Formulations of (R)-2-amino-3-phenylpropyl carbamate
View Patent ↗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. An immediate release compressed tablet for oral delivery of (R)-2-amino-3-phenylpropyl carbamate, 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 immediate release compressed tablet 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.
3. The immediate release compressed tablet of claim 1 , wherein the tablet does not comprise a disintegrant.
4. The immediate release compressed tablet 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.
5. The immediate release compressed tablet 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.
6. The immediate release compressed tablet 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 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.
7. The immediate release compressed tablet of claim 1 , further comprising a coating.
8. The immediate release compressed tablet of claim 1 , wherein the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate is (R)-2-amino-3-phenylpropyl carbamate hydrochloride.
9. The immediate release compressed tablet of claim 1 , wherein the tablet comprises about 300 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
10. The immediate release compressed tablet of claim 1 , wherein the tablet comprises about 150 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
11. The immediate release compressed tablet of claim 1 , wherein the tablet comprises about 75 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
12. The immediate release compressed tablet of claim 1 , wherein the tablet comprises about 37.5 mg of the pharmaceutically acceptable salt of (R)-2-amino-3-phenylpropyl carbamate.
13. The immediate release compressed tablet of claim 7 , wherein the coating is a color overcoat.
14. The immediate release compressed tablet of claim 1 , wherein the tablet is oblong in shape.
15. The immediate release compressed tablet of claim 1 , wherein the tablet is free of other excipients.
16. The immediate release compressed tablet of claim 7 , wherein the tablet is free of other excipients.
17. The immediate release compressed tablet 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 tablet and a total weight of between about 30 to about 300 mg per tablet.
18. The immediate release compressed tablet of claim 1 , comprising hydroxypropyl cellulose in an amount of about 1-3% by weight of the tablet.
19. The immediate release compressed tablet of claim 1 , comprising magnesium stearate in an amount of about 0.1% to about 1.0% by weight of the tablet.
20. An immediate release compressed tablet for oral delivery of (R)-2-amino-3-phenylpropyl carbamate, 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 and a total weight of between about 30 to about 300 mg per tablet;
hydroxypropyl cellulose in an amount of about 1-3% by weight of the tablet; and
magnesium stearate in an amount of about 0.1% to about 1.0% 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.
21. An immediate release compressed tablet for oral delivery of (R)-2-amino-3-phenylpropyl carbamate, 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 and a total weight of between about 30 to about 300 mg per tablet;
hydroxypropyl cellulose in an amount of about 2% by weight of the tablet; and
magnesium stearate in an amount of about 0.5% by weight of the tablet;
wherein the tablet releases at least 85% of the pharmaceutically acceptable salt of (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 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.