Claims for Patent: 11,439,597

Summary for Patent: 11,439,597

Title:	Formulations of (R)-2-amino-3-phenylpropyl carbamate
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.
Inventor(s):	Clark Patrick Allphin, Edwin Gerard Walsh
Assignee:	Axsome Malta Ltd
Application Number:	US17/154,336
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,439,597
Patent Claims:	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.