Optimization of the Composition and Production Technology of Fucoidan Tablets and their Biopharmaceutical Evaluation
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Pharmaceutical Chemistry Journal, Vol. 54, No. 5, August, 2020 (Russian Original Vol. 54, No. 5, May, 2020)
OPTIMIZATION OF THE COMPOSITION AND PRODUCTION TECHNOLOGY OF FUCOIDAN TABLETS AND THEIR BIOPHARMACEUTICAL EVALUATION E. D. Obluchinskaya,1 O. N. Pozharitskaya,1 E. V. Flisyuk,2 and A. N. Shikov1,2,* Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 5, pp. 38 – 42, May, 2020.
Original article submitted October 18, 2018. 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. Keywords: fucoidan, tablets, formulation, technology, dissolution.
Fucoidans are complex branched heteropolysaccharides from brown algae and several echinoderms. The main fucoidan monosaccharide is L-fucopyranose [1]. Fucoidan exhibits low toxicity and a broad spectrum of biological activity including anti-inflammatory, antiviral, antiadhesive, antitumor, antioxidant, and hypolipidemic [1 – 3]. Anticoagulant activity is one of the most important types of activity of fucoidans because it enables them to be used as direct anticoagulants. Hemorrhagic complications and recurrent diseases were reported after the use of known anticoagulants [4 – 8]. Therefore, the discovery of new peroral anticoagulants with low toxicity and risk is critical. Fucoidans from brown algae are a good alternative, especially for peroral administration. Thus, administration of fucoidan from Fucus evanescens to mice over 30 d produced a pronounced anticoagulant effect without side effects [9]. Fucoidan from Laminaria japonica inhibited formation of
arterial thrombosis and stimulated electrical shock in mice after peroral administration (30 d) [10]. A single peroral administration of fucoidan from F. vesiculosus increased anti-activated factor X activity (anti-Xa) in blood of outbred rats without signs of hemorrhagic complications and toxicity [11]. The anticoagulant activity of fucoidan powder was confirmed in pilot tests on volunteers [12]. Fucoidan drug substance is highly hygroscopic and possesses poor technological properties that hinder therapeutic application. The goal of the present study was to develop the optima
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