Abstract

Aspirin has low solubility in water therefore, dissolution is a rate limiting step for absorption. Floating tablet formulation is designed to improve the bioavailability of aspirin. The objective of this study was to determine in vitro dissolution study of aspirin floating tablet release kinetics model. The floating tablets were prepared by a direct compression method using Methocel K4M CR, NaHCO3, Ethocel, Aerosil, and dicalcium phospate anhydrous as excipients. Tablets were evaluated by different parameters such as physicochemical properties, floating lag time (Flag time), total floating time, and dissolution. The result showed that the tablet mass has good flow properties of 13.54 g/sec. Aspirin floating tablets had a weight uniformity (CV=1.45%), good hardness (6.42kg), and low friability (0.158%). The tablet has a short Flag time of 25.16 sec and long floating time of 8 hours. Dissolution data were evaluated using DDSolver conducted by (1) Statistical parameters: R2adjusted, AIC, MSC; (2) Visual goodness of fit (GOF). The results showed that aspirin floating tablets release kinetics followed the Korsmeyer-Peppas model. Aspirin release occurs through the mechanism of anomalous transport which combines Fickian diffusion and polymer relaxation. Key words: aspirin floating tablet, DDSolver, modeling of drug release

Highlights

  • Aspirin is used as an antiplatelet for stroke prophylaxis (Laurer, 2002; Awtry and Loscalzo, 2000; Patrono and Rocca, 2008)

  • Information on the mechanisms and kinetics of dissolution is important to estimate the absorption of aspirin floating tablet

  • Aspirin floating tablets was able to float during dissolution test, intact and not eroded

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Summary

Introduction

Aspirin is used as an antiplatelet for stroke prophylaxis (Laurer, 2002; Awtry and Loscalzo, 2000; Patrono and Rocca, 2008). Aspirin has low solubility in water (1:300) (Moffat et al, 2011; Sweetman, 2009) dissolution is one of the rate limiting step in their absorption and bioavailability (Gordon et al, 1994; Wells, 2002). The nonlinear fitting of dissolution data can be performed using a professional statistical programs such as Micro-Math Scientist, GraphPad Prism, SigmaPlot, or SYSTAT. These programs require the user to define the equations manually and need the initial value for each parameter (Zhang et al, 2010). DDSolver is a new software developed for the kinetic analysis of dissolution data (Murtaza et al, 2012) with a non-linear regression approach. Most scientists are already familiar with Excel because of its wide availability

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