom1.1ng/mLondayone
to1.9ng/mLonday11afterQIDdosingfor101/2days.Maximumserumofloxacinconcentrationsafterten
daysoftopicalophthalmicdosingweremorethan1000timeslowerthanthosereportedafterstandardoral
dosesofofloxacin.
Tearofloxacinconcentrationsrangedfrom5.7to31mcg/gduringthe40minuteperiodfollowingthelastdose
onday11.Meantearconcentrationmeasuredfourhours