SPL Set ID: be30f3cc-55fb-4a74-9778-60573a7f18c6

Paliperidone extended-release tablet contains paliperidone, USP, an atypical antipsychotic belonging to the chemical class of benzisoxazole derivatives. Paliperidone extended-release tablets contain a racemic mixture of (+)- and (-)- Paliperidone, USP. 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 [l,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, USP is sparingly soluble in 0.1 N hydrochloride and in methylene chloride, slightly soluble in N,N dimethyl formamide and in tetrahydrofuran; practically insoluble in water, in 0.1 N sodium hydroxide, and in hexane. Paliperidone extended-release tablets are intended for oral administration and are available in 1.5 mg (orange-brown), 3 mg (white), 6 mg (beige), 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 mannitol, microcrystalline cellulose, hypromellose, magnesium stearate, hydroxypropyl cellulose, hypromellose phthalate, ethylcellulose, dibutyl sebacate, polyethylene glycol and titanium dioxide. The 1.5 mg tablets also contain FD&C Yellow #6 Aluminum Lake, D&C Yellow #10 Aluminum Lake and FD&C Blue #2 Aluminum Lake. The 6 mg tablets also contain iron oxide yellow, iron oxide red and iron oxide black. The 9 mg tablets also contain iron oxide red. The tablets are imprinted with edible black ink. The edible ink contains shellac, isopropyl alcohol, iron oxide black, n-butyl alcohol, propylene glycol and ammonium hydroxide. Delivery System Components and Performance Paliperidone Extended-Release Tablet uses a pH-independent hydrophilic matrix and pH dependent enteric coating to deliver Paliperidone, USP at a controlled rate. The Paliperidone Extended-Release Tablet comprises of an inner core made of the drug, rate controlling pH independent hydrophilic polymers and other excipients. The core is surrounded by barrier layer of pH independent polymer followed by enteric coating. When tablet expose to an acidic environment such as the stomach, the drug release will be minimal due to outer enteric coating of the pH dependent polymer. The outer enteric coating upon reaching an environment of pH 5.5 and above it starts to dissolve and the polymer in the inner core tablet will hydrate to form a gel layer. The drug releases via diffusion from a gel layer and subsequently through gel erosion. structure