Pharmaceutical composition and method of manufacturing the same

Patent metadata

Field	Value
Publication number	US-2019343795-A1
Application number	US-201716474393-A
Country	US
Kind code	A1
Filing date	Dec 28, 2017
Priority date	Dec 28, 2016
Publication date	Nov 14, 2019
Grant date	—

Abstract

An object of the present invention is to provide a pharmaceutical composition comprising 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof at a high concentration, with a characteristic bitter taste masked, and a manufacturing method thereof. The present invention provides a pharmaceutical composition comprising fine granules having a core comprising 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof, and a binder; and a polymer layer with which a surface of the core is coated, wherein the fine granules have a roundness of 0.8 or more and a content of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt thereof in the fine granules is 30 to 90% by mass.

First claim

1 - 9 . (canceled)

10 . A pharmaceutical composition comprising fine granules having a core comprising 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof, and a binder; and a polymer layer with which a surface of the core is coated, wherein the fine granules have a roundness of 0.8 or more and a content of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt thereof in the fine granules is 30 to 90% by mass.

11 . The pharmaceutical composition according to claim 10 , wherein the content of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt thereof in the fine granules is 50 to 90% by mass.

12 . The pharmaceutical composition according to claim 10 , wherein the binder is one or more selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, carmellose sodium, gum arabic, pregelatinized starch, polyvinyl alcohol, and polyvinyl alcohol/polyethylene glycol graft polymer.

13 . The pharmaceutical composition according to claim 10 , wherein the binder is hydroxypropyl cellulose.

14 . The pharmaceutical composition according to claim 10 , wherein the polymer layer comprises at least one selected from the group consisting of ammonioalkyl methacrylate copolymer, methacrylic acid copolymer, ethyl cellulose, and ethyl acrylate/methyl methacrylate copolymer.

15 . The pharmaceutical composition according to claim 10 , further comprising an overcoat layer with which a surface of the polymer layer is coated.

16 . The pharmaceutical composition according to claim 10 , wherein the composition is a fine granule or a tablet.

17 . The pharmaceutical composition according to claim 10 , wherein the composition is an orally disintegrating tablet.

18 . A method of manufacturing the pharmaceutical composition according to claim 10 , the method comprising: a step of manufacturing a core comprising 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof, and a binder by a wet agitation granulation method using 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt thereof and the binder; and a step of forming a polymer layer on a surface of the core.

Assignees

• Fujifilm Toyama Chemical Co Ltd

Inventors

• Okada Kotaro
• Sakata Yoshinori
• Tsujihata Shigetomo

Classifications

• A61K9/16

  Agglomerates; Granulates; Microbeadlets {; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction (A61K9/20 takes precedence if the final form is a tablet; microspheres with drug-free outer coating, microcapsules A61K9/50; mixture of different granules, microcapsules, (coated) microparticles A61K9/5084; nanoparticles A61K9/51)} · CPC title

• A61K9/1652 Primary

  Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623) · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K31/397 Primary

  having four-membered rings, e.g. azetidine · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title