Claims for Patent: 10,898,444

Summary for Patent: 10,898,444

Title:	Extended release multiparticulates of ranolazine
Abstract:	The present invention relates to an extended release multiparticulate composition comprising a plurality of discrete units, each discrete unit comprising ranolazine or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients. The said multiparticulate composition is sprinkled onto soft foods or liquids for oral administration. Further, the multiparticulate composition is bioequivalent to the marketed extended release tablet. It further relates to a process of preparation of said multiparticulate composition and method of treatment of patients suffering from angina by administering said composition.
Inventor(s):	Singh; Harinder (Kangra, IN), Ahmad; Shavej (Uttar Pradesh, IN), Singh; Romi B. (Benares, IN)
Assignee:	Sun Pharmaceutical Industries Limited (Mumbai, IN)
Application Number:	15/879,246
Patent Claims:	1. An extended release multiparticulate composition comprising a plurality of discrete units, each discrete unit comprising: a) a drug layered core comprising an inert core and a drug layer, wherein the drug layer comprises ranolazine and one or more pharmaceutically acceptable excipients; b) an extended release coating over the drug layered core, wherein the extended release coating comprises a mixture of a water-insoluble polymer and a pH-dependent polymer, wherein said water-insoluble polymer and pH-dependent polymer are present in a weight ratio of from about 1:2 to about 1:3; wherein said multiparticulate composition releases: about 15% to about 40% of the ranolazine in an initial 2 hours in 900 mL 0.1N HCl and releases about 60% to about 90% of the ranolazine in 6 hours in 900 mL pH 6.8 phosphate buffer; when measured in United States Pharmacopoeia (USP) type II dissolution apparatus, rotated at 50 rpm at a temperature of 37.degree. C.; wherein the composition is filled into a capsule or a sachet and the composition comprises about 1000 mg of ranolazine and wherein ranolazine is present in an amount of about 40% to about 85% by weight of the multiparticulate composition. 2. The extended release multiparticulate composition of claim 1, wherein said discrete units are in a form selected from the group consisting of pellets, granules, minitablets and beads. 3. The extended release multiparticulate composition of claim 1, wherein said discrete units further comprise a top coat. 4. The extended release multiparticulate composition of claim 1, wherein said water-insoluble polymer is selected from the group consisting of cellulose ethers, cellulose esters, polymethacrylic acid ester copolymers, aminoalkyl methacrylate copolymers, a copolymer of polyvinyl acetate and polyvinylpyrrolidone, and mixtures thereof. 5. The extended release multiparticulate composition of claim 1, wherein said pH-dependent polymer is selected from the group consisting of methyl acrylate acrylic acid copolymer, methyl acrylate methacrylic acid copolymer, butyl acrylate styrene acrylic acid copolymer, methacrylic acid methyl methacrylate copolymer, methacrylic acid ethyl acrylate copolymer methyl acrylate methacrylic acid octyl acrylate copolymer; hydroxypropylmethylcellulose acetate succinate, hydroxypropylmethylcellulose phthalate, hydroxymethylethylcellulose phthalate, cellulose acetate phthalate, cellulose acetate succinate, cellulose acetate maleate, cellulose acetate trimelliate cellulose benzoate phthalate, cellulose propionate phthalate, methylcellulose phthalate, carboxymethylethylcellulose, ethylhydroxyethylcellulose phthalate, polyvinyl alcohol phthalate, polyvinylacetal phthalate, polyvinyl butylate phthalate, polyvinylacetoacetal phthalate, maleic acid copolymers and mixtures thereof. 6. The extended release multiparticulate composition of claim 1, wherein said water-insoluble polymer is cellulose ether and wherein said pH dependent polymer is methacrylic acid copolymer. 7. The extended release multiparticulate composition of claim 1, wherein said extended release coating layer further comprises a plasticizer selected from the group consisting of acetyl tributyl citrate, acetyl triethyl citrate, dibutyl sebacate, diethyl phthalate, castor oil, diacetylated monoglycerides, triacetin, tributyl citrate, triethyl citrate and mixtures thereof. 8. The extended release multiparticulate composition of claim 1, wherein the drug layer comprises about 50% to about 70% of ranolazine by total weight of the multiparticulate composition. 9. The extended release multiparticulate composition of claim 1, wherein the drug layer comprises about 60% to about 80% of ranolazine.