development and investigation of novel drug abuse deterrent technology for tapentadol hydrochloride

Abstract

Background: Increased misuse of pharmaceutical opioid formulation today become one of the big-socio economical problem for the world and as a part of multidisciplinary approach, USFDA encourage development and approval of only pharmaceutical opioid formulation having abuse deterrent characteristics. newlineObjectives: To develop and in-vitro investigation of novel controlled release anti-overdose crush and extraction-resistant drug delivery system. newlineMethods: Drug particulates of Tapentadol HCl was fabricated using different polymers by thermal and non-thermal manufacturing process. Controlled release properties were incorporate by applying extended-release coat on the drug particulates to match dissolution profile with Brand NUCYNTA-ER. Self-regulated pH modulating release properties was incorporated by addition of pH dependent release and pH elevating component. The drug particulates composition were optimized by-applying factorial design. Naltrexone HCl as separate subunits in non-releasable form was incorporated in the dosage form to hinder tampering with the dosage form. newlineResults: Only drug particulate made of Polyox retarded drug extraction by gt80% at RT and gt90°C. After 5 minutes of grinding in coffee grinder, crushed drug particulates containing Polyox were retained gt99% on the ASTM-170# screen. The syringeability/injectability attempt was unsuccessful. In normal conditions, Tapentadol HCl released gt90% at 8 hours while no release of Naltrexone HCl. In overdose condition, none of the Tapentadol HCl and Naltrexone HCl were release at 8 hours. Different in-vitro manipulation studies indicated that Tapentadol HCl and Naltrexone HCl were released/extracted simultaneously. newlineConclusion: The analytical data demonstrated successful anti-overdose properties of Tapentadol HCl while hindering crush-and-extraction resistant to the dosage form. newline newline