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开发用于炎症性肠病的氟比洛芬结肠定位微球。

Development of colon specific microspheres of flurbiprofen for inflammatory bowel disease.

机构信息

Department of Pharmaceutics, School of Pharmaceutical Sciences, Shoolini University, Bajhol, Solan (H.P.), India..

出版信息

Curr Drug Deliv. 2013 Oct;10(5):564-71. doi: 10.2174/1567201811310050008.

Abstract

In the present investigation chitosan microspheres loaded with flurbiprofen (FLB) were prepared by oil/oil emulsification method for colon specific drug delivery. FLB was entrapped in chitosan microspheres, following coating with Eudragit S-100 utilizing the benefits of pH dependent solubility of Eudragit S-100, so as to prevent the premature release of FLB in upper GIT. Different batches of FLB microspheres were prepared by varying FLB: chitosan ratio (1:1 to 1:4). The effect of chitosan concentration on size, entrapment efficiency, percent drug loading and degree of swelling was evaluated. DSC studies revealed the dispersion of FLB in the matrix of chitosan microspheres. SEM analysis indicated the nearly smooth surface and spherical shape of the prepared microspheres. X-ray diffract gram of FLB microspheres showed less intense peaks as compared to free FLB. In vitro release studies of uncoated FLB- chitosan microspheres showed burst release in initial 4 h, while Eudragit S-100 coated microspheres prevented the premature release of FLB and showed controlled release for 12 h following Higuchi model, thus suitable for colon specific drug delivery.

摘要

在本研究中,通过油/油乳化法制备了载有氟比洛芬(FLB)的壳聚糖微球,用于结肠定位药物传递。FLB 被包封在壳聚糖微球中,然后用 Eudragit S-100 进行涂层,利用 Eudragit S-100 的 pH 依赖性溶解度的优势,以防止 FLB 在上胃肠道中的过早释放。通过改变 FLB:壳聚糖比(1:1 至 1:4)来制备不同批次的 FLB 微球。评估了壳聚糖浓度对粒径、包封效率、载药量和溶胀度的影响。DSC 研究表明 FLB 分散在壳聚糖微球的基质中。SEM 分析表明,所制备的微球具有几乎光滑的表面和球形形状。FLB 微球的 X 射线衍射图谱显示,与游离 FLB 相比,其峰强度较小。未涂层的 FLB-壳聚糖微球的体外释放研究表明,在最初的 4 小时内会出现突释,而 Eudragit S-100 涂层的微球可以防止 FLB 的过早释放,并按照 Higuchi 模型在 12 小时内呈现控制释放,因此适用于结肠定位药物传递。

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