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两种配制成高粘度凝胶的类固醇与对照水性制剂在兔体内的生物利用度比较。

A bioavailability comparison in rabbits of two steroids formulated as high-viscosity gels and reference aqueous preparations.

作者信息

Schoenwald R D, Boltralik J J

出版信息

Invest Ophthalmol Vis Sci. 1979 Jan;18(1):61-6.

PMID:759386
Abstract

In order to assess the bioavailability of steroids from a high-viscosity gel, rabbit cornea and aqueous humor levels were measured over 12 hr following topical instillation of a gel and reference preparation. Concentrations associated with a 1% tritiated prednisolone acetate gel were found to be approximately four times larger than those of the reference preparation. A graphical comparison of the 1% tritiated prednisolone sodium phosphate data showed the area under corneal and aqueous time curves to be five and 10 times greater, respectively, with the gel than data associated with the reference preparation. The gel vehicle is well retained in the rabbit eye and is responsible for the large increases in bioavailability.

摘要

为了评估高粘度凝胶中类固醇的生物利用度,在局部滴注凝胶和参比制剂后12小时内,测量了兔角膜和房水中的药物水平。发现与1%氚标记醋酸泼尼松龙凝胶相关的浓度约为参比制剂的四倍。1%氚标记泼尼松龙磷酸钠数据的图形比较显示,凝胶组角膜和房水时间曲线下面积分别比参比制剂组大五倍和十倍。凝胶载体在兔眼中保留良好,这是生物利用度大幅提高的原因。

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