Solid preparations containing tofogliflozin and process of producing the same

Patent metadata

Field	Value
Publication number	US-10231930-B2
Application number	US-201415108335-A
Country	US
Kind code	B2
Filing date	Dec 26, 2014
Priority date	Dec 27, 2013
Publication date	Mar 19, 2019
Grant date	Mar 19, 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 tofogliflogin is present in the form of a 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 the tofogliflozin comprises a crystal form I, a crystal form II, an amorphous form, or a mixture thereof,
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,
wherein a weight ratio of the lubricant ranges from less than 4.0 wt % of the total weight of the composition, and
wherein 85% or more of the tofogliflozin is dissolved into water from the tablet within 15 minutes in the dissolution test at a temperature of 37±2° C. with paddle rotation of 50 rpm.

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 .

9. A solid preparation comprising 20 weight % of tofogliflozin as an active ingredient, 55 weight % of lactose hydrate, 20 weight % of crystalline cellulose, 2 weight % of croscarmellose sodium, and a total of 3 weight % of hydrogenated oil and magnesium stearate, wherein the tofogliflozin is present in the form of a monohydrate crystal.

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

• A61K47/02

  Inorganic compounds · CPC title

• A61K31/7048

  having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin} · CPC title

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title