Prudhviraj G, Vaidya Yogyata, Singh Sachin Kumar, Yadav Ankit Kumar, Kaur Puneet, Gulati Monica, Gowthamarajan K
School of Pharmaceutical Sciences, Lovely Professional University, Punjab 144 401, India.
School of Pharmaceutical Sciences, Lovely Professional University, Punjab 144 401, India.
Eur J Pharm Biopharm. 2015 Nov;97(Pt A):164-72. doi: 10.1016/j.ejpb.2015.09.012. Epub 2015 Sep 28.
Significant clinical success of colon targeted dosage forms has been limited by their inappropriate release profile at the target site. Their failure to release the drug completely in the colon may be attributed to changes in the colonic milieu because of pathological state, drug effect and psychological stress accompanying the diseased state or, a combination of these. Alteration in normal colonic pH and bacterial picture leads to incomplete release of drug from the designed delivery system. We report the effectiveness of a targeted delivery system wherein the constant replenishment of the colonic microbiota is achieved by concomitant administration of probiotics along with the polysaccharide based drug delivery system. Guar gum coated spheroids of sulfasalazine were prepared. In the dissolution studies, these spheroids showed markedly higher release in the simulated colonic fluid. In vivo experiments conducted in rats clearly demonstrated the therapeutic advantage of co-administration of probiotics with guar gum coated spheroids. Our results suggest that concomitant use of probiotics along with the polysaccharide based delivery systems can be a simple strategy to achieve satisfactory colon targeting of drugs.
结肠靶向剂型显著的临床成功一直受到其在靶部位不适当释放特性的限制。它们未能在结肠中完全释放药物可能归因于结肠环境的变化,这是由于病理状态、药物作用以及伴随疾病状态的心理压力,或者是这些因素的综合作用。正常结肠pH值和细菌状况的改变导致药物从设计的给药系统中不完全释放。我们报道了一种靶向给药系统的有效性,其中通过将益生菌与基于多糖的药物递送系统同时给药来实现结肠微生物群的持续补充。制备了瓜尔胶包衣的柳氮磺胺吡啶球体。在溶出度研究中,这些球体在模拟结肠液中显示出明显更高的释放率。在大鼠身上进行的体内实验清楚地证明了益生菌与瓜尔胶包衣球体联合给药的治疗优势。我们的结果表明,益生菌与基于多糖的递送系统同时使用可能是实现药物满意结肠靶向的一种简单策略。