Use of octenyl-succinate starches as a binder in wet granulation

Patent metadata

Field	Value
Publication number	US-12502359-B2
Application number	US-202017755758-A
Country	US
Kind code	B2
Filing date	Nov 6, 2020
Priority date	Nov 8, 2019
Publication date	Dec 23, 2025
Grant date	Dec 23, 2025

Abstract

The present invention relates to the use of octenyl succinate starch, in particular sodium octenyl succinate starch as a binder in wet granulation, in particular for pharmaceutical solid dosage form and the granule obtainable by the method thereof.

First claim

The invention claimed is:

1 . A method for preparing granules comprising one or several substances by wet granulation comprising the steps of:
a) wetting powder of substances with a granulation liquid in presence of a binder consisting of partially hydrolyzed waxy octenyl succinate starch having a weight average molecular weight from 10 4 to 10 6 g/mol in order to obtain granules and, b) drying said granules, wherein said partially hydrolyzed waxy octenyl succinate starch is a waxy octenyl succinate that as been partially hydrolyzed with an alpha-amylase.

2 . The method of claim 1 wherein the step a) comprises the steps of:
a1) mixing substance powder with powder of said binder,
a2) wetting said powder mixture of step a1) with a granulation liquid consisting of a solvent.

3 . The method of claim 1 wherein said substances powder in step a) is wetted with a granulation liquid which comprises said binder.

4 . The method of claim 3 wherein said granulation liquid comprising said binder is sprayed onto the substances powder.

5 . The method of claim 3 wherein said granulation liquid comprising said binder has a Brookfield viscosity from 10 to 10 3 mPa·s. as measured at 25° C. using a Brookfield Digital Viscometer DV-I at 100 rpm.

6 . The method according to claim 1 further comprising a step c) of milling the dried granules.

7 . The method according to claim 1 wherein said partially hydrolyzed octenyl succinate starch is a partially hydrolyzed waxy maize octenyl succinate starch.

8 . The method according to claim 1 wherein said partially hydrolyzed octenyl succinate starch content is between 1 and 50% by weight of the total dry weight of said granules.

9 . The method according to claim 1 wherein said substance is a pharmaceutical active agent.

10 . A method for preparing pharmaceutical tablets exhibiting a disintegration time lower than 60 minutes comprising the steps of preparing granules according to claim 1 and a final step of compressing the granules in order to obtain tablets.

11 . A granule comprising one or several substances and a partially hydrolyzed waxy octenyl succinate starch having a weight average molecular weight from 10 4 to 10 6 g/mol, wherein said partially hydrolyzed waxy octenyl succinate starch is a waxy octenyl succinate that has been partially hydrolyzed with an alpha-amylase.

12 . A pharmaceutical tablet exhibiting a disintegration time lower than 60 minutes comprising a granule of claim 11 .

13 . A method of binding a substance powder in a wet granulation process, the method comprising:
providing partially hydrolyzed waxy octenyl succinate starch having a weight average molecular weight comprised between 10 4 and 10 6 g/mol; and using the octenyl starch as a binder in the wet granulation process, wherein said partially hydrolyzed waxy octenyl succinate starch is a waxy octenyl succinate that has been partially hydrolyzed with an alpha-amylase.

14 . The method of claim 1 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 10 4 to 10 5 g/mol.

15 . The method of claim 1 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 10 5 to 10 6 g/mol.

16 . The method of claim 1 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 500,000 g/mol.

17 . The method of claim 1 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 400,000 g/mol.

18 . The method of claim 1 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 300,000 g/mol.

19 . The method of claim 1 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 200,000 g/mol.

20 . The method of claim 1 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight of 150,000 g/mol.

21 . The method of claim 1 , wherein said partially hydrolyzed octenyl succinate starch content is from 1 to 15% by weight of the total dry weight of said granules.

22 . The granule of claim 11 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 10 4 to 10 5 g/mol.

23 . The granule of claim 11 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 10 5 to 10 6 g/mol.

24 . The granule of claim 11 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 500,000 g/mol.

25 . The granule of claim 11 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 400,000 g/mol.

26 . The granule of claim 11 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 300,000 g/mol.

27 . The granule of claim 11 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight of from 100,000 to 200,000 g/mol.

28 . The granule of claim 11 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight of 150,000 g/mol.

29 . The method of claim 13 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 10 4 to 10 5 g/mol.

30 . The method of claim 13 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 10 5 to 10 6 g/mol.

31 . The method of claim 13 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 500,000 g/mol.

32 . The method of claim 13 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 400,000 g/mol.

33 . The method of claim 13 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 300,000 g/mol.

34 . The method of claim 13 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight from 100,000 to 200,000 g/mol.

35 . The method of claim 13 , wherein the partially hydrolyzed waxy octenyl succinate starch has a weight average molecular weight of 150,000 g/mol.

Assignees

• Roquette Freres

Inventors

• Lefevre Philippe
• Haeusler Olaf
• Descamps Nicolas
• Le Bihan Gregory

Classifications

• A61K9/2059

  Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin · CPC title

• A61K9/1694

  resulting in granules or microspheres of the matrix type containing more than 5% of excipient · CPC title

• A61K9/2095 Primary

  Tabletting processes · CPC title

• C08L3/06 Primary

  Esters · CPC title