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某些降血脂药物体外光毒性特性的评估:非诺贝特在UVA和UVB区域表现出显著的光毒性潜力。

Evaluation of the phototoxic properties of some hypolipidemics in vitro: fenofibrate exhibits a prominent phototoxic potential in the UVA and UVB region.

作者信息

Diemer S, Eberlein-König B, Przybilla B

机构信息

Dermatologische Klinik und Poliklinik, Ludwig-Maximilians-Universität, München, Germany.

出版信息

J Dermatol Sci. 1996 Nov;13(2):172-7. doi: 10.1016/s0923-1811(96)00552-x.

DOI:10.1016/s0923-1811(96)00552-x
PMID:8953418
Abstract

As some fibric acid derivatives have been reported to exhibit photosensitizing effects in vivo, the antilipemic drugs fenofibrate, bezafibrate, clofibrate, and gemfibrozil were tested for their phototoxic potential in vitro by a photohemolysis test using human erythrocytes and different irradiation sources. In this system only fenofibrate revealed strong phototoxic properties, which were dependent both on the drug concentration and the irradiation doses. Above a surface dose of 40 J/cm2 UVA of an UVA (320-400 nm)-rich irradiation source or 1.6 J/cm2 UVB/0.8 J/cm2 UVA of an UVB (280-320 nm)-rich irradiation source human red blood cells were completely photohemolysed in the presence of fenofibrate. Bezafibrate- and gemfibrozil-induced photohemolysis remained beneath 10%, and clofibrate showed no phototoxicity at all. As the phototoxic potential of fenofibrate lies in the UVB and UVA range, this might be of relevance with regard to clinical photosensitivity.

摘要

由于一些纤维酸衍生物已被报道在体内具有光敏作用,因此通过使用人红细胞和不同辐照源的光溶血试验,对降血脂药物非诺贝特、苯扎贝特、氯贝丁酯和吉非贝齐的体外光毒性潜力进行了测试。在该系统中,只有非诺贝特显示出较强的光毒性,这取决于药物浓度和辐照剂量。在富含UVA(320 - 400nm)的辐照源表面剂量达到40J/cm² UVA或富含UVB(280 - 320nm)的辐照源表面剂量达到1.6J/cm² UVB/0.8J/cm² UVA以上时,在非诺贝特存在的情况下,人红细胞会完全发生光溶血。苯扎贝特和吉非贝齐诱导的光溶血率保持在10%以下,氯贝丁酯则完全没有光毒性。由于非诺贝特的光毒性潜力存在于UVB和UVA范围内,这可能与临床光敏性有关。

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