Optimization of the Composition and Production Technology of Fucoidan Tablets and their Biopharmaceutical Evaluation

Abstract

The discovery and development of drugs that can compete in effectiveness with direct anticoagulants is a critical problem. Fucoidan is a complex branched heteropolysaccharide with anticoagulant and antithrombic activity. Fucoidan drug substance is hygroscopic and possesses poor technological properties. This study was aimed at development of the optimum composition and technology of fucoidan tablets and their biopharmaceutical evaluation. The generalized Harrington desirability function and dispersion and regression analyses were used for optimization of the fucoidan tablet formulation. The contents of crospovidone and lactose were the most significant factors affecting the disintegration and compressibility of model tablets. The lactose content had the greatest impact on the Carr index and Hausner ratio. The in vitro dissolution curves of the tablets were compared (at pH 1.2, 5.7, and 6.8). The in vitro release of fucoidan from the developed tablets obeyed a first-order kinetic equation.