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2011 Abstract List | < Previous | Next > 2011 OMIG Abstract 13 Comparative penetration of four fluoroquinolone eyedrops after topical dosing into rabbit eyes Purpose: We compared intraocular penetration of four fluoroquinolones eyedrops after topical dosing into rabbit eyes. Methods: Tested fluoroquinolone ophthalmic solutions were levofloxacin 1.5% (IQUIX®, LVFX), moxifloxacin 0.5% (VIGAMOX®, MFLX), gatifloxacin 0.3% (ZYMAR®, GFLX) and besifloxacin 0.6% (BESIVANCE®, BFLX). Forty-eight Japanese white rabbits were divided into two groups. In group 1 (40 rabbit 80 eyes) single instillation was done and tissue samples were acquired after 0.5, 1, 2, 4 and 6 hours. In group 2 (8 rabbits,16 eyes), repeated instillation (4 times, every 15 minutes) was done and tissues were acquired 1 hour after 4th instillation. The drug concentrations in ocular tissues (cornea, acqueous, conjunctiva, vitreous) were analyzed using HPLC method. Results: The [AUC0-6hr in Group 1 (μg·hr/g)] / {mean concentration in Group 2 (μg/g)} of each drug were cornea [22.97/13.54/6.44/3.29] / {22.60/13.69/6.99/1.91}, aqueous humor [5.66/3.38/1.43/0.42] / {5.52/2.47/1.29/0.19}, bulbar conjunctiva [2.33/2.17/0.91/9.83] / {4.51/1.48/0.78/2.09}, anterior vitreous [0.243/0.134/0.051/0.018] / {0.182/0.122/0.055/0.015}, equatorial vitreous [0.056/0.035/0.013/ND] / {0.043/0.027/0.008/ND} and posterior vitreous [0.037/0.025/0.009/ND] / {0.028/0.016/0.004/ND}. Repeated instillation showed about 2.2 times greater penetration than single instillation. Conclusions: LVFX and MFLX demonstrated good intraocular penetration especially in cornea, aqueous humor and anterior vitreous. BFLX showed high concentration in bulbar conjunctiva. Disclosure: N 2011 Abstract List | < Previous | Next >
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