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多次给药可提高局部应用氟比洛芬的眼部生物利用度。

Multiple dosing increases the ocular bioavailability of topically administered flurbiprofen.

作者信息

Anderson J A, Chen C C

机构信息

Department of Ophthalmology, University of California, Irvine.

出版信息

Arch Ophthalmol. 1988 Aug;106(8):1107-9. doi: 10.1001/archopht.1988.01060140263038.

Abstract

The ocular bioavailability of radiolabeled flurbiprofen was determined after single or multiple topical dosing of rabbits. Three doses at half-hour intervals of a 0.03% solution produced higher concentrations in the tissues than those after a single dose of either the 0.03% or the 0.1% solution. Three doses of 0.03% flurbiprofen gave intraocular concentrations in the range that inhibits cyclo-oxygenase activity. Administration of more than three doses did not significantly increase the concentration of flurbiprofen in most tissues. The drug distribution pattern in the ocular tissues after multiple dosing was the same as after single dosing. Although multiple dosing with the 0.03% concentration resulted in higher tissue levels of flurbiprofen, increasing the concentration to 0.1% did not result in greater ocular bioavailability of the drug.

摘要

在对兔子进行单次或多次局部给药后,测定了放射性标记氟比洛芬的眼内生物利用度。以0.03%溶液每隔半小时给药三次,其在组织中的浓度高于单次给予0.03%或0.1%溶液后的浓度。三次给予0.03%氟比洛芬产生的眼内浓度处于抑制环氧化酶活性的范围内。给予超过三次剂量后,大多数组织中氟比洛芬的浓度并未显著增加。多次给药后眼组织中的药物分布模式与单次给药后相同。虽然以0.03%浓度多次给药会使氟比洛芬在组织中的水平更高,但将浓度提高到0.1%并不会使该药物的眼内生物利用度更高。

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