Formulations of (R)-2-amino-3-phenylpropyl carbamate
The present invention relates to immediate release formulations of (R)-2-amino-3-phenylpropyl carbamate and methods of using the same to treat disorders.
1. A solid pharmaceutical formulation for oral delivery of (R)-2-amino-3-phenylpropyl carbamate, comprising:
a pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate in an amount of about 90-98% by weight of the formulation;
hydroxypropyl cellulose in an amount of 1-5% by weight of the formulation; and
magnesium stearate in an amount of about 0.1-2% by weight of the formulation;
wherein the formulation 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 formulation to a subject; and
wherein the formulation 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; and
wherein the formulation does not comprise a disintegrant.
2. The solid pharmaceutical formulation of claim 1 , wherein the pharmaceutical formulation is a tablet.
3. The solid pharmaceutical formulation of claim 1 , wherein the formulation 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 formulation to a subject.
4. The solid pharmaceutical formulation of claim 1 , further comprising a coating.
5. The solid pharmaceutical formulation of claim 4 , wherein the coating is a color overcoat.
6. The solid pharmaceutical formulation of claim 1 , wherein the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate is (R)-2-amino-3-phenylpropyl carbamate hydrochloride.
7. The solid pharmaceutical formulation of claim 1 , wherein the formulation comprises about 300 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
8. The solid pharmaceutical formulation of claim 1 , wherein the formulation comprises about 150 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
9. The solid pharmaceutical formulation of claim 1 , wherein the formulation comprises about 75 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
10. The solid pharmaceutical formulation of claim 1 , wherein the formulation comprises about 37.5 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
11. The solid pharmaceutical formulation of claim 1 , comprising a pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate in an amount of about 90-98% by weight of the formulation and a total weight of between about 30 to about 300 mg.
12. The solid pharmaceutical formulation of claim 1 , comprising hydroxypropyl cellulose in an amount of about 1% to about 3% by weight of the formulation.
13. The solid pharmaceutical formulation of claim 1 , comprising magnesium stearate in an amount of about 0.1% to about 1.0% by weight of the formulation.
14. The solid pharmaceutical formulation of claim 1 , comprising hydroxypropyl cellulose in an amount of about 2% by weight of the formulation.
15. The solid pharmaceutical formulation of claim 1 , comprising magnesium stearate in an amount of about 0.5% by weight of the formulation.
16. 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 solid pharmaceutical formulation for oral delivery of (R)-2-amino-3-phenylpropyl carbamate, the formulation comprising:
a pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate in an amount of about 90-98% by weight of the formulation;
hydroxypropyl cellulose in an amount of 1-5% by weight of the formulation; and
magnesium stearate in an amount of about 0.1-2% by weight of the formulation;
wherein the formulation 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 formulation to a subject; and
wherein the formulation 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; and
wherein the formulation does not comprise a disintegrant.
17. The method claim 16 , wherein the pharmaceutical formulation is a tablet.
18. The method claim 16 , wherein the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate is (R)-2-amino-3-phenylpropyl carbamate hydrochloride.
19. The method of claim 16 , wherein the formulation comprises between about 30 and about 300 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.