Development and evaluation of taste-masked dry suspension of cefuroxime axetil for enhancement of oral bioavailability

Abstract

Cefuroxime axetil (CA) is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally. This work was to mask the bitter taste of CA and enhance its oral bioavailability. Dry suspensions were prepared by means of wet granulation method and solid dispersion method. Binders, suspending agents and other compositions involved in the formulation were optimized. The differential scanning calorimetry (DSC) analysis indicated that CA was amorphous in the solid dispersion with stearic acid as the carrier, which contributed to an improvement of the dissolution rate. Taste evaluation was performed by three volunteers and taste masking was successfully achieved by the methods mentioned above. A pH 7.0 phosphate buffer was adopted to study the in vitro dissolution performance of the three formulations, i.e., two self-made dry suspensions and the commercial one. With a better release characteristic and a satisfying taste masking ability, the solid dispersion suspension was selected as the optimal formulation for the further pharmacokinetic study in beagle dogs. The values of Cmax and AUC0–12 for the solid dispersion suspension were about 1.78-fold and 2.17-fold higher than these of reference suspension, respectively. The obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability.