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Last Updated: September 21, 2021

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Claims for Patent: 9,446,057


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Summary for Patent: 9,446,057
Title:Controlled release doxycycline
Abstract: The disclosure provides controlled release compositions comprising tetracyclines and in some embodiments, doxycycline. The controlled release doxycycline compositions of the invention exhibit a superior dissolution profile and provide reduce side effects such as nausea and irritation.
Inventor(s): Lukas; Stefan (Manningham, AU), Lepore; Angelo (Rostrevor, AU), Mudge; Stuart (Northcote, AU)
Assignee: Mayne Pharma International Pty. Ltd. (Salisbury South, AU)
Application Number:14/939,936
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,446,057
Patent Claims: 1. A dosage form comprising a plurality of modified release doxycycline pellets, wherein each doxycycline pellet comprises: doxycycline; and a controlled release polymer composition disposed over the doxycycline, wherein said dosage form comprises 60, 90, or 120 mg of doxycycline and maintains doxycycline release levels measured under USP <711> conditions at pH 5 that provide a clinically effective plasma level of doxycycline.

2. The dosage form of claim 1, wherein when the amount of doxycycline of said dosage form is 60 mg, after administration of a single dose under fasting conditions to a patient in need thereof, the average C.sub.max is about 80% to about 125% of about 625-1600 ng/ml; or wherein when the amount of doxycycline of said dosage form is 90 mg, after administration of a single dose under fasting conditions to a patient in need thereof, the average C.sub.max is about 80% to about 125% of about 940-2400 ng/ml; or wherein when the amount of doxycycline of said dosage form is 120 mg, after administration of a single dose under fasting conditions to a patient in need thereof, the average C.sub.max is about 80% to about 125% of about 1250-3200 ng/ml.

3. The dosage form of claim 1, wherein when the amount of doxycycline of said dosage form is 60 mg, after administration of a single dose to a patient in need thereof, the average AUC.sub.0-.infin. is about 80% to about 125% of about 10000-24000 nghr/ml; or wherein when the amount of doxycycline of said dosage form is 90 mg, after administration of a single dose to a patient in need thereof, the average AUC.sub.0-.infin. is about 80% to about 125% of about 15000-36500 nghr/ml; or wherein when the amount of doxycycline of said dosage form is 120 mg, after administration of a single dose to a patient in need thereof, the average AUC.sub.0-.infin. is about 80% to about 125% of about 20000-48500 nghr/ml.

4. The dosage form of claim 2, wherein when the amount of doxycycline of said dosage form is 60 mg, after administration of a single dose to a patient in need thereof, the average AUC.sub.0-.infin. is about 80% to about 125% of about 10000-24000 nghr/ml; or wherein when the amount of doxycycline of said dosage form is 90 mg, after administration of a single dose to a patient in need thereof, the average AUC.sub.0-.infin. is about 80% to about 125% of about 15000-36500 nghr/ml; or wherein when the amount of doxycycline of said dosage form is 120 mg, after administration of a single dose to a patient in need thereof, the average AUC.sub.0-.infin. is about 80% to about 125% of about 20000-48500 nghr/ml.

5. The dosage form of claim 1, wherein the release of doxycycline at pH 5 measured under USP <711> conditions is at least one of the following: about 45% to about 50% after 10 minutes; about 55% to about 65% at 20 minutes; about 65% to about 70% at 30 minutes; about 70% to about 75% at 45 minutes; and about 75% to about 80% at 60 minutes.

6. The dosage form of claim 1, wherein the dosage form maintains release levels measured under USP <711> conditions that are low at pH values up to pH 4.5.

7. The dosage form of claim 2, wherein the dosage form maintains release levels measured under USP <711> conditions that are low at pH values up to pH 4.5.

8. The dosage form of claim 3, wherein the dosage form maintains release levels measured under USP <711> conditions that are low at pH values up to pH 4.5.

9. The dosage form of claim 4, wherein the dosage form maintains release levels measured under USP <711> conditions that are low at pH values up to pH 4.5.

10. The dosage form of claim 5, wherein the release of doxycycline at pH 5 measured under USP <711> conditions is at least two of the following: about 45% to about 50% after 10 minutes; about 55% to about 65% at 20 minutes; about 65% to about 70% at 30 minutes; about 70% to about 75% at 45 minutes; and about 75% to about 80% at 60 minutes.

11. The dosage form of claim 5, wherein the release of doxycycline at pH 5 measured under USP <711> conditions is at least three of the following: about 45% to about 50% after 10 minutes; about 55% to about 65% at 20 minutes; about 65% to about 70% at 30 minutes; about 70% to about 75% at 45 minutes; and about 75% to about 80% at 60 minutes.

12. The dosage form of claim 5, wherein the release of doxycycline at pH 5 measured under USP <711> conditions is at least four of the following: about 45% to about 50% after 10 minutes; about 55% to about 65% at 20 minutes; about 65% to about 70% at 30 minutes; about 70% to about 75% at 45 minutes; and about 75% to about 80% at 60 minutes.

13. The dosage form of claim 5, wherein the release of doxycycline at pH 5 measured under USP <711> conditions is: about 45% to about 50% after 10 minutes; about 55% to about 65% at 20 minutes; about 65% to about 70% at 30 minutes; about 70% to about 75% at 45 minutes; and about 75% to about 80% at 60 minutes.

14. The dosage form of claim 1, wherein the doxycycline pellets comprise a doxycycline-containing core, and the controlled release polymer composition is disposed as a layer over the core.

15. The dosage form of claim 14, wherein the controlled release polymer composition comprises a blend of an enteric polymer and a water soluble polymer.

16. The dosage form of claim 15, wherein the controlled release polymer composition further comprises a plasticizer.

17. The dosage form of claim 16, wherein the controlled release polymer composition consists essentially of a blend of an enteric polymer, a water soluble polymer, and a plasticizer.

18. The dosage form of claim 14, further comprising a stabilizing coating disposed between the core and the controlled release polymer composition layer.

19. A method of treating a skin condition in a patient, comprising orally administering the dosage form of claim 1 to a patient in need thereof.

20. A method of treating a skin condition in a patient, comprising orally administering the dosage form of claim 14 to a patient in need thereof.

21. The method of claim 19, wherein said skin condition is at least one condition selected from the group consisting of: a skin infection, rosacea, acne, papules, pustules, open comedo, closed comedo, or a combination thereof.

22. The method of claim 20, wherein said skin condition is at least one condition selected from the group consisting of: a skin infection, rosacea, acne, papules, pustules, open comedo, closed comedo, or a combination thereof.

23. The method of claim 19, wherein said administering is once-per-day.

24. The method of claim 20, wherein said administering is once-per-day.

25. The dosage form of claim 1, wherein the amount of doxycycline of said dosage form is 60 mg.

26. The dosage form of claim 1, wherein the amount of doxycycline of said dosage form is 90 mg.

27. The dosage form of claim 1, wherein the amount of doxycycline of said dosage form is 120 mg.

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