eskayef pharmaceuticals limited - Medication Listings

Paliperidone Extended-Release Tablets contains paliperidone, 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)-1piperidinyl]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 in methylene chloride; practically insoluble in water, in 0.1N NaOH and hexane; and slightly soluble in N, N-dimethyl formamide and in Tetrahydrofuran. Paliperidone Extended-Release Tablets are intended for oral administration and are available in 1.5 mg (blue), 3 mg (white), 6 mg (yellow), and 9 mg (beige) strengths. Paliperidone Extended-Release Tablets utilizes Osmotic Drug delivery (OROS, Push-Pull technology) system. Inactive ingredients are hydroxypropyl cellulose, butylated hydroxytoluene, polyethylene oxide, talc, sodium chloride, colloidal silicon dioxide, sodium stearyl fumarate, iron oxide red, cellulose acetate, polyethylene glycol, polyvinyl alcohol, and titanium dioxide. The 1.5 mg tablets also contain F D & C blue # 2 and the 6 mg, and 9 mg tablets also contain iron oxide yellow. The imprinting ink contains shellac, black iron oxide, propylene glycol, and ammonium hydroxide. Chemical Structure Delivery System Components and Performance Paliperidone Extended-Release Tablets uses osmotic pressure to deliver paliperidone at a controlled rate. The tablets contain an osmotically active bi-layer core tablet that consists of a drug layer containing the entire amount of active ingredient in a hydrophilic polymer matrix and a push layer that contains an osmotic agent in a hydrophilic, swell-able polymer matrix. The bi-layer core tablet is coated with a release-controlling semi-permeable membrane (SPM). The SPM allows water permeation into the core without allowing components to quickly dissipate from the core. A laser-drilled aperture is present on the drug layer side of the SPM-coated tablet and is necessary for delivery. The tablets contain a water-soluble cosmetic over-coating that is imprinted with an identifier. Once ingested, the cosmetic over-coating rapidly dissipates in the gastrointestinal tract. The SPM allows water to penetrate into the core as the osmotic agent in the push layer provides a driving force for water influx. Once hydrated, the swell-able polymer matrix in the push layer (high molecular weight polyethylene oxide) expands, exerting a pressure on the drug layer portion of the core tablet which forces it out of the laser-drilled aperture in a plug-flow fashion. As the release rate is controlled by the rate of water influx into the core (SPM permeability), the delivery is independent of pH or gastrointestinal motility. The biologically inert tablet core, containing residual push layer components, remains intact and is eliminated in the feces. Drug absorption is controlled by a combination of drug release from the tablet and subsequent dissolution in the gastrointestinal tract.

Pregabalin is described chemically as ( S )-3-(aminomethyl)-5-methylhexanoic acid. The molecular formula is C 8 H 17 NO 2 and the molecular weight is 159.23. The chemical structure of pregabalin is: Pregabalin is a white to off-white, crystalline solid with a pK a1 of 4.2 and a pK a2 of 10.6. It is freely soluble in 1N Hydrochloric acid and sparingly soluble in water. The log of the partition coefficient (n-octanol/0.05M phosphate buffer) at pH 7.4 is – 1.35. Pregabalin Capsules are administered orally and are supplied as imprinted hard-shell capsules containing 25, 50, 75, 100, 150, 200, 225, and 300 mg of pregabalin, along with pregelatinized starch and talc as inactive ingredients. The capsule shells contain gelatin, titanium dioxide, sodium lauryl sulfate and water. In addition, the orange capsule shells (75 mg, 100 mg, 200 mg, 225 mg and 300 mg strengths) contain red iron oxide. Colloidal silicon dioxide is used as processing aid. The imprinting ink contains shellac, black iron oxide, propylene glycol, potassium hydroxide. Structure