Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an inner layer and an outer layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralized polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.
药物在结肠中的延迟释放是通过延迟释放制剂实现的,该制剂包括一个核心和一个核心涂层。药芯由药物组成,包衣由内层和外层组成。外层包括易受结肠细菌攻击的第一种聚合物材料和 pH 值约为 5 或以上的第二种聚合物材料的混合物。内层包括可溶于肠液或胃肠液的第三种聚合材料,所述第三种聚合材料选自至少部分中和的聚
羧酸和非离子聚合物。在第三种聚合材料为非离子聚合物的实施方案中,内层包括缓冲剂和碱中的至少一种。根据本发明配制的制剂的优点包括:当药物暴露于结肠条件下时,可加速药物的释放,减少或消除给药后食物和/或
酒精对药物释放的影响。