A pH-dependent colon-targeted oral drug delivery system using methacrylic acid copolymers.: II.: Manipulation of drug release using Eudragit® L100 and Eudragit S100 combinations
A pH-dependent colon-targeted oral drug delivery system using methacrylic acid copolymers.: II.: Manipulation of drug release using Eudragit® L100 and Eudragit S100 combinations
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DOI：
10.1081/ddc-100101266
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发表时间：
2000-01-01
影响因子：
3.4
通讯作者：
Kurjakovic, N
中科院分区：
文献类型：
--
作者：
Khan, MZI;Stedul, HP;Kurjakovic, N
使用两种甲基丙烯酸共聚物（Eudragit（R）L100和Eudragit S100）的各种组合，通过从水性系统喷雾，对含有美沙拉秦作为模型药物的片剂进行包衣。所研究的Eudragit L100-Eudragit S100（w/w）组合为1：0、4：1、3：2、1：1、2：3、1：4、1：5和0：1。将包衣片剂置于体外，以确定其pH依赖性结肠靶向口服给药的适用性。从所研究的片剂获得的药物的溶出曲线表明，通过在6.0和7.0之间的pH范围内改变组合中的Eudragit L100-Eudragit S100比率可以控制药物的释放，其中各个聚合物可溶于pH范围内，并且由两种聚合物的组合组成的涂层制剂可以克服个体之间的高胃肠道（GI）pH变化性的问题。结果还证明了使用Eudragit L100-Eudragit S100组合的水性分散体用于包衣片剂以结肠靶向递送药物的可行性，并且可以调节制剂以在胃肠道的肠区域的任何其它期望部位递送药物，其中流体的pH在6.0至70的范围内。对于药物的结肠靶向递送，所提出的组合系统上级于单独用Eudragit L100或Eudragit S100包衣的片剂。
Tablets containing mesalazine as a model drug were coated using various combinations of two methacrylic acid copolymers, (Eudragit(R) L100 and Eudragit S100) by spraying from aqueous systems. The Eudragit L100-Eudragit S100 (w/w) combinations studied were 1:0, 4:1, 3:2, 1:1, 2:3, 1:4, 1:5, and 0:1. The coated tablets were rested in vitro for their suitability for pH-dependent colon-targeted oral drug delivery. The dissolution profiles of the drug obtained from the studied tablets demonstrate that the release of the drug could be manipulated by changing the Eudragit L100-Eudragit S100 ratios in the combinations within the pH range between 6.0 and 7.0 in which the individual polymers are soluble, and a coating formulation consisting of a combination of the two polymers can overcome the issue of high gastrointestinal (GI) pH variability among individuals. The results also demonstrate the feasibility of using using aqueous dispersions of Eudragit L100-Eudragit S100 combinations for coating tablets for colon-targeted delivery of drugs, and that the formulation can be adjusted to deliver drug(s) at any other desirable site of the intestinal region of the GI tract in which pH of the fluid is within the range 6.0 to 70. For colon-targeted delivery of drugs, the proposed combination system is superior to tablets coated with either Eudragit L100 or Eudragit S100 alone.