Formulations of (R)-2-amino-3-phenylpropyl carbamate

Patent metadata

Field	Value
Publication number	US-10512609-B2
Application number	US-201816225890-A
Country	US
Kind code	B2
Filing date	Dec 19, 2018
Priority date	Sep 6, 2016
Publication date	Dec 24, 2019
Grant date	Dec 24, 2019

Abstract

The present invention relates to immediate release formulations of (R)-2-amino-3-phenylpropyl carbamate and methods of using the same to treat disorders.

First claim

What is claimed is:

1. A method of treating narcolepsy, cataplexy, excessive daytime sleepiness, drug addiction, sexual dysfunction, fatigue, fibromyalgia, attention deficit/hyperactivity disorder, restless legs syndrome, depression, bipolar disorder, or obesity in a subject in need thereof, or promoting smoking cessation in a subject in need thereof, comprising administering to the subject an immediate release compressed tablet, the tablet comprising:
a pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate in an amount of about 90-98% by weight of the tablet;
at least one binder in an amount of about 1-5% by weight of the tablet; and
at least one lubricant in an amount of about 0.1-2% by weight of the tablet;
wherein the tablet releases at least 85% of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate contained therein within a period of less than 15 minutes after administration of the tablet to a subject; and
wherein the tablet exhibits substantially identical dissolution rates of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate at pH 1.2, pH 4.5, and pH 6.8.

2. The method of claim 1 , wherein the tablet is administered once per day.

3. The method of claim 1 , wherein the tablet is administered more than once per day.

4. The method of claim 1 , wherein the tablet releases at least 95% of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate contained therein within a period of less than 15 minutes after administration of the tablet to a subject.

5. The method of claim 1 , wherein the tablet does not comprise a disintegrant.

6. The method of claim 1 , wherein the at least one binder is selected from at least one of hydroxypropyl cellulose ethylcellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, hydroxyethyl cellulose, povidone, copovidone, pregelatinized starch, dextrin, gelatin, maltodextrin, starch, zein, acacia, alginic acid, carbomers (cross-linked polyacrylates), polymethacrylates, sodium carboxymethylcellulose, guar gum, hydrogenated vegetable oil (type 1), methylcellulose, magnesium aluminum silicate, and sodium alginate.

7. The method of claim 1 , wherein the at least one lubricant is selected from at least one of magnesium stearate, stearic acid, calcium stearate, hydrogenated castor oil, hydrogenated vegetable oil, light mineral oil, magnesium stearate, mineral oil, polyethylene glycol, sodium benzoate, sodium stearyl fumarate, and zinc stearate.

8. The method of claim 1 , wherein the tablet comprises:
a pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate in an amount of about 90-98% by weight of the tablet;
hydroxypropyl cellulose in an amount of about 1-5% by weight of the tablet; and
magnesium stearate in an amount of about 0.1-2% by weight of the tablet.

9. The method of claim 1 , wherein the tablet further comprises a coating.

10. The method of claim 9 , wherein the coating is a color overcoat.

11. The method of claim 1 , wherein the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate is (R)-2-amino-3-phenylpropyl carbamate hydrochloride.

12. The method of claim 1 , wherein the tablet is oblong in shape.

13. The method of claim 1 , wherein the tablet comprises about 300 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.

14. The method of claim 1 , wherein the tablet comprises about 150 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.

15. The method of claim 1 , wherein the tablet comprises about 75 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.

16. The method of claim 1 , wherein the tablet comprises about 37.5 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.

Assignees

• Jazz Pharmaceuticals International Iii Ltd
• Jazz Pharmaceuticals Ireland Ltd

Inventors

• Allphin Clark Patrick
• Walsh Edwin Gerard

Classifications

• A61P25/34

  Tobacco-abuse · CPC title

• A61P25/30

  for treating abuse or dependence · CPC title

• A61P25/24

  Antidepressants · CPC title

• A61P25/18

  Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title