| Antibiotics therapy is a kind of very important prevention and treatment to endophthalmitis, a indispensable part of which is topical antibiotic eyedrop therapy. At present, the major topical treatment to eye infection in our country is quinolone eyedrop represented by ofloxacin and ciprofloxacin, and aminoglycoside eyedrop represented by tobramycin. Tobramycin has some activity against several staphylococci and many Gram negative bacteria and is invalid to staphylococcus aureus, staphylococcus epidermis, some Gram negative bacteria and most anaerobes. Ofloxacin, ciprofloxacin and other quinolones have a broad-spectrum activity against various Gram positive and negative bateria, which can stop the effect of DNA racemase to inhibit the synthesis of DNA. Compared with other drugs, quinolone has the minimum toxicity to corneal epithelium and nearly no toxicity to corneal endothelium and retina under therapy dose, and has a excellent aqueous humor penetration, so it is a suitable prevention and treatment drug to intraocular infection.By now, the human eye pharmcokinetics reseachs of topically applied quinolones were samples from single point and lack a continuous observation. There was hardly a report about this. Therefore, the main purpose of this reseach is to investigate the most commomly used three antibiotic eyedrops, ofloxacin, ciprofloxacin and tobramycin, detecting the aqueous drug concentration and comparing the bioavailablity, in order to provide topical therapy proofs of prevention and treatment on bacterial endophthalmitis.Method1, 125 senile cataract patients ( one eye very one patient) undertaking phacoemulsificationwere enrolled. The citerion is that no other eye diseases, no diabetes mellitus, no allergichistory to antibiotics and no oral or topical antibiotic therapy at the same time.2,eyedrops0.3% ofloxacin, 0.3% ciprofloxacin, 0.3% tobramycin.3, groupingThere were 3 groups, including ofloxacin group consist of 21 female and 21 male with average age of 71.6±9.8, ciprofloxacin group consist of 21 female and 20 male with average age of 72.9±9.0 and tobramycin group consist of 21 female and 21 male with average age of 70.5 ±11.2. The average age of three group were analyzed by q test (P>0.05) and there was no significant difference between each two groups. Every group was randomly divided into 5 sub-group. Every sub-group was consist of 8 or 9 patients. Aqueous samples were obtained at different time after the last drop.4, samplingPatients were topical applied ofloxacin, ciprofloxacin or tobramycin according their group. Eyedrops were instilled for six times at a frequency of one drop every 15 minutes. Aqueous samples were obtained during surgery 7.5, 15, 30, 60 and 120min after the last drop according sub-group. 0.1 ml aqueous humor was aspirated from anterior chamber and preserved at -20 ℃. 5,Drug detectingHPLC (high pressure liquid chromatography) was applied to detect the drug concentration. The minimal detecting limit of ofloxacin and ciprofloxacin in aqueous humor is 0.01 μg/ml and tobramycin is 0.05 μg/ml.6, statistical methodTo calculate the mean concentration of drugs at different time and then Rank sum test was used to compare them by using SPSS 1.0 software package.7, Double blind procedure was applied during the reseach. Drug administration, surgery, drug concentration detecting and statistic analysis were carried out by different person.ResultAt 7.5, 15, 30, 60 and 120 minutes after the last drop, the aqueous concentration of ofloxacinwas 2.32±1.33, 2.5911.34, 3.23±1.60, 2.94±1.41, 1.73±0.64 μ g /ml, and reached the peak of3.23±1.60 u g/ml at 30 minutes. At the same 5 time, the aqueous concentration ofciprofloxacin was 0.27±0.16, 0.51±0.19, 0.37±0.24, 0.45±0.26, 0.44±0.25 μ g /ml, and reachedthe peak of 0.51±0.19 μg/ml at 15 minutes. At every same time, the average concentration ofofloxacin was obviously higher than ciprofloxacin. There was significant difference betweenthe concentration... |
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