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预滴注散瞳剂对局部用0.1%普拉洛芬眼内浓度及抗炎作用的影响(2)——多次给药研究

[Effects of pre-instilled mydriatics on the intraocular concentration and anti-inflammatory action of topical 0.1% pranoprofen (2)--Study on multiple dosing].

作者信息

Ogawa T, Ohara K, Shimizu H

机构信息

Department of Ophthalmology, Jichi Medical School, Tochigi, Japan.

出版信息

Nippon Ganka Gakkai Zasshi. 1992 Sep;96(9):1079-84.

PMID:1414697
Abstract

We studied the effects of multiple dosing and pre-instilled mydriatics (0.5% tropicamide and 0.5% phenylephrine) on the intraocular concentration and anti-inflammatory action of topical 0.1% pranoprofen (PPF) in rabbit eyes. PPF was applied in a single or multiple doses: 1 to 4 times consecutively at 5-minute intervals with or without pre-instilled mydriatics. PPF concentrations in the aqueous humor increased dose-dependently. The PPF concentrations also increased dose-dependently, and reached the maximal concentration by instillation 3 times in the presence of pre-instilled mydriatics, and the concentrations were 3.4 to 5.8 times higher than those without mydriatics. The PPF concentrations in the cornea, secondary aqueous, and iris-ciliary body increased in a dose-dependent manner, and the concentrations were higher in the presence of mydriatics. PPF reduced the protein rise in the secondary aqueous and miotic responses which were seen after paracentesis. The percent inhibitions ranged from 75 to 83, but the inhibitory actions were not enhanced by increases of intraocular PPF concentrations. These data indicate that the potent anti-inflammatory actions of PPF were obtainable by a single instillation, but it might be useful to instill the drug 3 times consecutively to ensure higher intraocular drug concentrations in combination with pre-instilled mydriatics.

摘要

我们研究了多次给药以及预先滴入散瞳剂(0.5%托吡卡胺和0.5%去氧肾上腺素)对0.1%普拉洛芬(PPF)滴眼液在兔眼内浓度及抗炎作用的影响。PPF采用单次或多次给药:在滴入或未滴入散瞳剂的情况下,每隔5分钟连续给药1至4次。房水中PPF浓度呈剂量依赖性增加。在预先滴入散瞳剂的情况下,PPF浓度也呈剂量依赖性增加,滴入3次时达到最大浓度,且该浓度比未使用散瞳剂时高3.4至5.8倍。角膜、房水及虹膜睫状体中的PPF浓度呈剂量依赖性增加,且在使用散瞳剂时浓度更高。PPF可降低穿刺后房水中蛋白质增加及瞳孔缩小反应。抑制率在75%至83%之间,但眼内PPF浓度升高并未增强其抑制作用。这些数据表明,单次滴入PPF即可获得有效的抗炎作用,但连续滴入3次该药物,结合预先滴入散瞳剂,可能有助于确保更高的眼内药物浓度。

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