Compositions comprising dexamethasone

• US 10,537,585 B2
• Filed: 12/18/2017
• Issued: 01/21/2020
• Est. Priority Date: 12/18/2017
• Status: Active Grant

• Current Assignee: Dexcel Pharma Technologies (Dexcel Limited)
• Original Assignee: Dexcel Pharma Technologies (Dexcel Limited)
• Inventors: Kreyenborg, Caterina, Meimberg, Elisabeth, Tissen, Corinna, Bannefeld, Karl-Heinz, Gold, Tomer
• Primary Examiner(s): Cruz, Kathrien A
• Application Number:
  US15/845,232
• Publication Number:
  US 20190183907A1
• Time in Patent Office: 764 Days
• Field of Search: None
• CPC Class Codes: A61K 31/454 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid

Abstract

A pharmaceutical composition useful for the treatment of multiple myeloma in combination with an anti-cancer drug is provided. The pharmaceutical composition includes high-dose dexamethasone or a pharmaceutically acceptable salt or solvate thereof.

Claims

1. A high-dose immediate release dexamethasone tablet or caplet for oral administration in the form of a single unit dosage form consisting of:

i) 20 mg dexamethasone,

ii) 4 mg to 8 mg sodium carboxymethyl starch,

iii) 48 mg to 58 mg lactose,

iv) 12.5 mg to 22.5 mg starch,

v) 2.5 mg polyvinylpyrrolidone, and

vi) 0.5 mg to 1.5 mg magnesium stearate,

wherein the unit dosage form has a total weight of about 100 mg.

2. The high-dose immediate release dexamethasone tablet or caplet of claim 1, which is uncoated.

3. The high-dose immediate release dexamethasone tablet or caplet of claim 1, having a hardness value of about 40 N to about 100 N.

4. The high-dose immediate release dexamethasone tablet or caplet of claim 3, having a hardness value of about 47 N to about 73 N.

5. The high-dose immediate release dexamethasone tablet or caplet of claim 1, having a friability of about 0.05% to about 0.5%.

6. The high-dose immediate release dexamethasone tablet or caplet of claim 5, having a friability of about 0.08% to about 0.22%.

7. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 51 mg to 55 mg lactose.

8. The high-dose immediate release dexamethasone tablet or caplet of claim 7, wherein the lactose is lactose monohydrate.

9. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 20 mg dexamethasone, 58 mg lactose monohydrate, 6 mg sodium carboxymethyl starch, 12.5 mg corn starch, 2.5 mg polyvinylpyrrolidone, and 1 mg magnesium stearate, wherein the unit dosage form has a total weight of about 100 mg.

10. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 20 mg dexamethasone, 53 mg lactose monohydrate, 6 mg sodium carboxymethyl starch, 17.5 mg corn starch, 2.5 mg polyvinylpyrrolidone, and 1 mg magnesium stearate, wherein the unit dosage form has a total weight of about 100 mg.

11. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 20 mg dexamethasone, 48 mg lactose monohydrate, 6 mg sodium carboxymethyl starch, 22.5 mg corn starch, 2.5 mg polyvinylpyrrolidone, and 1 mg magnesium stearate, wherein the unit dosage form has a total weight of about 100 mg.

12. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 20 mg dexamethasone, 55 mg lactose monohydrate, 4 mg sodium carboxymethyl starch, 17.5 mg corn starch, 2.5 mg polyvinylpyrrolidone, and 1 mg magnesium stearate, wherein the unit dosage form has a total weight of about 100 mg.

13. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 20 mg dexamethasone, 51 mg lactose monohydrate, 8 mg sodium carboxymethyl starch, 17.5 mg corn starch, 2.5 mg polyvinylpyrrolidone, and 1 mg magnesium stearate, wherein the unit dosage form has a total weight of about 100 mg.

14. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 20 mg dexamethasone, 53.5 mg lactose monohydrate, 6 mg sodium carboxymethyl starch, 17.5 mg corn starch, 2.5 mg polyvinylpyrrolidone, and 0.5 mg magnesium stearate, wherein the unit dosage form has a total weight of about 100 mg.

15. The high-dose immediate release dexamethasone tablet or caplet of claim 1, containing 20 mg dexamethasone, 52.5 mg lactose monohydrate, 6 mg sodium carboxymethyl starch, 17.5 mg corn starch, 2.5 mg polyvinylpyrrolidone, and 1.5 mg magnesium stearate, wherein the unit dosage form has a total weight of about 100 mg.