US2016184275A2PendingUtilityA2

Pharmaceutical composition for modified use

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Assignee: TAKAISHI YUUKIPriority: Sep 30, 2008Filed: Sep 28, 2009Published: Jun 30, 2016
Est. expirySep 30, 2028(~2.2 yrs left)· nominal 20-yr term from priority
Inventors:Yuuki TakaishiYutaka TakahashiTakashi NishizatoDaisuke MurayamaEmiko MurayamaSoichiro NakamuraKazuhiro Sako
A61K 31/426A61K 47/32A61K 9/2031A61K 9/2853A61K 9/2866A61P 13/08A61P 13/10A61P 3/04A61P 3/06A61P 3/08A61P 3/10A61K 47/34A61K 47/38A61K 9/06A61K 9/2009A61K 9/2013A61K 9/2054A61K 9/2095
69
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Claims

Abstract

A pharmaceutical composition for modified release, comprising (1) (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof, (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 10 mL or less, and (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 or more, or a viscosity of 12 mPa·s or more at a 5% aqueous solution at 25° C. is disclosed.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical composition for modified release, comprising
 (1) 10 mg to 200 mg of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof,   (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 10 mL or less, and   (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 to 5,000,000, or a viscosity of 12 mPa·s at a 5% aqueous solution at 25° C. to 7500 mPa·s at a 1% aqueous solution at 25° C.,   wherein the hydrogel-forming polymer is present in an amount of 1% by weight to 40% by weight with respect to the total weight of the pharmaceutical composition; and   wherein a drug dissolution rate from the pharmaceutical composition is 75% or less after 1.5 hours, and 75% or more to 100% or less after 7 hours from the beginning of a dissolution test.   
     
     
         2 . The pharmaceutical composition for modified release according to  claim 1 , wherein the additive which ensures penetration of water into the pharmaceutical composition is one compound, or two or more compounds selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, D-mannitol, D-sorbitol, xylitol, lactose, sucrose, anhydrous maltose, D-fructose, dextran, glucose, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene glycol, polyoxyethylene sorbitan higher fatty acid ester, sodium chloride, magnesium chloride, citric acid, tartaric acid, glycine, β-alanine, lysine hydrochloride, and meglumine. 
     
     
         3 . The pharmaceutical composition for modified release according to  claim 2 , wherein the additive which ensures penetration of water into the pharmaceutical composition is one compound, or two or more compounds selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, D-mannitol, lactose, sucrose, sodium chloride, and polyoxyethylene polyoxypropylene glycol. 
     
     
         4 . The pharmaceutical composition for modified release according to  claim 1 , wherein an amount of the additive which ensures penetration of water into the pharmaceutical composition is 5% by weight to 75% by weight with respect to the total weight of the pharmaceutical composition. 
     
     
         5 . The pharmaceutical composition for modified release according to  claim 4 , wherein an amount of the additive which ensures penetration of water into the pharmaceutical composition is 5% by weight to 70% by weight with respect to the total weight of the pharmaceutical composition. 
     
     
         6 . The pharmaceutical composition for modified release according to  claim 1 , wherein the hydrogel-forming polymer is one compound, or two or more compounds selected from the group consisting of polyethylene oxide, hydoxypropyl methylcellulose, hydroxypropyl cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, and a carboxyvinyl polymer. 
     
     
         7 . The pharmaceutical composition for modified release according to  claim 6 , wherein the hydrogel-forming polymer is one compound, or two or more compounds selected from the group consisting of polyethylene oxide, hydoxypropyl methylcellulose, and hydroxypropyl cellulose. 
     
     
         8 . (canceled) 
     
     
         9 . The pharmaceutical composition for modified release according to  claim 1 , further comprising an antioxidant. 
     
     
         10 . The pharmaceutical composition for modified release according to  claim 9 , wherein the antioxidant is one compound, or two or more compounds selected from the group consisting of butyl hydroxytoluene, propyl gallate, and sodium ascorbate. 
     
     
         11 . The pharmaceutical composition for modified release according to  claim 10 , wherein the antioxidant is butyl hydroxytoluene. 
     
     
         12 . The pharmaceutical composition for modified release according to  claim 9 , wherein an amount of the antioxidant is 0.025% by weight to 0.25% by weight. 
     
     
         13 . The pharmaceutical composition for modified release according to  claim 1 , further comprising a stabilizer. 
     
     
         14 . The pharmaceutical composition for modified release according to  claim 13 , wherein the stabilizer is one compound, or two or more compounds selected from the group consisting of yellow ferric oxide, red ferric oxide, and black iron oxide. 
     
     
         15 . The pharmaceutical composition for modified release according to  claim 14 , wherein the stabilizer is yellow ferric oxide and/or red ferric oxide. 
     
     
         16 . The pharmaceutical composition for modified release according to  claim 13 , wherein an amount of the stabilizer is 0.05% by weight to 1% by weight. 
     
     
         17 . A process of manufacturing a pharmaceutical composition for modified release, characterized by comprising mixing (1) (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof with (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 10 mL or less and (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 or more, or a viscosity of 12 mPa·s or more at a 5% aqueous solution at 25° C., wherein an amount of the additive is 5% by weight to 75% by weight with respect to the total weight of the pharmaceutical composition, and an amount of the hydrogel-forming polymer is 1% by weight to 40% by weight with respect to the total weight of the pharmaceutical composition. 
     
     
         18 . The process according to  claim 17 ,
 wherein the additive which ensures penetration of water into the pharmaceutical composition is one compound, or two or more compounds selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, D-mannitol, D-sorbitol, xylitol, lactose, sucrose, anhydrous maltose, D-fructose, dextran, glucose, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene glycol, polyoxyethylene sorbitan higher fatty acid ester, sodium chloride, magnesium chloride, citric acid, tartaric acid, glycine, β-alanine, lysine hydrochloride, and meglumine.   
     
     
         19 . The process according to  claim 17 , wherein the hydrogel-forming polymer is one compound, or two or more compounds selected from the group consisting of polyethylene oxide, hydoxypropyl methylcellulose, hydroxypropyl cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, and a carboxyvinyl polymer. 
     
     
         20 . The pharmaceutical composition for modified release according to  claim 1 , wherein a drug dissolution rate from the pharmaceutical composition is 92%, 93% or 95% after 4.5 hours from the beginning of a dissolution test. 
     
     
         21 . The pharmaceutical composition for modified release according to  claim 1 , wherein the average molecular weight of the hydrogel-forming polymer is 100,000 to 2,000,000. 
     
     
         22 . A method of reducing an effect of food intake, comprising the step of administering a pharmaceutical composition comprising a drug, which is a pharmaceutical composition for modified release, comprising
 (1) 10 mg to 200 mg of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof,   (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 10 mL or less, and   (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 to 5,000,000, or a viscosity of 12 mPa·s at a 5% aqueous solution at 25° C. to 7500 mPa·s at a 1% aqueous solution at 25° C.,   wherein the hydrogel-forming polymer is present in an amount of 1% by weight to 40% by weight with respect to the total weight of the pharmaceutical composition; and   wherein a drug dissolution rate from the pharmaceutical composition is 75% or less after 1.5 hours, and 75% or more to 100% or less after 7 hours from the beginning of a dissolution test.   
     
     
         23 . The method according to  claim 22 , wherein the additive which ensures penetration of water into the pharmaceutical composition is one compound, or two or more compounds selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, D-mannitol, D-sorbitol, xylitol, lactose, sucrose, anhydrous maltose, D-fructose, dextran, glucose, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene glycol, polyoxyethylene sorbitan higher fatty acid ester, sodium chloride, magnesium chloride, citric acid, tartaric acid, glycine, β-alanine, lysine hydrochloride, and meglumine. 
     
     
         24 . The method according to  claim 23 , wherein the additive which ensures penetration of water into the pharmaceutical composition is one compound, or two or more compounds selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, D-mannitol, lactose, sucrose, sodium chloride, and polyoxyethylene polyoxypropylene glycol. 
     
     
         25 . The method according to  claim 22 , wherein an amount of the additive which ensures penetration of water into the pharmaceutical composition is 5% by weight to 75% by weight with respect to the total weight of the pharmaceutical composition. 
     
     
         26 . The pharmaceutical composition for modified release according to  claim 25 , wherein an amount of the additive which ensures penetration of water into the pharmaceutical composition is 5% by weight to 70% by weight with respect to the total weight of the pharmaceutical composition. 
     
     
         27 . The method according to  claim 22 , wherein the hydrogel-forming polymer is one compound, or two or more compounds selected from the group consisting of polyethylene oxide, hydoxypropyl methylcellulose, hydroxypropyl cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, and a carboxyvinyl polymer. 
     
     
         28 . The method according to  claim 27 , wherein the hydrogel-forming polymer is one compound, or two or more compounds selected from the group consisting of polyethylene oxide, hydoxypropyl methylcellulose, and hydroxypropyl cellulose. 
     
     
         29 . The pharmaceutical composition for modified release according to  claim 22 , further comprising an antioxidant. 
     
     
         30 . The method according to  claim 29 , wherein the antioxidant is one compound, or two or more compounds selected from the group consisting of butyl hydroxytoluene, propyl gallate, and sodium ascorbate. 
     
     
         31 . The method according to  claim 30 , wherein the antioxidant is butyl hydroxytoluene. 
     
     
         32 . The method according to  claim 29 , wherein an amount of the antioxidant is 0.025% by weight to 0.25% by weight. 
     
     
         33 . The method according to  claim 22 , further comprising a stabilizer. 
     
     
         34 . The method according to  claim 33 , wherein the stabilizer is one compound, or two or more compounds selected from the group consisting of yellow ferric oxide, red ferric oxide, and black iron oxide. 
     
     
         35 . The method according to  claim 34 , wherein the stabilizer is yellow ferric oxide and/or red ferric oxide. 
     
     
         36 . The method according to  claim 33 , wherein an amount of the stabilizer is 0.05% by weight to 1% by weight. 
     
     
         37 . The method according to  claim 22 , wherein a drug dissolution rate from the pharmaceutical composition is 92%, 93% or 95% after 4.5 hours from the beginning of a dissolution test. 
     
     
         38 . The method according to  claim 22 , wherein the average molecular weight of the hydrogel-forming polymer is 100,000 to 2,000,000.

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