Design and characterization of enteric-coated controlled release mucoadhesive microcapsules of Rabeprazole sodium

作者:Swain Suryakanta*; Behera Upali A; Beg Sarwar; Sruti J; Patro Ch Niranjan; Dinda S C; Rao M E B
来源:Drug Development and Industrial Pharmacy, 2013, 39(4): 548-560.
DOI:10.3109/03639045.2012.676047

摘要

The objectives of present work was to design and characterize the rabeprazole sodium loaded microcapsules prepared by solvent evaporation technique using ethyl cellulose (EC) based various mucoadhesive polymer, followed by a triple coating with Eudragit L100. The Box-behnken design (BBD) was applied for optimization of formulations containing EC, HPMCK100M and Eudragit L100 as factors for selected responses like entrapment efficiency, mucoadhesive property and drug release in 24 h. The prepared microcapsules were characterized for particle size, drug content, swelling index, mucoadhesive strength, and in vivo antiulcer activity. FT-IR studies revealed that there was no drug-polymer interaction. SEM studies revealed that microcapsules were non-aggregated, spherical shape and smooth appearance. In vitro drug release data from microcapsules was fitted to different kinetic models to explain release profiles. The correlation coefficient value (r(2)) indicated that the drug release followed Higuchi model. Analysis of variance (ANOVA) showed significant difference in the release of drug from all formulations at p < 0.05 level. Accelerated stability study of optimized formulation (F4) upto 6 months showed there was no change in drug content and release characteristics during storage. In vivo antiulcer activity showed that the optimized microcapsules were able to protect rat stomach against ulcer formation vis-a-vis aqueous solution of the drug showed only negligible and minimum effect.

  • 出版日期2013-4