IP Library Granted Patent US 10,300,039
Granted Patent B2
US 10,300,039 · App. 15/159,008 · Granted May 28, 2019

Ferric citrate dosage forms

Inventor: Henry Trong Le (Englewood Cliffs, NJ)
Assignee: KERYX BIOPHARMACEUTICALS, INC.
A61K31/295A61K9/2013A61K9/2054A61K9/2059A61K9/2077A61K9/2095
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Quick Facts
Patent No.
US 10,300,039
App. No.
15/159,008
Granted
May 28, 2019
Kind
B2
Abstract

Disclosed herein are ferric citrate-containing tablets. In various embodiments, the tablets include ferric citrate formulations that meet certain dissolution, tableting and disintegration standards. In various aspects, the tablet formulations can include ferric citrate as the active ingredient and a binder. The formulations also can include a lubricant and/or a disintegrant (which, in some embodiments, can be the same as the binder).

Claims (38)

1. A method for the prophylaxis or treatment of hyperphosphatemia comprising administering to a patient in need thereof a ferric citrate tablet, wherein the ferric citrate tablet comprises:

(a) a core comprising approximately 90% to approximately 92% by weight of ferric citrate, approximately 4.5% to approximately 30% by weight of pregelatinized starch, and approximately 0.5% to approximately 3% by weight of a lubricant; and

(b) a coating,

wherein the tablet has a friability equal or less than 1% w/w, and wherein at least 80% of the ferric citrate in the tablet is dissolved in less than or equal to 60 minutes as measured by test method USP <711>, and the moisture content of the tablet is less than 10% by loss on drying (LOD).

2. The method of claim 1 , wherein the lubricant is calcium stearate.

3. The method of claim 1 , wherein the tablet comprises approximately 1000 mg of ferric citrate.

4. A method for the prophylaxis or treatment of hyperphosphatemia comprising administering to a patient in need thereof a ferric citrate tablet containing approximately 210 mg of ferric iron, wherein the ferric citrate tablet comprises:

(a) a core comprising approximately 87.6% by weight of ferric citrate, approximately 10% by weight of pregelatinized starch, and approximately 2.4% by weight of calcium stearate; and

(b) a coating,

wherein the tablet has a friability equal or less than 1% w/w and a disintegration time less than 15 minutes, and wherein at least 80% of the ferric citrate in the tablet is dissolved in less than or equal to 60 minutes as measured by test method USP <711>, and the moisture content of the tablet is 8.84% (LOD).

5. A method for the prophylaxis or treatment of hyperphosphatemia comprising administering to a patient in need thereof a ferric citrate tablet, wherein the ferric citrate tablet comprises:

(a) a core comprising approximately 90% to approximately 92% by weight of ferric citrate, approximately 4.5% to approximately 30% by weight of pregelatinized starch, and approximately 0.5% to approximately 3% by weight of a lubricant; and

(b) a coating,

wherein the tablet has a friability equal or less than 1% w/w, and wherein at least 80% of the ferric citrate is dissolved in less than or equal to 60 minutes as measured by test method USP <711>, and the moisture content of the tablet is between 5% to 10% by LOD.

6. The method of claim 5 , wherein the lubricant is calcium stearate.

7. The method of claim 5 , wherein the tablet comprises approximately 1000 mg of ferric citrate.

8. A method for the prophylaxis or treatment of hyperphosphatemia comprising administering to a patient in need thereof a ferric citrate tablet, wherein the ferric citrate tablet comprises:

(a) a core comprising approximately 90% to approximately 92% by weight of ferric citrate, approximately 1.5% to approximately 15% by weight of pregelatinized starch, and approximately 0.5% to approximately 3% by weight of a lubricant; and

(b) a coating,

wherein the tablet has a friability equal or less than 1%, and wherein at least 80% of the ferric citrate in the tablet is dissolved in less than or equal to 60 minutes as measured by test method USP<711>, and the moisture content of the tablet is between 5% to 10% by LOD.

9. The method of claim 8 , wherein the lubricant is calcium stearate.

10. The method of claim 8 , wherein the tablet comprises approximately 1000 mg of ferric citrate.

11. A method for controlling serum phosphorus levels in an end-stage renal disease patient on hemodialysis comprising administering to the patent a ferric citrate tablet, wherein the ferric citrate tablet comprises:

(a) a core comprising approximately 90% to approximately 92% by weight of ferric citrate, approximately 4.5% to approximately 30% by weight of pregelatinized starch, and approximately 0.5% to approximately 3% by weight of a lubricant; and

(b) a coating,

wherein the tablet has a friability equal or less than 1% w/w, and wherein at least 80% of the ferric citrate in the tablet is dissolved in less than or equal to 60 minutes as measured by test method USP <711>, and the moisture content of the tablet is less than 10% by loss on drying (LOD).

12. The method of claim 11 , wherein the lubricant is calcium stearate.

13. The method of claim 11 , wherein the tablet comprises approximately 1000 mg of ferric citrate.

14. A method for controlling serum phosphorus levels in an end-stage renal disease patient on hemodialysis comprising administering to the patent a ferric citrate tablet containing approximately 210 mg of ferric iron, wherein the ferric citrate tablet comprises:

(a) a core comprising approximately 87.6% by weight of ferric citrate, approximately 10% by weight of pregelatinized starch, and approximately 2.4% by weight of calcium stearate; and

(b) a coating,

wherein the tablet has a friability equal or less than 1% w/w and a disintegration time less than 15 minutes, and wherein at least 80% of the ferric citrate in the tablet is dissolved in less than or equal to 60 minutes as measured by test method USP <711>, and the moisture content of the tablet is 8.84% (LOD).

15. A method for controlling serum phosphorus levels in an end-stage renal disease patient on hemodialysis comprising administering to the patent a ferric citrate tablet, wherein the ferric citrate tablet comprises:

(a) a core comprising approximately 90% to approximately 92% by weight of ferric citrate, approximately 4.5% to approximately 30% by weight of pregelatinized starch, and approximately 0.5% to approximately 3% by weight of a lubricant; and

(b) a coating,

wherein the tablet has a friability equal or less than 1% w/w, and wherein at least 80% of the ferric citrate is dissolved in less than or equal to 60 minutes as measured by test method USP <711>, and the moisture content of the tablet is between 5% to 10% by LOD.

16. The method of claim 15 , wherein the lubricant is calcium stearate.

17. The method of claim 15 , wherein the tablet comprises approximately 1000 mg of ferric citrate.

Assignments (18)
TERMINATION AND RELEASE OF SECURITY INTEREST IN PATENTS Recorded Jun 25, 2024
From: BIOPHARMA CREDIT PLC
To: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
Reel/Frame 067839/0134 →
SECURITY INTEREST Recorded Jan 29, 2024
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: KREOS CAPITAL VII (UK) LIMITED
Reel/Frame 066377/0654 →
TERMINATION AND RELEASE OF SECURITY INTEREST IN PATENTS Recorded Jan 29, 2024
From: BIOPHARMA CREDIT PLC
To: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
Reel/Frame 066377/0741 →
FIFTEENTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Jan 4, 2024
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 066205/0143 →
THIRTEENTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Mar 29, 2023
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 063189/0065 →
TWELFTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Nov 29, 2022
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 062012/0561 →
ELEVENTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Aug 22, 2022
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 061297/0238 →
TENTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Jun 16, 2022
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 060529/0168 →
SECURITY INTEREST Recorded Dec 15, 2021
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 058399/0055 →
SEVENTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Sep 12, 2021
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 057474/0770 →
SIXTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Jun 11, 2021
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 056544/0468 →
FIFTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Mar 30, 2021
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 055776/0491 →
FOURTH AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 17, 2020
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 054793/0455 →
THIRD AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Sep 10, 2020
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 054173/0451 →
SECOND AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Sep 2, 2020
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 053671/0221 →
SECURITY INTEREST Recorded Apr 2, 2020
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 052295/0662 →
SECURITY INTEREST Recorded Nov 26, 2019
From: AKEBIA THERAPEUTICS, INC.; KERYX BIOPHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 051119/0089 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 23, 2018
From: LE, HENRY TRONG
To: KERYX BIOPHARMACEUTICALS, INC.
Reel/Frame 045886/0236 →
Continuity (3)
Division 13255326
Provisional Application 61227124 · Jul 21, 2009
Related Publication 20160263075A1 · Sep 15, 2016