Abstract

FORMULATION AND EVALUATION OF RIVAROXABAN ORODISPERSIBLE TABLETS

Mahmoud Mahyoob Alburyhi*, Mohammed Abbas Hamidaddin, Abdalwali Ahmed Saif and Maged Alwan Noman

ABSTRACT

The most common and preferable route of drug administration is through the oral route. Novel oral drug delivery systems aim to enhance safety and efficacy of drug molecule by formulating a convenient dosage form for ease of administration and to achieve better patient compliance. Orodispersible tablets (ODTs) are among these systems, the concept of Orodispersible tablets is to disperse the tablets within seconds in the mouth in the presence of saliva with no need for water, and without any difficulty of swallowing, due to the presence of superdisintegrants in their formulation. Rivaroxaban is a direct oral anticoagulant, that works by inhibition of factor Xa. Rivaroxaban is available in different doses. The 20 mg dose is used in the treatment of atrial fibrillation. The 15 and 10mg doses are used in the treatment and prevention of deep vein thrombosis and pulmonary embolism. The 2.5 mg dose is used in combination with aspirin, to reduce the risk of major cardiovascular events and major thrombotic vascular events in patients with coronary artery disease and peripheral artery disease respectively. Rivaroxaban is absorbed primarily in the
stomach, as there is reduced absorption when the drug is released into the proximal small intestine, with further reduction as the drug is released more distally into the small intestine and colon. The objective of this study was to formulate Rivaroxaban Orodispersible tablets to ensure the release of the drug at the sites of its absorption, also to develop a patient-friendly Orodispersible tablets of Rivaroxaban to increase the patient’s adherence and compliance to the therapy. Rivaroxaban was prepared as an Orodispersible tablets in 2.5mg dose. Six formulae containing crospvidone, sodium starch glycolate, and croscarmellose sodium as superdisintegrants in different ratios. Then, each formula was evaluated for precompression parameters, then prepared by direct compression method. Finally, the compressed tablets of each formulae were evaluated for the post compression parameters. All the formulae showed satisfactory tablet properties. Among all formulations the best formulation was F1 due to the maximum drug release, which was 83.2% in one minute and the assay of Rivaroxaban was within the acceptable limit.

Keywords: Rivaroxaban, Orodispersible tablets, Superdisintegrants, Oral anticoagulant.