Pharmaceutical formulations comprising naltrexone and/or bupropion
AssigneeNalpropion Pharmaceuticals LLC
InventorsRob Churchill, Aaron Chesnut
Life of this patent
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Abstract
Described are pharmaceutical formulations comprising naltrexone and/or bupropion. Such pharmaceutical formulations can comprise extended-release, multilayer beads. Also described are methods of administering such formulations, such as for the treatment of overweight or obesity.
Claims30
An oral dosage form comprising a plurality of naltrexone-containing beads and a plurality of bupropion-containing beads,
- wherein the naltrexone-containing beads are extended-release, multilayer beads comprising:
- a core particle, wherein the core particle is drug-free;
- an optional seal coating coated on the surface of the core particle;
- a drug layer comprising naltrexone, or a salt thereof, coated on the surface of the core particle or, when present, the seal coating;
- a non-aqueous barrier coating coated on the surface of the drug layer;
- an extended-release coating coated on the surface of the barrier coating;
- and
- an optional top coating coated on the surface of the extended-release coating;
- wherein the naltrexone-containing beads have an in vitro naltrexone dissolution profile in a dissolution test of USP Apparatus 1 Basket Method at 100 rpm in a dissolution medium of water at 37° C. of:
- i. 2% to 20% of the naltrexone released in one hour;
- ii. 10% to 50% of the naltrexone released in two hours;
- and
- iii. 50% to 90% of the naltrexone released in four hours;
- and
- wherein the bupropion-containing beads are extended-release, multilayer beads comprising:
- a core particle comprising bupropion, or a salt thereof;
- an optional seal coating coated on the surface of the core particle;
- an extended-release coating coated on the surface of the core particle, or if present, on the surface of the seal coating;
- and
- an optional top coating coated on the surface of the extended-release coating.
A method of treating overweight or obesity in a subject in need thereof, the method comprising:
- administering to the subject a first oral dosage form comprising about 8 mg of naltrexone or salt thereof and about 90 mg of bupropion or salt thereof, wherein the first oral dosage form is administered once a day for a first week;
- administering to the subject a second oral dosage form comprising about 16 mg of naltrexone or salt thereof and about 180 mg of bupropion or salt thereof, wherein the second oral dosage form is administered once a day for a second week;
- administering to the subject a third oral dosage form comprising about 24 mg of naltrexone or salt thereof and about 270 mg of bupropion or salt thereof, wherein the third oral dosage form is administered once a day for a third week;
- and
- administering to the subject a fourth oral dosage form comprising about 32 mg of naltrexone or salt thereof and about 360 mg of bupropion or salt thereof, wherein the fourth oral dosage form is administered once a day for a fourth and subsequent weeks,
- wherein each of the first oral dosage form, the second oral dosage form, the third oral dosage form and the fourth oral dosage form comprises a plurality of naltrexone-containing beads and a plurality of bupropion-containing beads, wherein the naltrexone-containing beads are extended-release, multilayer beads and wherein the bupropion-containing beads are extended-release, multilayer beads;
- wherein the naltrexone-containing beads have an in vitro naltrexone dissolution profile in a dissolution test of USP Apparatus 1 Basket Method at 100 rpm in a dissolution medium of water at 37° C. of:
- i. 2% to 20% of the naltrexone released in one hour;
- ii. 10% to 50% of the naltrexone released in two hours;
- and
- iii. 50% to 90% of the naltrexone released in four hours.
A method of treating overweight or obesity in a subject in need thereof, the method comprising administering to the subject an oral dosage form comprising naltrexone and bupropion once a day, wherein the oral dosage form comprises a naltrexone extended-release formulation having an in vitro naltrexone dissolution profile in a dissolution test of USP Apparatus 1 Basket Method at 100 rpm in a dissolution medium of water at 37° C. of:
- iv. 2% to 20% of the naltrexone released in one hour;
- v. 10% to 50% of the naltrexone released in two hours;
- and
- vi. 50% to 90% of the naltrexone released in four hours.
Dependencies are inferred from the claim text.