Solid preparations containing tofogliflozin and process of producing the same

Patent metadata

Field	Value
Publication number	US-10398653-B2
Application number	US-201916260530-A
Country	US
Kind code	B2
Filing date	Jan 29, 2019
Priority date	Dec 27, 2013
Publication date	Sep 3, 2019
Grant date	Sep 3, 2019

Abstract

The present invention provides a method for producing a pharmaceutical composition which is a tablet and which contains tofogliflozin as an active ingredient. The method comprises mixing an additive and tofogliflozin to prepare a powder mixture and obtaining a tablet from the powder mixture by direct compression. The additive comprises at least one filler.

First claim

The invention claimed is:

1. A method for producing a pharmaceutical composition which is a tablet comprising tofogliflozin as an active ingredient, wherein the tofogliflozin is present in a form of monohydrate crystal, wherein the method comprises:
mixing an additive and tofogliflozin to prepare a powder mixture, and
obtaining a tablet from the powder mixture by direct compression,
wherein the additive comprises at least one filler, and at least one lubricant,
wherein the composition is substantially free from calcium silicate,
wherein a weight ratio of the active ingredient tofogliflozin ranges from 2.5 to 40 wt % with respect to the total weight of the composition, and
wherein a weight ratio of the lubricant ranges from less than 4.0 wt % of the total weight of the composition.

2. The method of claim 1 , wherein the filler is selected from the group consisting of corn starch, potato starch, wheat starch, rice starch, partial alpha starch, alpha starch, lactose hydrate, fructose, glucose, mannitol, anhydrous dibasic calcium phosphate, crystalline cellulose, and precipitate calcium carbonate.

3. The method of claim 1 , wherein the additive further comprises at least one disintegrant.

4. The method of claim 3 , wherein the disintegrant is selected from the group consisting of sodium starch glycolate, carboxymethyl cellulose, carboxymethylcellulose calcium, carboxymethyl starch sodium, croscarmellose sodium, crospovidone, low substituted hydroxypropylcellulose, and hydroxypropyl starch.

5. The method of claim 1 , wherein the lubricant is selected from the group consisting of magnesium stearate, calcium stearate, talc, sucrose fatty acid ester, sodium stearyl fumarate, and hydrogenated oil.

6. The method of claim 3 , wherein a weight ratio of the filler ranges from 20 to 80 wt % of the total weight of the composition and a weight ratio of the disintegrant ranges from 1.0 to 4.0 wt % of the total weight of the composition.

7. The method of claim 1 , wherein the additive comprises lactose hydrate, crystalline cellulose, croscarmellose sodium, and hydrogenated oil and/or magnesium stearate.

8. A pharmaceutical composition which is a tablet produced by the method of claim 1 .

Assignees

• Chugai Pharmaceutical Co Ltd

Inventors

• Wada Kenta
• Hirayama Tomoaki
• Sakai Kenichi
• Yoshimura Shiho

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K47/36

  Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin · CPC title

• A61K47/32

  Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} · CPC title