Pharmaceutical composition for oral administration

Patent metadata

Field	Value
Publication number	US-2021346392-A1
Application number	US-201917272028-A
Country	US
Kind code	A1
Filing date	Aug 30, 2019
Priority date	Aug 31, 2018
Publication date	Nov 11, 2021
Grant date	—

Abstract

In a pharmaceutical composition for oral administration comprising 6-(4,4-dimethylcyclohexyl)-4-[(1,1-dioxo-1λ 6 -thiomorpholin-4- yl )methyl]-2-methylthieno[2,3- d ]pyrimidine or a pharmaceutically acceptable salt thereof, a stable pharmaceutical composition for oral administration with rapid drug dissolution properties is provided. The pharmaceutical composition for oral administration contains a water-swellable substance, which is a polymer compound obtained by condensation polymerization of β-glucose, a polymer compound obtained by condensation polymerization of α-glucose, or a polymer compound having a pyrrolidone functional group.

First claim

1 . A pharmaceutical composition for oral administration comprising 6-(4,4-dimethylcyclohexyl)-4-[(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)methyl]-2-methylthieno[2,3-d]pyrimidine or a pharmaceutically acceptable salt thereof, and a water-swellable substance, wherein said water-swellable substance is one, or two or more members selected from the group consisting of a polymer compound obtained by condensation polymerization of β-glucose, a polymer compound obtained by condensation polymerization of α-glucose, and a polymer compound having a pyrrolidone functional group.

2 . The pharmaceutical composition for oral administration according to claim 1 , wherein said water-swellable substance is one or more members selected from the group consisting of:
i) carmellose, carmellose calcium, croscarmellose sodium, and low substituted hydroxypropylcellulose, which are the polymer compounds obtained by condensation polymerization of β-glucose,
ii) corn starch, potato starch, rice starch, partially pregelatinized starch, and pregelatinized starch, which are the polymer compounds obtained by condensation polymerization of α-glucose, and
iii) crospovidone, which is the polymer compound having a pyrrolidone functional group.

3 . The pharmaceutical composition for oral administration according to claim 2 , wherein said water-swellable substance is a polymer compound obtained by condensation polymerization of β-glucose, and said polymer compound obtained by condensation polymerization of β-glucose is one or more members selected from the group consisting of carmellose, carmellose calcium, croscarmellose sodium, and low substituted hydroxypropylcellulose.

4 . The pharmaceutical composition for oral administration according to claim 3 , wherein said polymer compound obtained by condensation polymerization of β-glucose is low substituted hydroxypropylcellulose.

5 . The pharmaceutical composition for oral administration according to claim 2 , wherein said water-swellable substance is a polymer compound obtained by condensation polymerization of α-glucose, and said polymer compound obtained by condensation polymerization of α-glucose is one or more members selected from the group consisting of corn starch, potato starch, rice starch, partially pregelatinized starch, and pregelatinized starch.

6 . The pharmaceutical composition for oral administration according to claim 2 , wherein said water-swellable substance is a polymer compound having a pyrrolidone functional group, and said polymer compound having a pyrrolidone functional group is crospovidone.

7 . The pharmaceutical composition for oral administration according to claim 2 , wherein said water-swellable substance is one or more members selected from the group consisting of low substituted hydroxypropylcellulose, corn starch, and crospovidone.

8 . The pharmaceutical composition for oral administration according to claim 1 , wherein said water-swellable substance is present in an amount of 20% by weight to 6000% by weight with respect to the weight of said 6-(4,4-dimethylcyclohexyl)-4-[(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)methyl]-2-methylthieno[2,3-d]pyrimidine or pharmaceutically acceptable salt thereof.

9 . The pharmaceutical composition for oral administration according to claim 1 , which is in the form of a tablet, a capsule, a granule, or a powder.

10 . A method of manufacturing a stable pharmaceutical composition for oral administration comprising 6-(4,4-dimethylcyclohexyl)-4-[(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)methyl]-2-methylthieno[2,3-d]pyrimidine or a pharmaceutically acceptable salt thereof, said method comprising formulating said 6-(4,4-dimethylcyclohexyl)-4-[(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)methyl]-2-methylthieno[2,3-d]pyrimidine or pharmaceutically acceptable salt thereof with a water-swellable substance which is one or more members selected from the group consisting of low substituted hydroxypropylcellulose, corn starch, and crospovidone.

Assignees

• Astellas Pharma Inc

Inventors

• Kojima Ryo
• Sakai Toshiro
• Azuma Ryota
• Tanaka Marina

Classifications

• A61K31/541 Primary

  Non-condensed thiazines containing further heterocyclic rings · CPC title

• A61P21/02

  Muscle relaxants, e.g. for tetanus or cramps · CPC title

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61K9/2095

  Tabletting processes · CPC title