Poly(meth)acrylic acid popcorn polymerizates as disintegrants for tablets

Patent metadata

Field	Value
Publication number	US-11723871-B2
Application number	US-201917052934-A
Country	US
Kind code	B2
Filing date	May 15, 2019
Priority date	May 16, 2018
Publication date	Aug 15, 2023
Grant date	Aug 15, 2023

Abstract

The use of powder-form, crosslinked, water-insoluble, low-swelling polyacrylates as disintegrants for solid pharmaceutical dosage forms.

First claim

The invention claimed is:

1. A solid pharmaceutical dosage form comprising a disintegrant, wherein the disintegrant is a powder-form water-insoluble, low-swelling crosslinked polyacrylate, and wherein the polyacrylate is a popcorn polymer and has a gel time of greater than 30 seconds.

2. The dosage form according to claim 1 , wherein the polyacrylate comprises structural elements of acrylic acid or methacrylic acid or mixtures thereof.

3. The dosage form according to claim 1 , wherein the polyacrylate contains up to 20% by weight of comonomer structural elements.

4. The dosage form according to claim 1 , wherein the comonomer structural elements comprise a (meth)acrylic ester.

5. The dosage form of claim 4 , wherein the (meth)acrylic ester is selected from the group consisting of methyl acrylate, methyl methacrylate, hydroxyethyl methacrylate, hydroxyethyl acrylate and ethyl acrylate, butyl acrylate, and 2-ethylhexyl acrylate ester.

6. The dosage form according to claim 1 , wherein powder-form polyacrylate has an average particle size within a range from 100 to 200 μm.

7. The dosage form according to claim 1 , wherein the polyacrylate additionally comprises structural elements from a crosslinker.

8. The dosage form according to claim 7 , wherein the crosslinker is at least trifunctional.

9. The dosage form according to claim 8 , wherein the crosslinker is pentaerythritol triallyl ether.

10. The dosage form according to claim 8 , wherein the polyacrylate comprises 0.1% to 15% by weight, based on the amount of acrylic acid or methacrylic acid, of the trifunctional crosslinker.

11. The dosage form of claim 10 , wherein the polyacrylate comprises 0.5% to 10% by weight, based on the amount of acrylic acid or methacrylic acid, of the trifunctional crosslinker.

12. The dosage form of claim 10 , wherein the polyacrylate comprises 1% to 5% by weight, based on the amount of acrylic acid or methacrylic acid, of the trifunctional crosslinker.

13. The dosage form of claim 1 wherein the crosslinked polyacrylate is partially neutralized.

14. A solid pharmaceutical dosage form comprising a disintegrant, wherein the disintegrant is a powder-form, water-insoluble, low-swelling crosslinked polyacrylate consisting of
(a) structural elements selected from the group consisting of acrylic acid, methacrylic acid, and a mixture thereof;
(b) up to 20% by weight of (meth)acrylic ester comonomer structural elements; and
(c) 0.5 to 10% by weight, based on the amount of structural elements (a) of a trifunctional crosslinker;
wherein the polyacrylate is a popcorn polymer and has a gel time of greater than 30 seconds.

15. The dosage form of claim 14 , wherein the (meth)acrylic ester comonomer is selected from the group consisting of methyl acrylate, methyl methacrylate, hydroxyethyl methacrylate, hydroxyethyl acrylate and ethyl acrylate, butyl acrylate, and 2-ethylhexyl acrylate ester.

16. The dosage form of claim 14 wherein the trifunctional crosslinker is pentaerythritol triallyl ether.

Assignees

• Basf Se

Inventors

• Smit Theo
• Karl Matthias
• Guth Felicitas
• Angel Maximilian
• Kolter Karl
• Schmidt Frank
• Blochberger-Claus Maximilian

Classifications

• A61K9/2027 Primary

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

• A61K9/2031

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers · CPC title

• A61K9/2846 Primary

  Poly(meth)acrylates · CPC title

• A61K9/1635

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