Ocular distribution of lomefloxacin 0.3% after a single instillation in the infected eye of pigmented rabbits

被引:5
作者
Elena, PP [1 ]
Jauch, A [1 ]
机构
[1] Iris Pharma, Preclin Studies Ophthalmol, F-06610 La Gaude, France
关键词
D O I
10.1089/jop.1997.13.551
中图分类号
R77 [眼科学];
学科分类号
100212 ;
摘要
We investigated the distribution of lomefloxacin, a fluoroquinolone, in the infected eye of pigmented rabbits after one instillation of 50 mu l lomefloxacin 0.3 % eye drop, and compared tissue concentrations with therapeutic levels. Infection was induced by 6 instillations of Pseudomonas aeruginosa inoculum (6 x 10(5) bacteria) on centrally scratched cornea of 32 pigmented rabbits. Fifty microliters of (14)[C] lomefloxacin 0.3 % were instilled 24 hours after infection and animals were sacrificed 0.25, 0.5, 1, 2, 4, 8 and 12 hours later. Ocular structures, tear fluid, whole blood and plasma were then sampled, and tissue levels over time, Tmax, Cmax and area under the curve (AUC) were calculated. Lomefloxacin rapidly penetrated into the ocular structures: tear (Tmax 0.25 hours, Cmax 366 mu g/ml, AUC 360 mu g/ml x hour), corresponding values were for: eye lids (0.25, 7, 33), conjunctiva (0.25, 11, 7), cornea (0.25, 56, 70), aqueous humor (1, 8, 14), iris ciliary-body (4, 34, 252), lens (1, 0.2, 0.6). Tear levels remained high for many hours and were 34, 48, 1 and 27 mu g/ml at 1, 2, 4 and 8 hours following a single instillation. Elimination from ocular structures was rapid. Therapeutic levels were achieved after a single instillation (mainly in the external ocular structures) when compared with MIC 90 % values (1-10 mu g/ml).
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页码:551 / 558
页数:8
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