Cross linked alginate gel beads as floating drug delivery system for cefdinir: optimization using Box–Behnken design

摘要

Regional absorption of several drugs necessitates the continuous monitoring of the movement of dosage form through gastro-intestinal tract. Sometimes it is important to deliver the drug at a particular physiological region of the gastrointestinal tract for better effects. Floating delivery system is a prominent approach to release the drug in the gastric fluid. The objective of present study was to formulate, evaluate and optimize cefdinir loaded intra-gastric floating beads of sodium alginate. Floating alginate beads were prepared by ionic gelation method according to Box–Behnken design with three factors varied at three levels. Uniform beads buoyant up to 24 h were formed with rough surface and porous internal structure. Characterization by Fourier transform infrared spectroscopy, differential scanning calorimetry, thermo-gravimetric analysis and powder x-ray diffractometry suggested an excellent compatibility of drug with excipients and formulation process. The effect of selected independent variables [amount of sodium alginate (X1), myristyl alcohol (X2) and cefdinir (X3) each at three levels] on the dependent variables [density (Y1), entrapment efficiency (Y2), time to release 20 % (Y3), cumulative percentage of cefdinir released at 12th hour (Y4) and dissolution efficiency (Y5)] were studied using regression equations and response surface plots. The predicted and adjusted r2 values were in reasonable agreement and the models were significant with p 0.05. Criteria were set for each responses and optimized formulation was prepared according to the software determined levels. The predicted and observed responses were in good agreement with low percent bias errors (10 %), marking the validity of the developed model. Thus, cefdinir loaded, extended release, intra-gastric floating gel beads of calcium alginate were formulated and optimized.