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Tailoring of Colon Targeting with Sodium Alginate‐Assam Bora Rice Starch Based Multi Particulate System Containing Naproxen
Starch ( IF 2.3 ) Pub Date : 2020-05-10 , DOI: 10.1002/star.201900307
Manoj Kumar Sarangi 1, 2 , M.E. Bhanoji Rao 3, 4 , Versha Parcha 1, 5 , Aadesh Upadhyay 1
Affiliation  

This research is focused on the formulation and optimization of Assam Bora rice starch (ABRS)‐alginate beads containing a non‐steroidal anti‐inflammatory drug (NSAID) such as Naproxen (NA), by an ionotropic gelation technique using 32 factorial design for colon targeting against rheumatoid arthritis, inflammatory bowel disease, and colon cancer. The impact of a polymeric blend of sodium alginate (SA) and ABRS on the drug entrapment efficiency (DEE, %), bead size (BS), and percentage cumulative drug release in the first 6 h (Q6, %) is optimized. The DEE (%) of all the developed beads is found to be in between 45.25% and 85.14% with an in vitro drug release of 32.81–42.18% in first 6 h. The optimized batches of beads are coated with Eudragit S100 (ES100) (5%, 10%, and 15% w/v) to facilitate colon targeting in a prominent way. The average size of the developed beads is found to be within the range of 751.61–822.22 µm. The optimized ABRS‐alginate beads containing NA show significant drug permeability over a prolonged period on ex vivo permeability through a goat colon. The in vivo roentgenographic study on rats shows the colon targeting of the beads without degradation.

中文翻译:

海藻酸钠-阿萨姆博拉稻淀粉基于含萘普生的多颗粒系统的结肠靶向定制

这项研究致力于通过使用3 2的离子胶凝技术,对包含非甾体抗炎药(NSAID)如萘普生(NA)的阿萨姆波拉米淀粉(ABRS)-海藻酸盐微珠进行配方和优化。针对风湿性关节炎,炎症性肠病和结肠癌的结肠靶向设计。优化了藻酸钠(SA)和ABRS的聚合物共混物对药物包封效率(DEE,%),珠粒大小(BS)和前6小时内累积药物释放百分比(Q6,%)的影响。发现所有已开发微珠的DEE(%)在45.25%至85.14%之间,在头6小时内体外药物释放为32.81–42.18%。优化批次的珠子用Eudragit S100(ES100)(5%,10%和15%w / v)包衣,以显着方式促进结肠靶向。发现显影珠的平均大小在751.61–822.22 µm的范围内。经过优化的含有NA的ABRS藻酸盐珠在长时间内对山羊结肠的离体通透性表现出显着的药物通透性。
更新日期:2020-05-10
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