Absorption of topical moxifloxacin ophthalmic solution into human aqueous humor.
OBJECTIVE
To investigate the absorption of moxifloxacin into human aqueous humor after administration of moxifloxacin hydrochloride ophthalmic solution, 0.5% as base.


METHODS
Cataract patients were randomly allocated to receive 1 drop every 15 minutes for 4 doses before surgery (group 1) or 1 drop 4 times per day on the day before surgery plus the same preoperative regimen as group 1 (group 2). The last dose was administered 0.25, 0.50, 1, 2, or 3 hours before aqueous humor sampling. Samples from 30 patients per group were analyzed by a validated HPLC/MS/MS method.


RESULTS
For group 1, the mean +/- SD C(max) was 1.50 +/- 0.75 microg/mL and occurred at 0.5 hour after dosing. The mean C(max) for group 2 was 1.74 +/- 0.66 microg/mL and was reached at 1 to 2 hours. Mean AUC(0-3h) for groups 1 and 2 were 3.16 +/- 0.29 and 4.41 +/- 0.48 microg.h/mL, respectively. The difference in AUC(0-3h) was statistically significant (P = 0.04), but the difference in Cmax was not.


CONCLUSIONS
Topical moxifloxacin was well absorbed. Maximum moxifloxacin concentrations were approximately 30 times higher than the median MICs for common pathogens in bacterial endophthalmitis, indicating that either regimen may provide sufficient concentrations to prevent postoperative endophthalmitis.
Katz
Harold R
HR
Wilmer Eye Institute and the Krieger Eye Institute, Baltimore, MD 21215, USA. hall1999@aol.com
Masket
Samuel
S
Lane
Stephen S
SS
Sall
Kenneth
K
Orr
Susan C
SC
Faulkner
Robert D
RD
McCue
Bette A
BA
Dahlin
David C
DC
D000042:Absorption; D000368:Aged; D000369:Aged, 80 and over; D019072:Antibiotic Prophylaxis; D001082:Aqueous Humor / Q000378:metabolism*; D001372:Aza Compounds / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002387:Cataract Extraction / Q000009:adverse effects; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D009877:Endophthalmitis / Q000209:etiology / Q000378:metabolism / Q000517:prevention & control*; D005260:Female; D024841:Fluoroquinolones; D005500:Follow-Up Studies; D006801:Humans; D008297:Male; D008875:Middle Aged; D000077266:Moxifloxacin; D009883:Ophthalmic Solutions / Q000008:administration & dosage / Q000493:pharmacokinetics; D011300:Preoperative Care; D011804:Quinolines / Q000008:administration & dosage / Q000493:pharmacokinetics*
D001372:Aza Compounds; D024841:Fluoroquinolones; D009883:Ophthalmic Solutions; D011804:Quinolines; D000077266:Moxifloxacin