Pharmaceutical development of composition of effervescent tablets with acetylsalicylic acid, paracetamol, and...

This study aims to develop and optimize a stable composition of effervescent tablets containing acetylsalicylic acid (300 mg), paracetamol (200 mg), and ascorbic acid (300 mg) for the Ukrainian pharmaceutical market. A systematic pharmaceutical development approach was employed, utilizing dispersion and regression analysis to evaluate the impact of various functional groups of excipients on twelve critical quality indicators. The research included a comprehensive assessment of the tableting blend's pharmaco-technological properties (bulk/tapped density, Carr's index, flowability, and angle of repose) and the finished tablets' quality (pressing process, appearance, mass uniformity, hardness, friability, and disintegration). Organoleptic attributes of the resulting solution, including transparency, odor, and taste, were also evaluated. The initial screening phase identified the most effective types of fillers, disintegrants, and lubricants for direct compression. Experimental data scientifically established the optimal stoichiometric ratio between anhydrous citric acid and sodium bicarbonate as 1:1.312. Subsequent optimization using a utility function and regression analysis allowed for the selection of the best glidants, sweeteners, and flavorings. The interaction between the quantities of a co-processed binder and a sorbitol-based filler was proved to be critical for achieving the required tablet hardness and rapid disintegration. The finalized composition, containing an optimized matrix of anhydrous citric acid, sodium bicarbonate, lactose, polyvinylpyrrolidone, crospovidone, sorbitol, sodium saccharin, lemon flavoring, and sodium stearyl fumarate, successfully met all pharmacopoeial requirements and exceeded the criteria of the Quality Target Product Profile. Long-term stability studies confirmed a 24-month shelf life in aluminum-polymer packaging. The study resulted in a scientifically validated composition that provides a fast-acting, consumer-friendly, and cost-effective domestic alternative to imported analgesic and antipyretic combinations, significantly enhancing patient compliance and accessibility within the local market.