Szejtli J
CYCLOLAB Cyclodextrin Research and Development Laboratory Ltd., Budapest, Hungary.
Med Res Rev. 1994 May;14(3):353-86. doi: 10.1002/med.2610140304.
Some cyclodextrins are produced industrially, and available in pharmaceutical quality, at reasonable prices. Their medicinal use means mainly--but not exclusively--the complexation of problematic drugs (poorly soluble, unstable, irritating, difficult to formulate substances). The CD complexation generally results in improved wettability, dissolution, and solubility; improved stability; reduced side effects; or in mildering of other undesired properties (e.g., bitter tastes, bad smells). CDs can be used advantageously practically in any drug forms: oral, rectal, pulmonary, external, ocular, etc. formulations. In oral solid and liquid formulations the chemical and physical stability and bioavailability, but particularly the role of absorption is improved. With appropriate highly soluble chemically modified CDs aqueous parenteral formulations can be prepared from poorly soluble drugs. Using CDs the transdermal penetration or nasal absorption of such drugs becomes possible, which earlier could not be administered through these ways. The direct therapeutic effects of CDs (or their derivatives) are demonstrated in several examples as well as the use of beta CD as vehicle in tabletting.
一些环糊精是工业生产的,以合理的价格提供药用级产品。它们的药用主要是——但不限于——对有问题的药物(难溶性、不稳定、刺激性、难以制剂的物质)进行络合。环糊精络合通常会改善润湿性、溶出度和溶解度;提高稳定性;减少副作用;或减轻其他不良性质(如苦味、难闻气味)。环糊精几乎可实际应用于任何药物剂型:口服、直肠、肺部、外用、眼部等制剂。在口服固体和液体制剂中,可提高化学和物理稳定性以及生物利用度,尤其是吸收方面的作用。使用适当的高溶性化学修饰环糊精,可以由难溶性药物制备水性注射剂。使用环糊精可使此类药物实现经皮渗透或鼻内吸收,而这些药物以前无法通过这些途径给药。环糊精(或其衍生物)的直接治疗作用在几个例子中得到了证明,以及β-环糊精在压片中作为载体的应用。