SPL Set ID: 163898a4-6088-46a0-9253-dd9187c557be

Paliperidone extended-release tablets contains paliperidone USP, an atypical antipsychotic belonging to the chemical class of benzisoxazole derivatives. Paliperidone extended-release tablets 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 426.48. The structural formula is: Paliperidone, USP is sparingly soluble in 0.1N hydrochloride and methylene chloride; practically insoluble in water, 0.1N sodium hydroxide and hexane; and slightly soluble in N,N-dimethylformamide, tetrahydrofuran. 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 (beige) and 9 mg (pink) strengths. Paliperidone extended-release tablets utilizes OROS ® osmotic drug-release technology. Paliperidone extended-release tablets contain the following inactive ingredients: butylated hydroxy toluene, cellulose acetate, ferric oxide red, hydroxy ethyl cellulose, hypromellose, polyethylene glycol, polyethylene oxide, povidone, sodium chloride, sodium stearyl fumarate and titanium dioxide. Additionally, each 1.5 mg and 6 mg tablet contains iron oxide yellow, and 3 mg tablet contains talc. The tablet is imprinted with black pharmaceutical ink and contains following inactive ingredients: ferrosoferric oxide, propylene glycol and shellac. Delivery System Components and Performance Paliperidone Extended-Release Tablets uses osmotic pressure to deliver paliperidone at a controlled rate. The delivery system, which resembles a round-shaped tablet in appearance, consists of an osmotically active bilayer core surrounded by a subcoat and semipermeable membrane. The bilayer core is composed of two drug layers containing the drug and excipients, and a push layer containing osmotically active components. There is two precision laser-drilled orifice on the drug-layer side of the tablet. Each tablet strength has a different colored water-dispersible overcoat and print markings. In an aqueous environment, such as the gastrointestinal tract, the water-dispersible color overcoat erodes quickly. Water then enters the tablet through the semipermeable membrane that controls the rate at which water enters the tablet core, which, in turn, determines the rate of drug delivery. The hydrophilic polymers of the core hydrate and swell, creating a gel containing paliperidone that is then pushed out through the tablet orifice. The biologically inert components of the tablet remain intact during gastrointestinal transit and are eliminated in the stool as a tablet shell, along with insoluble core components. Image