提高眼科配方水不溶性药物的溶解度

Sunisha Kulkarni, S. Gupta, N. Upmanyu, S. D. Tonpay
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引用次数: 11

摘要

近年来,眼科制剂的产品开发受到了相当大的关注。随着对其不育性的日益重视,它们与注射制剂之间的一些差异正变得不那么明显。这两类制剂使用类似的添加物质和制造程序。低水溶性药物的成功配方是制药生产中的主要问题之一。水溶性较差的药物,如吲哚美辛,由于药物在胃肠道液体中溶解较差,口服生物利用度低且不稳定。吲哚美辛是一种不溶于水的药物,所以配制含水滴眼液的问题是众所周知的。此外,吲哚美辛水溶液制剂的不稳定性也是一大挑战。在本研究工作中,考虑到药物吲哚美辛的药理重要性,我们试图通过将其制成盐来克服其水溶性差的问题,从而配制出一种眼用水制剂。关键词:眼科制剂;吲哚美辛盐;滴眼液;
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Solubility Enhancement of Water Insoluble Drug for Ophthalmic Formulation
Product development of ophthalmic preparations has received considerable attention in the last few years. With the increasing emphasis on their sterility, some of the differences between them and parenteral preparations are becoming less evident. Both classes of preparations employ similar added substances and manufacturing procedures. The successful formulation of poorly water-soluble drugs is one of the major problems in pharmaceutical manufacturing. Poorly water-soluble drugs, such as indomethacin, may show low and erratic oral bioavailability due to poor dissolution of the drug in the fluids of the gastrointestinal tract. Indomethacin is a water insoluble drug, so problems of formulating an aqueous eye-drop are well known. Moreover, unstability of Indomethacin aqueous preparations is also a great challenge. In this research work, considering pharmacological importance of drug Indomethacin, we tried to overcome the problem of poor water solubility by making a salt of it and thus formulating an aqueous ophthalmic preparation. Keywords: ophthalmic preparation, indomethacin salt, aqueous eye drops, poor water soluble drugs.
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