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氟比洛芬,S(+),滴眼液:制剂、对映体测定、保质期及药理学

Flurbiprofen, S(+), eyedrops: formulation, enantiomeric assay, shelf-life and pharmacology.

作者信息

van Sorge A A, Wijnen P H, van Delft J L, Coré-Bodelier V M, van Haeringen N J

机构信息

Rijnstate Hospital Dept of Pharmacy, Arnhem, The Netherlands.

出版信息

Pharm World Sci. 1999 Apr;21(2):91-5. doi: 10.1023/a:1008609513880.

Abstract

Aphakic cystoid macula edema, occurring after cataract extraction is ascribed to trauma-induced production of intra-ocular prostaglandins. Sufficient experimental and clinical evidence supports the use of prostaglandin synthesis inhibitors to countervail this clinical condition. The active S(+)-enantiomer of flurbiprofen, a prostaglandin synthesis inhibitor, has been formulated into a stereoselective, ballast free eyedrop solution in a concentration of 0.015%. Analysis by capillary zone electrophoresis shows shelf-life stability up to four years at room temperature of this enantiomer. The inhibitory effect on the synthesis of prostaglandins as measured on a homogenate bovine iris/ciliary body, remained unaffected during a shelf-life period of three years.

摘要

无晶状体性黄斑囊样水肿发生于白内障摘除术后,被认为是由创伤诱导眼内前列腺素生成所致。充分的实验和临床证据支持使用前列腺素合成抑制剂来对抗这种临床病症。氟比洛芬的活性S(+)对映体作为一种前列腺素合成抑制剂,已被配制成浓度为0.015%的无载体立体选择性滴眼液。毛细管区带电泳分析表明,该对映体在室温下保质期长达四年。在三年的保质期内,对牛虹膜/睫状体匀浆测定的前列腺素合成抑制作用未受影响。

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