Development of Sodium Benzoate Tablets with Dual Burst Release: Hydrophilic Matrix System

Abstract

Sodium benzoate is the sodium salt of benzoic acid, well soluble in water and is primarily known and used as a preservative due to its antifungal and antimicrobial qualities. Therefore, it is widely used in products such as medicines, foods, and cosmetics.The aim of this research project was to develop a dosage form with a dual burst release system over an eight-hour period. The targeted dissolution profile was defined as 25% release at 30–60 minutes, 50% ± 5% at five hours, 70% ± 5% at six hours, and 90–100% at eight hours. Dual burst release system is a method for regulating active pharmaceutical ingredient (API) release in two distinct phases. This type of release system is often preferred over more conventional systems as it enhances efficacy, decreases adverse reactions and reduces dosing frequency. To achieve dual burst release, tablets with hydrophilic matrix system were developed. These tablets consist of a hydrophilic matrix system that incorporates the API. The hydrophilic polymers swell up and function as a barrier and control the release of the API. A total of 27 formulations containing various proportions of hydrophilic polymers with specific characteristics and excipients were manufactured and tested. The formulations underwent a dissolution test and the one with the dissolution profile that most closely aligned with the goal was selected as the final formulation. F23 was chosen as a final formulation. The amount of sodium benzoate released during the initial burst averaged approximately 23%, which, although slightly below the target of 25%, was considered acceptably close. The overall dissolution profile met the goal for complete release; however, other aspects of the release profile did not fully align with the original goal. Additionally, most formulations exhibited dissolution profiles consistent with first-order kinetics. The final formulation underwent testing according to European Pharmacopoeia (Ph. Eur.) standards, with inconsistent results. Although further optimization is needed, the study demonstrates the feasibility of using matrix tablets to achieve dual burst release of sodium benzoate.