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用于肠道给药的基于海藻酸盐的美沙拉嗪片剂的评估。

Evaluation of alginate based mesalazine tablets for intestinal drug delivery.

作者信息

Tuğcu-Demiröz Fatmanur, Acartürk Füsun, Takka Sevgi, Konuş-Boyunağa Oznur

机构信息

Department of Pharmaceutical Technology, Gazi University, Ankara, Turkey.

出版信息

Eur J Pharm Biopharm. 2007 Sep;67(2):491-7. doi: 10.1016/j.ejpb.2007.03.003. Epub 2007 Mar 12.

Abstract

The aim of this study was to develop the alginate based mesalazine tablets for intestinal delivery. Sodium alginate is a biocompatible, natural polymer with pH-sensitive gel-forming ability. Matrix tablets were prepared with two types of sodium alginate of different amounts. The in vitro release characteristics of mesalazine from alginate tablets were compared with those of the commercial product (Salofalk). X-ray imaging was used to monitor the tablets throughout the gastrointestinal system. Although alginate tablets gave a faster release in an acidic medium compared with the commercial product (Salofalk), the cumulative amount of released drug of the optimum formulation was found to be almost the same as that of the commercial product at the end of 4 h. The alginate type and amount in the matrices played an important role in basic media. The release of the optimum formulation containing low viscosity alginate was found to be almost identical to that of the commercial product in acidic and basic media. Tablets were visualized to determine whether they were located in the terminal ileum or cecum for 3-6 h. Mesalazine-alginate matrix tablet formulations can deliver the drug to the small and large intestine. Thus, the alginate matrix system may be a promising system for the treatment of Crohn's disease involving both the ileum and large intestine.

摘要

本研究的目的是开发用于肠道给药的基于海藻酸钠的美沙拉嗪片剂。海藻酸钠是一种具有pH敏感凝胶形成能力的生物相容性天然聚合物。用两种不同用量的海藻酸钠制备了骨架片。将美沙拉嗪从海藻酸盐片剂中的体外释放特性与市售产品(莎尔福)进行了比较。采用X射线成像技术监测片剂在整个胃肠道系统中的情况。尽管与市售产品(莎尔福)相比,海藻酸盐片剂在酸性介质中释放更快,但在4小时结束时,最佳配方的药物累积释放量与市售产品几乎相同。骨架中海藻酸盐的类型和用量在碱性介质中起重要作用。发现在酸性和碱性介质中,含有低粘度海藻酸盐的最佳配方的释放几乎与市售产品相同。观察片剂3至6小时,以确定它们是否位于回肠末端或盲肠。美沙拉嗪-海藻酸盐骨架片制剂可将药物输送至小肠和大肠。因此,海藻酸盐骨架系统可能是治疗累及回肠和大肠的克罗恩病的一种有前景的系统。

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