Development of Conventional Liquid Oral Suspension of Posaconazole by using Quality by Design approach

Abstract

The aim of our research was to apply experimental design methodology in the development and optimization of Posaconazole in conventional suspension form. The conventional suspension technology can be applied to drugs that are water and organic solvents insoluble. Posaconazole is hydrophobic drug so it was selected for suspension formulation. The various common screening designs, such as two-level full factorial, fractionate factorial, and PlackettBurman designs and optimization designs, such as three-level full factorial, central composite designs, and Box–Behnken designs, were used in designing Posaconazole in suspension. On the basis of previous results, response surface methodology and Centre composite design (CCD) experimental design was used to characterize and optimize three physicochemical parameters, that is, particle size, particle shape, morphology rotation speeds of the stirring elements, pH, and ionic strengths of the dissolution medium, affecting the release of Posaconazole from the suspension in vitro.  Afterward, the information about the model reliability was verified using the analysis of variance. The estimation of various factors was done using Design Expert® software (Version 11.0.5.0, Stat-EaseInc., MN). Our study proved that experimental design methodology could efficiently be applied for characterization and optimization of analytical parameters affecting drug release and oral bioavailability of Posaconazolein vitro and invivo that it is an economical way of obtaining the maximum amount of information in a short period of time and with the fewest number of experiments.Therefore, design of expert was presented in detail since it is the main component of pharmaceutical and analytical QbD. The optimized suspension is a promising drug delivery system that may increase the bioavailability of posaconazole.