Articulation and Evaluation of Extended-Release Beads using a Sulfasalazine Drug

K. Krishna, V. Patro
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Abstract

The present study was focused on optimization of the formulation for the extended-release capsule of mesalamine. Multi particulate system has long been employed to improve the bioavailability of drugs. Mesalamine pellets were prepared by Coating drug solution on sugar sphere followed by functional coating. The release pattern depends upon the pore formation on the outer surface of the unit particle or beads and then slowly and steadily releasing drugs from the inner core. Ethocel grade 7cps was used as a release controlling polymer with the aid of hydrophilic polymer HPMC E5 with pore former to work as a controlled drug delivery system. The functional coated Pellets were used for various parameters like assay and in-vitro dissolution profile. The study confirmed that mesalamine can deliver its effect into lower part of intestine. The finally prepared pellets were used for the treatment of IBD (Ulcerative colitis) Batch 2 had gave optimised result which follow the US specification. Kinetics was applied to the optimized Batch B-2 which was following Higuchi matrix and the mechanism of release was diffusion as the polymer used was HPMC E5 and Tri ethyl citrate –pore former and Ethocel- impenetrable barrier.
柳氮磺胺嘧啶类药物缓释微珠的制备与评价
本研究主要对美沙拉明缓释胶囊的处方进行优化。多颗粒系统长期以来被用于提高药物的生物利用度。采用糖球包覆药液,再包覆功能包覆法制备美沙拉胺微丸。释放模式取决于单位颗粒或小珠的外表面孔隙的形成,然后缓慢而稳定地从内核释放药物。以乙塞酯级7cps为控释聚合物,与具有孔前形成的亲水性聚合物HPMC E5共同作为控释给药体系。对功能包被微丸进行了测定和体外溶出度等参数分析。研究证实,美沙拉胺可以将其作用传递到肠道下部。最后制备的微丸用于治疗IBD(溃疡性结肠炎),第2批给出了符合美国规范的优化结果。优化后的B-2批为Higuchi基质,采用HPMC - E5和柠檬酸三乙酯-孔洞形成剂和乙塞酯-不可穿透屏障,以扩散为释放机制。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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