Balasubramaniam Jagdish, Kant Shri, Pandit Jayanta Kumar
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221 005, India.
Acta Pharm. 2003 Dec;53(4):251-61.
The poor bioavailability and therapeutic response exhibited by the conventional ophthalmic solutions due to pre-corneal elimination of the drug may be overcome by the use of in situ gel forming systems, which upon instillation as drops into the eye undergo a sol-gel transition in the cul-de-sac. This may result in better ocular availability of the drug. The purpose of this work was to develop an ophthalmic delivery system of the NSAID indomethacin, based on the concept of ion activated in situ gelation. Gelrite gellan gum, a novel ophthalmic vehicle, which gels in the presence of mono or divalent cations present in the lacrimal fluid, was used as the gelling agent. The developed formulations were therapeutically efficacious (in a uveitis induced rabbit eye model) and provided sustained release of the drug over an 8-hour period in vitro.
由于药物在角膜前的消除,传统眼科溶液表现出较差的生物利用度和治疗反应,而使用原位凝胶形成系统可以克服这一问题,该系统以滴剂形式滴入眼内后,会在眼穹窿处发生溶胶-凝胶转变。这可能会使药物在眼内的可用性更好。这项工作的目的是基于离子激活原位凝胶化的概念,开发一种非甾体抗炎药吲哚美辛的眼科给药系统。结冷胶,一种新型眼科载体,在泪液中存在的单价或二价阳离子存在下会发生凝胶化,被用作胶凝剂。所开发的制剂具有治疗效果(在葡萄膜炎诱导的兔眼模型中),并在体外8小时内提供药物的持续释放。