Kim N S, Kawata M, Uchida T, Goto S
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
J Pharm Sci. 1992 Jun;81(6):537-40. doi: 10.1002/jps.2600810613.
A novel method was established for the preparation of Eudragit S, Eudragit L, and Eudispert high-viscosity (hv) hydrogel and xerogel preparations containing a medicinal component such as pentoxifylline (an agent that improves cerebral microcirculation). A significant correlation was found between the in vitro mean dissolution time and the in vivo mean residence time of pentoxifylline after rectal administration of these preparations in rabbits. Staying properties of the hydrogel and xerogel preparations in the lower part of the rectum were compared with those of polyethylene glycol 2000 and Witepsol S-55 suppositories in rats, with water-insoluble dye. Eudispert hv hydrogel and xerogel preparations have excellent staying properties in the rectum. The efficacy of Eudispert hv xerogel preparations may be reduced by first passage through the liver after oral administration.
建立了一种制备含有己基丙烯酸甲酯共聚物（Eudragit S）、甲基丙烯酸甲酯-丙烯酸乙酯共聚物（Eudragit L）和高粘度（hv）的尤迪斯珀特（Eudispert）水凝胶和干凝胶制剂的新方法，这些制剂含有诸如己酮可可碱（一种改善脑微循环的药物）等药用成分。在兔直肠给药这些制剂后，己酮可可碱的体外平均溶出时间与体内平均驻留时间之间发现了显著相关性。使用水不溶性染料，在大鼠中将水凝胶和干凝胶制剂在直肠下部的滞留特性与聚乙二醇2000和维特泊索尔S - 55栓剂的滞留特性进行了比较。尤迪斯珀特hv水凝胶和干凝胶制剂在直肠中具有优异的滞留特性。尤迪斯珀特hv干凝胶制剂口服给药后可能会因首先经过肝脏而降低疗效。
