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Abstract

This work aims to develop a Tapentadol Hydrochloride (TPHCl) sustained-release tablet. TPHCl is an analgesic drug that can act centrally, so it has efficacy in different types of pain, such as inflammatory origin pain, neuropathic pain, as well as acute and chronic pain. Tapentadol has very low plasma protein binding, and its activity is independent of metabolic activity. The research showed that conventional therapy cannot obtain prolonged release of the drug from the dosage form. TP belongs to the BPCS class- I drug, and in order to reduce the frequency of its administration, Tapentadol is suggested to be prepared as a sustained-release dosage form through oral delivery. Sustained release tablets of TPHCI were prepared by using polymers such as Hydroxypropyl methylcellulose (HPMC K4M) and Eudragit RL100 by the wet granulation method, and then the physical and chemical characteristics were evaluated. The tablets with a hydrophilic-based matrix were unsuccessful in extending the release of the drug, whereas the tablets with a hydrophobic-based matrix had less drug release. Zero-order kinetics can be obtained from the tablets with a hydrophilic and hydrophobic polymer matrix, and the drug release mechanism was non-Fickian diffusion-controlled. Therefore, the latter tablets can be formulated as an alternative to conventional TPHCl tablets‎.

Keywords: TPHCl, HPMC K4M, Sustained release, Matrix tablet, Dissolution

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