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 (APC) consisting of
i) a pharmaceutically acceptable salt of APC containing 75 mg of APC;
ii) a binder in an amount not exceeding 5% by weight of the formulation;
iii) a lubricant in an amount of about 0.1-2% by weight of the formulation; and
iv) an optional coating;
wherein the formulation releases at least 85% of the pharmaceutically acceptable salt of APC in less than 15 minutes after oral administration of the formulation to a subject; and wherein the formulation exhibits substantially identical dissolution rates of the pharmaceutically acceptable salt of APC at pH 1.2, pH 4.5, and pH 6.8;
wherein the binder is selected from hydroxypropyl cellulose, hydroxypropyl methylcellulose, and povidone; and
wherein the lubricant is selected from magnesium stearate, calcium stearate, and sodium stearyl fumarate.
2. The solid pharmaceutical formulation of claim 1 , wherein the formulation releases at least 95% of the (R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof contained therein within a period of less than 15 minutes after administration of the formulation to a subject.
3. The solid pharmaceutical formulation of claim 1 , wherein hydroxypropyl cellulose is in an amount of about 1-3% by weight of the formulation.
4. The solid pharmaceutical formulation of claim 1 , wherein magnesium stearate is in an amount of about 0.1% to about 1.0% by weight of the formulation.
5. The solid pharmaceutical formulation of claim 1 , wherein
(R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof is in an amount of about 90-98% by weight of the formulation;
hydroxypropyl cellulose is in an amount of about 1-5% by weight of the formulation; and
magnesium stearate is in an amount of about 0.1-2% by weight of the formulation.
6. The solid pharmaceutical formulation of claim 1 , wherein
(R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof is in an amount of about 90-98% by weight of the formulation;
hydroxypropyl cellulose is in an amount of about 2% by weight of the formulation; and
magnesium stearate is in an amount of about 0.5% by weight of the formulation.
7. The solid pharmaceutical formulation of claim 1 , wherein the (R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof is (R)-2-amino-3-phenylpropyl carbamate hydrochloride.
8. The solid pharmaceutical formulation of claim 1 , wherein the coating is present.
9. The solid pharmaceutical formulation of claim 8 , wherein the coating is a color overcoat.
10. A solid pharmaceutical formulation for oral delivery of (R)-2-amino-3-phenylpropyl carbamate (APC) consisting of
i) a pharmaceutically acceptable salt of APC containing 150 mg of APC;
ii) a binder in an amount of about 1-5% by weight of the formulation;
iii) a lubricant in an amount of about 0.1-2% by weight of the formulation; and
iv) an optional coating;
wherein the formulation releases at least 85% of the pharmaceutically acceptable salt of APC in less than 15 minutes after oral administration of the formulation to a subject; and wherein the formulation exhibits substantially identical dissolution rates of the pharmaceutically acceptable salt of APC at pH 1.2, pH 4.5, and pH 6.8;
wherein the binder is selected from hydroxypropyl cellulose, hydroxypropyl methylcellulose, and povidone:
wherein the lubricant is selected from magnesium stearate, calcium stearate, and sodium stearyl fumarate, and sodium stearyl fumarate.
11. The solid pharmaceutical formulation claim 10 , wherein the formulation releases at least 95% of the (R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof contained therein within a period of less than 15 minutes after administration of the formulation to a subject.
12. The solid pharmaceutical formulation of claim 10 , wherein hydroxypropyl cellulose is in an amount of about 1-3% by weight of the formulation.
13. The solid pharmaceutical formulation of claim 10 , wherein magnesium stearate is in an amount of about 0% to about 1.0% by weight of the formulation.
14. The solid pharmaceutical formulation of claim 10 , wherein
(R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof is in an amount of about 90-98% by weight of the formulation;
hydroxypropyl cellulose is in an amount of about 1-5% by weight of the formulation; and
magnesium stearate is in an amount of about 0.1-2% by weight of the formulation.
15. The solid pharmaceutical formulation of claim 10 , wherein
(R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof is in an amount of about 90-98% by weight of the formulation;
hydroxypropyl cellulose is in an amount of about 2% by weight of the formulation; and
magnesium stearate is in an amount of about 0.5% by weight of the formulation.
16. The solid pharmaceutical formulation of claim 10 , wherein the (R)-2-amino-3-phenylpropyl carbamate or a pharmaceutically acceptable salt thereof is (R)-2-amino-3-phenylpropyl carbamate hydrochloride.
17. The solid pharmaceutical formulation of claim 10 , wherein the coating is present.
18. The solid pharmaceutical formulation of claim 10 , wherein the coating is a color overcoat.