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用于治疗炎症性肠病的新型口服给药系统。

New oral delivery systems for treatment of inflammatory bowel disease.

作者信息

Friend David R

机构信息

MicroDose Technologies, Inc., Monmouth Junction, NJ 08852, USA.

出版信息

Adv Drug Deliv Rev. 2005 Jan 6;57(2):247-65. doi: 10.1016/j.addr.2004.08.011.

Abstract

Inflammatory bowel disease (IBD) is often localized to specific sites in the gastrointestinal tract (GIT). As a result, this disease can be treated with oral site-specific (targeted) drug delivery systems. Targeted delivery systems for treatment of IBD are designed to increase local tissue concentrations of antiinflammatory drugs from lower doses compared with systemic administration. This review addresses the impact disease has or may have on oral targeted delivery for treatment of IBD as well as a number of delivery approaches currently used in marketed products or under investigation. Delivery systems reviewed rely on temporal control, changes in pH along the GIT, the action of local enzymes to trigger drug release, and changes in intraluminal pressure. Dissolution of enteric polymer coatings due to a change in local pH and reduction of azo-bonds to release an active agent are both used in commercially marketed products. Newer approaches showing promise in treating IBD are based on polysaccharides. These materials are most effective when used as compression coatings around core tablets, which contain the active agent. More complex polymeric prodrugs systems are also under investigation. If the dose of the drug is sufficiently low, this approach may also prove useful in improving treatment of IBD.

摘要

炎症性肠病(IBD)通常局限于胃肠道(GIT)的特定部位。因此,这种疾病可以通过口服部位特异性(靶向)给药系统进行治疗。用于治疗IBD的靶向给药系统旨在与全身给药相比,以更低剂量提高抗炎药物在局部组织中的浓度。本综述阐述了该疾病对IBD口服靶向治疗已经产生或可能产生的影响,以及目前市售产品或正在研究中的多种给药方法。所综述的给药系统依赖于时间控制、胃肠道pH值的变化、局部酶触发药物释放的作用以及腔内压力的变化。由于局部pH值变化导致肠溶聚合物包衣溶解以及偶氮键还原以释放活性剂,这两种方法都用于商业销售产品中。在治疗IBD方面显示出前景的较新方法基于多糖。这些材料用作含有活性剂的核心片剂周围的压制包衣时最为有效。更复杂的聚合物前药系统也在研究中。如果药物剂量足够低,这种方法也可能被证明有助于改善IBD的治疗。

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