Formulation by design approach for effervescent granules of vitamin C using statistical optimization methodologies

Introduction: Ascorbic acid (vitamin C), is a potent antioxidant, and the human body cannot synthesis it, so ascorbic acid can be obtained from external sources as food and pharmaceutical products. Objective: This study was using formulation by design (FbD) concept to prepare effervescent granules of vitamin C with high quality and more patient compliance in less effort and cost. Methods: A 23 factorial design was used to study the physical and chemical characteristics of the granules (disintegration time (DT), taste of product (TP), carbon dioxide amount (CO2), and pH of the solution). Also the effects of and interaction between selected independent variables (citric acid, tartaric acid, and sodium bicarbonate) evaluated, while, their concentrations were optimized by application of optimization model methodology for factorial design. Formulations were prepared by non-aqueous wet granulation method. Results: From the results of designed batches, the disintegration time ranged from 33±2.7 to 153±3.3sec while the amount of carbon dioxide ranged from 0.360±0.004gm to 1,512±0.002gm also the pH range was from 2.9±0.09 to 6.42±0.07 but the taste of product was coded numerically in proportional with acceptability from 1 to 5.   According to the experimental design, both of studied independent variables have significant effect in determining the physicochemical characteristics of effervescent granules. Conclusion: FbD concept effectively was utilized for the development of vitamin C effervescent granules as per modern quality practices used in pharmaceutical industries