SPL Set ID: e713556e-028e-0f4c-e053-2995a90a9e9f

Paliperidone Extended-Release Tablets contain paliperidone, USP, an atypical antipsychotic belonging to the chemical class of benzisoxazole derivatives. Paliperidone extended-release tablets contain a racemic mixture of (+)- and (-)- paliperidone. The chemical name is (9 RS )-3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4 H -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 3 mg (white), 6 mg (light beige), and 9 mg (pink) strengths. Paliperidone extended-release tablets utilize osmotic drug-release technology [see Description (11) ] . Inactive ingredients are butylated hydroxytoluene, cellulose acetate, colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose, polyethylene glycol, polyethylene oxide, red iron oxide, sodium chloride, sodium stearyl fumarate, talc, titanium dioxide and yellow iron oxide. The 3 mg tablets also contain polyvinyl alcohol. The 6 mg tablets also contain black iron oxide, FD&C Blue No. 1 Aluminum Lake and polyvinyl alcohol. The 9 mg tablets also contain FD&C Blue No. 1 Aluminum Lake and polyvinyl alcohol. The imprinting ink contains the following: black iron oxide, hypromellose and propylene glycol. Delivery System Components and Performance Paliperidone extended-release uses osmotic pressure to deliver paliperidone at a controlled rate. The delivery system, which resembles a capsule-shaped tablet in appearance, consists of an osmotically active trilayer core surrounded by a subcoat and semipermeable membrane. The trilayer core is composed of two drug layers containing the drug and excipients, and a push layer containing osmotically active components. There are two precision laser-drilled orifices on the drug-layer dome 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 orifices. 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. description