Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Czech Republic.
Drug Dev Ind Pharm. 2011 Sep;37(9):1100-9. doi: 10.3109/03639045.2011.560156. Epub 2011 Mar 21.
In recent years, many achievements have been realized in the therapy of inflammatory bowel disease (IBD) although its etiology remains unknown. Thus IBD treatment is symptomatic and targets general inflammatory mechanisms. Oral formulations containing 5-aminosalicylic acid (5-ASA) have become the standard therapy for mild-to-moderate IBD.
This article is a review of recently published research dealing with new 5-ASA dosage forms. Thus promising candidates for IBD treatment evaluated in vitro are reported; systems tested in vivo in trinitrobenzene sulfonic acid (TNBS)-induced colitis in rats are mentioned; and 5-ASA formulations used in clinical studies are presented. Moreover, all oral dosage forms containing 5-ASA or its prodrugs are reviewed; their characteristics and utilization in IBD treatment are discussed.
In several clinical studies, it has been shown that multiparticulates such as pellets offer more advantages as compared with single unit forms, that is, coated tablets. Prolonged presence close to the site of the action, improved drug bioavailability, and easier administration of large drug doses belong to the benefits of pellets.
近年来,尽管炎症性肠病(IBD)的病因仍不清楚,但在其治疗方面已取得许多成就。因此,IBD 的治疗是对症的,针对的是一般的炎症机制。含有 5-氨基水杨酸(5-ASA)的口服制剂已成为治疗轻中度 IBD 的标准疗法。
本文综述了最近发表的关于新型 5-ASA 剂型的研究。因此,报告了在体外评估的有前途的 IBD 治疗候选药物;提到了在三硝基苯磺酸(TNBS)诱导的大鼠结肠炎中进行体内测试的系统;并介绍了用于临床研究的 5-ASA 制剂。此外,还综述了所有含有 5-ASA 或其前药的口服剂型;讨论了它们的特性及其在 IBD 治疗中的应用。
在几项临床研究中,已经表明与单个单位形式(即包衣片剂)相比,多颗粒剂(如颗粒剂)具有更多优势。延长在作用部位附近的停留时间、提高药物生物利用度以及更方便地施用大剂量药物均属于颗粒剂的优势。