ABSTRACT:
Osteoporosis is a major problem worldwide especially in postmenopausal women and is treated with bisphosphonates. The drug belongs to BCS class II, and thus has high solubility and low permeability and has severe gastric ulceration side effects. To overcome these problems Risedronate (drug) loaded in microsphere in an enteric coated formulation were prepared. Microparticles were prepared by simple emulsification technique based on glutaraldehyde crosslinking and were coated with Eudragit L-100. The microspheres were characterized for entrapment efficiency, drug loading, in vitro drug release, surface morphology, as well as particle size analysis, and FTIR spectroscopy. Particle sizes, as measured by the optical microscopic technique, were of an average size in the range 200 um to 320 um with drug content 5.02- 9.88 and entrapment efficiency upto 82%. FTIR data signifies no interaction between the drug and polymer used. In vitro release studies were performed into phosphate buffers (pH 1.2 for 2 hr and pH 6.8 at 37°C) as a function of cross linking coating density of the microspheres. Less than 10 % release was at pH 1.2 which confirms the enteric coating of microsphers. Drug release was in the range of 65- 80% in 6 hrs and follows Higuchi release kinetics. The findings of the present study conclusively state that enteric coated microspheres of Risedronate are potential for restricting drug release in stomach and sustained drug delivery in intestinal region avoiding the gastric iritation effect of Risedronate.
Cite this article:
Gautam and Suresh (2016). Enteric Coated Microparticulate System: Novel Approach for the Treatment of Osteoporosis. Journal of Ravishankar University (Part-B: Science), 29(1), pp.152-153.