Extended Release Pharmaceutical Composition Of Entacapone Or Salts Thereof

Abstract

There is provided an extended release pharmaceutical composition comprising from about 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also provides an extended release pharmaceutical composition comprising triple combination of from about 30 mg to about 300 mg of levodopa, 10 mg to about 100 mg of carbidopa and 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.

1 - 18 . (canceled) 
     
     
         19 . An extended release pharmaceutical composition comprising from about 200 mg to about 1000 mg of entacapone or salts thereof, the entacapone being coated by or embedded in matrix with one or more hydrophilic or hydrophobic polymers for achieving extended release along with other pharmaceutically acceptable excipients. 
     
     
         20 . The pharmaceutical composition of  claim 19 , wherein the composition comprises one or more of tablet, bilayered tablet, trilayered tablet, capsule, powder, disc, caplet, granules, pellets, granules in capsule, minitablets, minitablets in capsule, pellets in capsule or sachet. 
     
     
         21 . The pharmaceutical composition of  claim 19 , wherein the one or more hydrophilic or hydrophobic polymers are selected from the group consisting of polyvinyl acetate, cellulose acetate, cellulose acetate butyrate, cellulose acetate propionate, ethyl cellulose, a fatty acid, a fatty acid ester, an alkyl alcohol, a wax, shellac, rosin, zein (prolamine from corn), povidone, kollidon SR, a polymethacrylate, microcrystalline cellulose or polyethylene oxide, polyuronic acid salts, cellulose ethers, xanthan gum, tragacanth gum, gum karaya, guar gum, acacia, gellan gum locust bean gum, alkali metal salts of alginic acid or pectic acid, sodium alginate, potassium alginate, ammonium alginate, hydroxypropyl cellulose, hydroxy ethyl cellulose, hydroxypropyl methyl cellulose, carboxyvinyl polymers, polymerized gelatin, shellac, methacrylic acid copolymer type C NF, cellulose butyrate phthalate, cellulose hydrogen phthalate, cellulose propionate phthalate, polyvinyl acetate phthalate (PVAP), cellulose acetate phthalate (CAP), cellulose acetate trimellitate (CAT), hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate, dioxypropyl methylcellulose succinate, carboxymethyl ethyl cellulose (CMEC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), acrylic acid polymers and copolymers, methyl acrylate, ethyl acrylate, methyl methacrylate and/or ethyl methacrylate with copolymers of acrylic and methacrylic acid esters, Eudragit NE, Eudragit RL and Eudragit RS. 
     
     
         22 . The pharmaceutical composition of  claim 19 , wherein one tablet of said composition exhibits no significant difference in rate and/or extent of absorption of entacapone as compared to 2 tablets of 200 mg immediate release entacapone commercially marketed as Comtan® administered at the interval of 3-4 hours. 
     
     
         23 . A method of treating Parkinson's disease in a mammal, comprising administering to a mammal in need thereof, a pharmaceutical composition of  claim 19 . 
     
     
         24 . A method of reducing “wearing off” phenomena in Parkinson's patients, comprising administering to a mammal in need thereof, a pharmaceutical composition of  claim 19 . 
     
     
         25 . A process for preparing an extended release pharmaceutical composition comprising from about 200 mg to about 1000 mg of entacapone or salts thereof, the entacapone being coated by or embedded in matrix with one or more hydrophilic or hydrophobic polymers for achieving extended release along with other pharmaceutically acceptable excipients, wherein the said process comprises of coating or mixing entacapone with one or more pharmaceutically acceptable polymers, optionally mixing with other pharmaceutical excipients and converting the mixture into suitable dosage form. 
     
     
         26 . The pharmaceutical composition of  claim 19 , wherein the said composition is extended release which exhibits a dissolution profile such that within 60 minutes at least 15% of entacapone is released, wherein the release rate is measured in Apparatus 2 (USP, Dissolution, paddle, 75 rpm) using 1000 ml of pH 5.5 phosphate buffer at 37° C.±0.5° C. 
     
     
         27 . The pharmaceutical composition of  claim 19 , wherein the said composition is extended release which exhibits a dissolution profile such that within 4 hrs at least 60% of entacapone is released, wherein the release rate is measured in Apparatus 2 (USP, Dissolution, paddle, 75 rpm) using 1000 ml of pH 5.5 phosphate buffer at 37° C.±0.5° C. 
     
     
         28 . The pharmaceutical composition of  claim 19 , further comprising from about 30 mg to about 300 mg of levodopa, and 10 mg to about 100 mg of carbidopa or salts thereof. 
     
     
         29 . The pharmaceutical composition of  claim 28 , wherein the composition comprises one or more of tablet, bilayered tablet, trilayered tablet, capsule, powder, disc, caplet, granules, pellets, granules in capsule, minitablets, minitablets in capsule, pellets in capsule or sachet. 
     
     
         30 . The pharmaceutical composition of  claim 28 , wherein one tablet of said composition exhibits no significant difference in rate and/or extent of absorption of entacapone, levodopa and carbidopa as compared to 2-4 tablets of 200 mg immediate release entacapone, levodopa and carbidopa formulation commercially marketed as Stalevo® administered at the interval of 3-4 hours. 
     
     
         31 . A method of treating Parkinson's disease in a mammal, comprising administering to a mammal in need thereof, a pharmaceutical composition of  claim 28 . 
     
     
         32 . A method of reducing “wearing off” phenomena in Parkinson's patients, comprising administering to a mammal in need thereof, a pharmaceutical composition of  claim 28 . 
     
     
         33 . A process for preparing an extended release pharmaceutical composition from about 30 mg to about 300 mg of levodopa, 10 mg to about 100 mg of carbidopa and 200 mg to about 1000 mg of entacapone or salts thereof, wherein the said process comprises of coating or mixing levodopa, carbidopa and entacapone with one or more pharmaceutically acceptable polymers, optionally mixing with other pharmaceutical excipients and converting the mixture into suitable dosage form. 
     
     
         34 . The pharmaceutical composition of  claim 28 , wherein said composition is extended release which exhibits a dissolution profile such that within 60 minutes at least 15% of entacapone or at least 15% of levodopa or at least 15% of carbidopa is released, wherein the release rate is measured in Apparatus 2 (USP, Dissolution, paddle, 75 rpm) using 1000 ml of pH 5.5 phosphate buffer at 37° C.±0.5° C. 
     
     
         35 . The pharmaceutical composition of  claim 28 , wherein said composition is extended release which exhibits a dissolution profile such that within 4 hrs at least 60% of entacapone or at least 60% of levodopa or at least 60% of carbidopa is released, wherein the release rate is measured in Apparatus 2 (USP, Dissolution, paddle, 75 rpm) using 1000 ml of pH 5.5 phosphate buffer at 37° C.±0.5° C.