Immediate release abuse-deterrent granulated dosage forms

Patent metadata

Field	Value
Publication number	US-11207318-B2
Application number	US-202016751043-A
Country	US
Kind code	B2
Filing date	Jan 23, 2020
Priority date	Oct 31, 2013
Publication date	Dec 28, 2021
Grant date	Dec 28, 2021

Abstract

Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses.

First claim

What is claimed:

1. An abuse deterrent, compressed, orally ingestible tablet comprising:
more than one gelling polymer,
a disintegrant, and
an active pharmaceutical ingredient (API) selected from the group consisting of esketamine and pharmaceutically acceptable salts thereof;
wherein at least one of the gelling polymers in present within a matrix;
wherein said tablet provides for an immediate release profile having not less than 90% of API released in 60 minutes, as evaluated by dissolution of the tablet in 300 mL of 0.1 HCl media using USP II apparatus at 50 RPM paddle speed and 37° C.; and
wherein the abuse deterrence comprises reducing the risk of one or more types of abuse selected from:
a) abuse by injection,
b) abuse by nasal insufflation, and
c) abuse by consumption of a supratherapeutic dose or
d) combinations of the above.

2. The tablet according to claim 1 , wherein the gelling polymers are independently selected from the group consisting of a natural starch, a synthetic starch, a natural cellulose, a synthetic cellulose, an acrylate, a polyalkylene oxide, a carbomer and combinations thereof.

3. The tablet according to claim 1 , wherein the gelling polymers are independently selected from the group consisting of polyethylene oxide, polyvinyl alcohol, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, methyl cellulose, hydroxyethylmethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, polyacrylic acid and polyvinyl carboxy polymers, carbomer polymers and combinations thereof.

4. The tablet according to claim 3 , wherein the gelling polymers comprise hydroxypropyl methyl cellulose (HPMC) and a carbomer.

5. The tablet according to claim 1 , wherein the gelling polymer present within a matrix comprises a carbomer.

6. The tablet according to claim 1 , wherein the gelling polymer present within a matrix comprises polyethylene oxide.

7. The tablet according to claim 1 , wherein the total amount of gelling polymers is about 0.7 to about 20 weight percent gelling polymer based on total weight of the tablet.

8. The tablet according to claim 7 , wherein the total amount of gelling polymers is about 2 to about 15 weight percent gelling polymer based on total weight of the tablet.

9. The tablet according to claim 1 , wherein the gelling polymer present within a matrix is present in an amount from 0.5 to 15 weight percent based on the total weight of the tablet.

10. The tablet according to claim 1 comprising esketamine, wherein the esketamine is present in a total amount of about 1 mg to 400 mg.

11. The tablet according to claim 10 , wherein the esketamine is present in a total amount of about 1 mg to about 100 mg.

12. The tablet according to claim 10 , wherein the esketamine is present in a total amount of about 1 mg to about 56 mg.

13. The tablet according to claim 1 , wherein the API is esketamine and the gelling polymers are HPMC and a carbomer.

14. A method of treating a subject in need thereof comprising orally administering to the subject the tablet according to claim 1 .

Assignees

• Clexio Biosciences Ltd

Inventors

• Haswani Dinesh K
• Moe Derek V
• O'Neill Victoria A
• Vega Zepeda Manuel A

Classifications

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• A61K9/2018

  Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates · CPC title

• A61K31/4458

  only substituted in position 2, e.g. methylphenidate · CPC title

• A61K31/485 Primary

  Morphinan derivatives, e.g. morphine, codeine · CPC title

• A61K9/2009

  Inorganic compounds · CPC title