科研之友
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摘要
The present work aimed at development of ranolazine loaded floating biomaterial gellan beads to enhance its site specific absorption. The beads obtained by ionotropic gelation method using sodium bicarbonate as gas-forming agent, calcium chloride and chitosan as a crosslinker were evaluated for physicochemical properties and in vitro performance. Yield and entrapment efficiency varied from 90 to 97% and 58 to 81% respectively. Surface topography revealed spherical microparticles with evenly distributed pores. Differential scanning calorimetry and powder X-ray diffraction pointed out amorphous nature of the drug. Effect of formulation variables on floating lag time and time required for 50% drug release was studied using Box-Behnken factorial design. The beads displayed good in vitro floatability in 0.1 N HCl with initial burst release followed by a controlled release up to 10 h whereas slow drug release was observed in phosphate buffer pH 6.8; probably due to decreased drug solubility and accelerated internal gelation through ionic crosslinking of gellan monomers. The beads, when studied in non-everted rat stomach and intestinal sac models, demonstrated twofold decrease in flux and apparent permeability coefficient as compared to pure ranolazine. Floating gellan beads proved advantageous for controlling the release and enhancing therapeutic activity of ranolazine.
- 出版日期2015-1
