SPL Set ID: d7033e52-3df2-48e2-adda-15a57c2f148f

Paliperidone extended-release tablets contain paliperidone, 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), 6 mg (beige), and 9 mg (pink) strengths. Paliperidone extended-release tablets utilize OROS ® osmotic drug-release technology. Inactive ingredients are butylated hydroxytoluene, cellulose acetate, ferric oxide red, hydroxypropyl cellulose, hypromellose, polyethylene glycol, polyethylene oxides, povidone, stearic acid and sodium chloride. The film coating of 1.5 mg and 6 mg tablets contains ferric oxide red, ferric oxide yellow, ferrosoferric oxide, hypromellose, polyethylene glycol and titanium dioxide. The film coating of 3 mg tablets contains lactose monohydrate, hypromellose, titanium dioxide and triacetin. The film coating of 9 mg tablets contains ferric oxide red, hypromellose, polyethylene glycol and titanium dioxide. The imprinting ink contains ammonium hydroxide, ferrosoferric oxide, isopropyl alcohol, N-butyl alcohol, shellac glaze and propylene glycol. Delivery System Components and Performance Paliperidone extended-release tablets use 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 is one precision laser-drilled orifice 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 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. chem draw structure