Influence of immediate release tablet formulation on dissolution profile of paracetamol

Abstract

Introduction: Paracetamol is analgesic and antipyretic, which is usually in the form of an immediate release tablet formulations. Therapeutic eff ects in terms of the speed and intensity of the analgesic eff ect is dependent on speed of liberation from formulation. Aim: The aim of this work was to determine and compare dissolution profi les of 4 paracetamol immediate release tablet formulations and to determine infl uence of excipients on kinetic of paracetamol dissolution. Materials and Methods: Dissolution profi les of paracetamol tablets were determined using method with paddles and phosphate buff er pH 6.8 as a medium. Release of paracetamol was followed 60 minutes (using 6 time points). Concentration of paracetamol was measured using UV/Vis spectrophotometric method (243 nm). Dissolution profi les were compared using model-independent method (diff erence factor and similarity factor), statistic method (ANOVA-based method and pair Student's T-test, p<0.05) and model dependent methods (to determinate the release kinetics of paracetamol). Results: All formulations in the fi rst 45 minutes liberated more than 85 % of the labled content. Formulation D, which contained superdesintegrator, released 90% of the content in the fi rst 5 minutes. Though based on values of diff erence and similarity factors formulations are, not signifi cantly diff erent, ANOVA-based method showed that formulation A and B, B and C, as well as formulation B and D do statistically diff er in all 6 time points, meaning they have parallel profi les. The release of paracetamol from formulations A and D is best described by the fi rst order kinetic model, while the release of formulations B and C by the logistic model. Conclusions: The release kinetic of paracetamol is mostly infl uenced by the type of superdisintegrants and lubricants. Formulation with superdisintegrant technology OptiZorb ® demonstrated fastes release rate and thus it is expected to produce the fastest pharmacodynamic eff ect.

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