Kaur Rupinderjeet, Gulati Monica, Singh Sachin Kumar
School of Pharmaceutical Sciences, Lovely Professional University, Punjab, 144 401, India.
School of Pharmaceutical Sciences, Lovely Professional University, Punjab, 144 401, India.
Int J Biol Macromol. 2017 Feb;95:438-450. doi: 10.1016/j.ijbiomac.2016.11.066. Epub 2016 Nov 19.
The present study explains the effect of concomitant administration of synbiotics with the polysaccharide based colon targeted delivery system. As the gut microflora get deranged on administration of mesalamine, drug release from such delivery systems is expected to be jeopardised because the release trigger is dependent solely on the colonic microbiota. To overcome this limitation, mesalamine was formulated as microspheres with guar gum and xanthan gum (prebiotics). These were combined with probiotics containing Lactobacillus acidophilus, L. rhamnosus, Bifidobacterium longumand Saccharomyces boulardi. Dissolution studies of the prepared formulation conducted in simulated colonic fluid clearly demonstrated its superiority over the marketed, delayed release dosage forms of mesalamine. The therapeutic benefit of the concomitant administration of synbiotic with mesalamine was evidenced by the comparative evaluation of faecal contents, weight gain trend and histopathological studies conducted in rats. The results suggest that co-administration of synbiotics with mesalamine can be used as a convenient methodology to achieve efficient and cost-effective targeting of the drug to colon.
本研究阐述了合生元与基于多糖的结肠靶向递送系统联合给药的效果。由于服用美沙拉嗪后肠道微生物群会紊乱，预计此类递送系统的药物释放会受到影响，因为释放触发因素仅依赖于结肠微生物群。为克服这一局限性，将美沙拉嗪与瓜尔胶和黄原胶（益生元）制成微球。这些微球与含有嗜酸乳杆菌、鼠李糖乳杆菌、长双歧杆菌和布拉氏酵母菌的益生菌相结合。在模拟结肠液中对所制备制剂进行的溶出度研究清楚地表明，其优于市售的美沙拉嗪缓释剂型。通过对大鼠粪便内容物、体重增加趋势和组织病理学研究的比较评估，证明了合生元与美沙拉嗪联合给药的治疗益处。结果表明，合生元与美沙拉嗪联合给药可作为一种方便的方法，实现药物高效且经济高效地靶向结肠。
