Study objectives were to develop a unique floating ring capsule dosage form which combines gastric soluble and insoluble portions, and to evaluate its suitability for stomach specific drug delivery. New floating ring capsules were developed using different polymers and were compared for various parameters. The formulation with HPMC and sodium CMC has better floating properties. The effects of polymers concentration on drug release were studies by in vitro release studies. The interaction studies of combined drug with polymers were determined using FT-IR spectroscopy. The entrapped air within the gel barrier and lower densities of HPMC and sodium CMC resulted in better floating behavior. Steady slow gel formations showed prolonged drug release. The in vitro release rates were generally found to be faster with low concentration of carbopol showing release within 2 h, while formulations containing high amount of HPMC showed release in 8 h. In particular, the higher concentration of HPMC formulation shows the best drug release performance. A very low change in peak shift was observed only with sodium alginate formulations. Further, FT-IR measurements confirmed the absence of any chemical interactions. Results indicate that new floating ring capsule is a promise dosage form for stomach specific delivery.
Lactulose is used as a triggering substance in a unique colon-specific delivery technology called CODESTM. Colonic microflora degrades lactulose and forms short-chain fatty acids to activate the CODESTM system. However, lactulose has been reported to cause a Maillard-type reaction with substances containing primary or secondary amino groups that may produce carcinogenic compounds. Thus, the aim of this study was to look into the possibility to substitute lactulose with isomalt for fabrication of CODESTM. The in vitro degradation of both sugars before incorporating them into the CODESTM system was evaluated with the help of rat caecal microflora. The results showed that isomalt was less efficient with regard to its rate and extent of degradation into short-chain fatty acids by the microflora compared to lactulose. However, the in vitro dissolution study did not show a significant difference in the performance between lactulose and isomalt when they were incorporated separately in CODESTM. A similar result was also obtained in the in vivo study. Based on the above results, isomalt could be used as an alternative to lactulose for colonic delivery system utilizing the principles of CODESTM.
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