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J Cataract Refract Surg ; 24(10): 1365-70, 1998 Oct.
Article in English | MEDLINE | ID: mdl-9795853

ABSTRACT

PURPOSE: To establish the corneal penetration of diclofenac in the presence of gentamicin in patients having cataract surgery. SETTING: Kantonsspital Augenklinik, Aarau, and Hôpital Jules Gonin, Lausanne, Switzerland. METHODS: Eligible patients having cataract surgery (39 women, 30 men) were treated with 4 drops of diclofenac 0.1%-gentamicin 0.3% (Voltamicin) instilled at 20 minute intervals. Paracentesis was performed 15, 30, or 60 minutes after the last instillation, and a sample of aqueous humor was collected for analysis of diclofenac by high-performance liquid chromatography. Blood samples of some patients were obtained before surgery for analysis. RESULTS: Mean diclofenac levels (+/- SD) in the aqueous humor 15, 30, and 60 minutes after the last instillation were 72 +/- 84, 108 +/- 87, and 201 +/- 116 ng/mL (= 682 nMol/L), respectively. Diclofenac remained below the limit of detection (5 ng/mL) in all samples of blood serum. In general, local tolerance was good; no side effects were reported. Comparison of the data with published results of topically instilled diclofenac 0.1% suggests that the concentration of diclofenac in the aqueous humor achieved with 4 instillations of the combination product is similar to that achieved with 8 instillations of diclofenac 0.1% (Voltaren Ophtha) alone. CONCLUSIONS: Drug levels of diclofenac in the aqueous humor well above IC-50 for cyclo-oxygenase were achieved with the regimen applied. No inhibitory effect by the gentamicin or vehicle was observed. Comparison of these data with published results of Voltaren Ophtha implies a 2-fold better penetration of diclofenac with the diclofenac-gentamicin combination.


Subject(s)
Anti-Bacterial Agents/pharmacokinetics , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Cataract Extraction , Cornea/metabolism , Diclofenac/pharmacokinetics , Gentamicins/pharmacokinetics , Aged , Anti-Bacterial Agents/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Aqueous Humor/metabolism , Chromatography, High Pressure Liquid , Diclofenac/administration & dosage , Drug Therapy, Combination , Female , Gentamicins/administration & dosage , Humans , Male , Ophthalmic Solutions
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