SPL Set ID: a5492459-e0a2-4c16-9fff-c886e0b4c700

Paliperidone extended-release tablet contains paliperidone USP, an atypical antipsychotic belonging to the chemical class of benzisoxazole derivatives. Paliperidone contains a racemic mixture of (+)- and (-)- paliperidone. The chemical name is (±)-3-[2-[4-(6-fluoro-1,2-­benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-­pyrido[1,2-a]pyrimidin-4-one. Its molecular formula is C 23 H 27 FN 4 O 3 and its molecular weight is 426.49. The structural formula is: Paliperidone is sparingly soluble in 0.1N HCl and methylene chloride; practically insoluble in water, 0.1N NaOH, and hexane; and slightly soluble in N,N-dimethylformamide. Paliperidone extended-release tablets are intended for oral administration and are available in 1.5 mg (brown), 3 mg (white to off-white), 6 mg (yellow), and 9 mg (pink) strengths. Paliperidone extended-release tablets are formulated as a polymer matrix based once-a-day controlled release tablet for oral use. Inactive ingredients are polyethylene oxide, hypromellose, anhydrous lactose, magnesium stearate, ethyl cellulose, triethyl citrate, talc, titanium dioxide and polyethylene glycol. The 1.5 mg and 6 mg tablets also contain lactose monohydrate, iron oxide yellow and iron oxide red. The 9 mg tablets also contain lactose monohydrate and iron oxide red. Imprinting ink contains shellac glaze, iron oxide black, N-butyl alcohol, propylene glycol and ammonium hydroxide. structure Delivery System Components and Performance Paliperidone extended release tablets employ a film-coated hydrophilic hydrogel matrix to deliver paliperidone at a controlled rate over 24 hours. The system comprises of: a core consists of the drug, rate-controlling polymer (forming hydrogel) and other excipients with pH independent coat surrounding core, comprising of water soluble and insoluble polymer and a film coat over it. Upon ingestion outer film coat dissolves exposing the coated tablet to the gastric fluids. Once the water soluble polymer from coat gets dissolved, pores are formed which allow penetration of fluid inside the membrane leading to hydration of core-forming hydrogel. Drug release occurs via slow diffusion out of the gel layer and subsequent gel erosion.