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[口服左氧氟沙星在兔眼内的渗透情况]

[Intraocular penetration of oral levofloxacin in rabbits].

作者信息

Mochizuki K, Ohkubo S, Torisaki M, Yamashita Y, Tanahashi T, Jin Y, Okamura Y, Tanaka M

机构信息

Department of Ophthalmology, Kanazawa University School of Medicine, Ishikawa-ken, Japan.

出版信息

Nippon Ganka Gakkai Zasshi. 1994 Nov;98(11):1085-90.

PMID:7825501
Abstract

The intraocular penetration of levofloxacin was studied in albino and pigmented rabbits after oral administration of 14C-levofloxacin at a dose of 20 mg/kg. The radioactivity of the eyeball of albino rabbits in the autoradiogram was much higher at 1 hr than at 2 or 6 hr after administration. On the other hand, the distribution of radioactivity in pigmented rabbits was similar at 1, 2, and 6 hr after administration. The radioactivity levels in melanin-containing tissues such as the iris-ciliary body and the choroid-retina were significantly higher in pigmented rabbits than in albino rabbits 2 hr after oral administration. The radioactivity levels in the ocular tissues without melanin except for the cornea were similar in albino and pigmented rabbits. These results indicate that the intraocular pharmacokinetics of levofloxacin are markedly affected by its affinity for melanin.

摘要

以20mg/kg的剂量给白化病兔和有色兔口服14C-左氧氟沙星后,研究了左氧氟沙星的眼内渗透情况。给药后1小时,白化病兔眼球在放射自显影片中的放射性比给药后2小时或6小时高得多。另一方面,有色兔在给药后1小时、2小时和6小时的放射性分布相似。口服给药2小时后,有色兔虹膜睫状体和脉络膜视网膜等含黑色素组织中的放射性水平明显高于白化病兔。除角膜外,白化病兔和有色兔无黑色素的眼组织中的放射性水平相似。这些结果表明,左氧氟沙星的眼内药代动力学受到其对黑色素亲和力的显著影响。

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