Immediate release abuse-deterrent granulated dosage forms

Patent metadata

Field	Value
Publication number	US-11534409-B2
Application number	US-202117559158-A
Country	US
Kind code	B2
Filing date	Dec 22, 2021
Priority date	Dec 8, 2014
Publication date	Dec 27, 2022
Grant date	Dec 27, 2022

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. A method of treating depression comprising orally administering to a subject in need thereof a therapeutically effective amount of a compressed tablet comprising between 10 and 25 wt % of ketamine, esketamine, or a pharmaceutically acceptable salt thereof;
wherein the tablet comprises a core comprising from 40 to 85 wt % of a first polymer of average molecular weight of at least 10,000 and selected from the group consisting of polyethylene oxide, polyvinyl alcohol, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, methyl cellulose, hydroxyethylmethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, polyacrylic acid, polyvinyl carboxy polymers, carbomer polymers and combinations thereof; and
wherein the core is coated by a second polymer having an average molecular weight of less than 50,000 and in an amount of about 2-30 wt % with respect to the total weight of the tablet, that is selected from the group consisting of hydroxypropyl cellulose, poly(methyl methacrylates), ethyl cellulose, hydroxypropyl methyl cellulose, hydroxyl methyl cellulose, polyvinyl alcohol, and any combination thereof.

2. The method of claim 1 , wherein the first polymer comprises polyethylene oxide of average molecular weight between 100,000 and 7,000,000, hydroxypropyl methyl cellulose of average molecular weight between 10,000 and 1,500,000, hydroxypropyl cellulose of average molecular weight between 40,000 and 1,150,000, sodium carboxymethylcellulose of average molecular weight between 49,000 and 725,000, hydroxyethylcellulose of average molecular weight between 90,000 and 1,300,000, polyacrylic acid of average molecular weight between 80,000 and 200,000 or carbomer polymers of average molecular weight between 700,000 and 3,000,000,000.

3. The method of claim 2 , wherein the first polymer comprises hydroxypropyl methyl cellulose of average molecular weight between 10,000 and 1,500,000.

4. The method of claim 3 , wherein the first polymer comprises hydroxypropyl methyl cellulose of average molecular weight between 20,000 and 746,000.

5. The method of claim 3 , wherein the first polymer comprises hydroxypropyl methyl cellulose of average molecular weight between 164,000 and 1,200,000.

6. The method of claim 2 , wherein the first polymer comprises polyethylene oxide of average molecular weight between 100,000 and 7,000,000.

7. The method of claim 2 , wherein the first polymer comprises polyvinyl carboxy polymers of average molecular weight between 700,000 and 3,000,000,000.

8. The method of claim 1 , wherein the first polymer comprises about 2 to about 15 wt % of the total weight of the compressed tablet.

9. The method of claim 1 , wherein the core comprises at least 60 wt % of a first polymer.

10. The method of claim 1 , wherein the second polymer comprises poly(methyl methacrylates).

11. The method of claim 1 , wherein the second polymer comprises hydroxypropyl methyl cellulose.

12. The method of claim 1 , wherein the compressed tablet comprises about 1 mg to about 400 mg of ketamine, esketamine, or a pharmaceutically acceptable salt thereof.

13. The method of claim 12 , wherein the compressed tablet comprises about 1 mg to about 100 mg of ketamine, esketamine, or a pharmaceutically acceptable salt thereof.

14. The method of claim 12 , wherein the compressed tablet comprises about 1 mg to about 56 mg of ketamine, esketamine, or a pharmaceutically acceptable salt thereof.

15. The method of claim 12 , wherein the compressed tablet comprises about 56 mg of ketamine, esketamine, or a pharmaceutically acceptable salt thereof.

16. The method of claim 1 , wherein the administration of the compressed tablet to the subject in need thereof, further reduces the potential for abuse of ketamine, esketamine, or a pharmaceutically acceptable salt thereof.

17. The method of claim 1 , wherein the administration further reduces the risk of abuse of ketamine, esketamine, or a pharmaceutically acceptable salt thereof by simultaneous oral ingestion of multiple units of the compressed tablet.

18. The method according to claim 1 , wherein the administration further reduces the risk of abuse of ketamine, esketamine, or a pharmaceutically acceptable salt thereof by nasal insufflation.

19. The method according to claim 1 , wherein the administration further reduces the risk of abuse of ketamine, esketamine, or a pharmaceutically acceptable salt thereof by injection.

Assignees

• Clexio Biosciences Ltd

Inventors

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

Classifications

• A61K31/515

  Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital · CPC title

• A61K9/2009

  Inorganic compounds · CPC title

• A61K47/61

  the organic macromolecular compound being a polysaccharide or a derivative thereof · CPC title

• A61K31/00

  Medicinal preparations containing organic active ingredients · CPC title

• A61K31/437

  the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline · CPC title