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2011 OMIG Abstract 13

Comparative penetration of four fluoroquinolone eyedrops after topical dosing into rabbit eyes
J.L. Chung1, K.Y. Seo2, S.Y. Song1, B.Y. Kim1, J.H. Lee1, F.S. Mah3
1Kim’s Eye Hospital, Konyang University, Seoul, Kyoungkido, Republic of Korea
2Shinchon Severance Hospital, Yonsei University, Seoul, Kyoungkido, Republic of Korea, 3Charles T. Campbell Ophthalmic Microbiology Laboratory, University of Pittsburgh, Pittsburgh, PA

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 >