Immediate release multilayer tablet
AssigneeAlkermes Pharma Ireland Limited
InventorsRenato A. Chiarella, Hector Guzman, Paul Hurley, David Manser, Kristopher Perkin
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Abstract
Described herein, in part, are tablets, such as immediate release multi-layer or bilayer tablets for orally delivering olanzapine and samidorphan, methods of using said tablets in the treatment of disorders described herein, and kits comprising said tablets.
Claims13
A method of treating schizophrenia or bipolar I disorder in a patient in need thereof, the method comprising orally administering to the patient, once daily, a pharmaceutically acceptable coated immediate release bilayer tablet for orally delivering a fixed dose of olanzapine and 10 mg of samidorphan, wherein the bilayer tablet comprises:
- a first tablet layer comprising:
- 10 mg samidorphan or a pharmaceutically acceptable salt of samidorphan in an amount to deliver 10 mg samidorphan;
- about 35-43 wt % microcrystalline cellulose, based on the weight of the first tablet layer;
- about 37-43 wt % lactose or a hydrate thereof, based on the weight of the first tablet layer;
- and
- about 1.5 to about 2 wt % magnesium stearate;
- a second tablet layer comprising:
- a dose of olanzapine selected from the group consisting of 5 mg, 10 mg, 15 mg and 20 mg of the olanzapine;
- about 38-42 wt % microcrystalline cellulose, based on the weight of the second tablet layer;
- about 46-49 wt % lactose or a hydrate thereof, based on the weight of the second tablet layer;
- and
- about 1.0 wt % magnesium stearate;
- and
- a film coating over the first and second tablet layer, wherein the tablet releases at least 97% of olanzapine and at least 97% of the samidorphan after 30 minutes when the tablet is tested in 500 mL USP acetate buffer at pH 1.0 using a USP Apparatus II (Paddle Method) at 37 with a paddle speed of 75 rpm and using a three-prong sinker.
A method of treating schizophrenia or bipolar I disorder in a patient in need thereof, the method comprising orally administering to the patient, once daily, a pharmaceutically acceptable coated immediate release bilayer tablet for orally delivering a fixed dose of olanzapine and 10 mg of samidorphan, wherein the bilayer tablet comprises:
- a first tablet layer comprising:
- 13.6 mg samidorphan L-malate;
- about 40 wt % microcrystalline cellulose, based on the weight of the first tablet layer;
- about 42 wt % lactose monohydrate, based on the weight of the first tablet layer;
- and about 1.75 wt % magnesium stearate;
- and
- a second tablet layer comprising:
- a dose of olanzapine selected from the group consisting of 5 mg, 10 mg, 15 mg and 20 mg of the olanzapine;
- about 40 wt % microcrystalline cellulose, based on the weight of the second tablet layer;
- about 47 wt % lactose or a hydrate thereof, based on the weight of the second tablet layer;
- and about 1.0 wt % magnesium stearate;
- and a film coating over the first and second tablet layer,
- wherein the tablet releases at least 97% of olanzapine and at least 97% of the samidorphan after 30 minutes when the tablet is tested in 500 mL USP acetate buffer at pH 1.0 using a USP Apparatus II (Paddle Method) at 37 with a paddle speed of 75 rpm and using a three-prong sinker.
A method of treating schizophrenia or bipolar I disorder in a patient in need thereof, the method comprising orally administering to the patient, once daily, a pharmaceutically acceptable coated immediate release bilayer tablet for orally delivering olanzapine and 10 mg of samidorphan as a fixed dose, comprising:
- a first tablet layer comprising:
- 10 mg samidorphan or a pharmaceutically acceptable salt of samidorphan in an amount to deliver 10 mg samidorphan;
- about 35-43 wt % microcrystalline cellulose, based on the weight of the first tablet layer;
- and
- about 37-43 wt % lactose or a hydrate thereof, based on the weight of the first tablet layer;
- a second tablet layer comprising:
- a dose of olanzapine selected from the group consisting of 5 mg, 10 mg, 15 mg and 20 mg of the olanzapine;
- about 38-42 wt % microcrystalline cellulose, based on the weight of the second tablet layer;
- about 46-49 wt % lactose or a hydrate thereof, based on the weight of the second tablet layer;
- and
- a film coating over the first and second tablet layer;
- wherein the bi-layer tablet releases at least 85% of olazanpine and at least 85% of the samidorphan after 15 minutes when the bi-layer tablet is tested in 500 mL USP acetate buffer at pH 4.5 using a USP Apparatus II (Paddle Method) at 37° C., with a paddle speed of 75 rpm and using a three-prong sinker.
A method of treating schizophrenia or bipolar I disorder in a patient in need thereof, the method comprising orally administering to the patient, once daily, a pharmaceutically acceptable coated immediate release bilayer tablet for orally delivering, as a fixed dose, olanzapine and 10 mg of samidorphan wherein the bilayer tablet, comprises:
- a first tablet layer comprising:
- 10 mg samidorphan or a pharmaceutically acceptable salt of samidorphan in an amount to deliver 10 mg samidorphan;
- about 30-45 wt % microcrystalline cellulose, based on the weight of the first tablet layer;
- about 35-50 wt % lactose or a hydrate thereof, based on the weight of the first tablet layer;
- a second tablet layer comprising:
- a dose of olanzapine selected from the group consisting of 2.5 mg, 5 mg, 10 mg, 15 mg and 20 mg of the olanzapine;
- about 35-45 wt % microcrystalline cellulose, based on the weight of the second tablet layer;
- about 45-55 wt % lactose or a hydrate thereof, based on the weight of the second tablet layer;
- and a film coating over the first and second tablet layer,
- wherein the tablet releases at least 97% of olanzapine and at least 97% of the samidorphan after 30 minutes when the tablet is tested in 500 mL USP acetate buffer at pH 1.0 using a USP Apparatus II (Paddle Method) at 37 with a paddle speed of 75 rpm and using a three-prong sinker.
Dependencies are inferred from the claim text.