Novel Formulation of Meloxicam

US 20160101110A1
Filed: 12/18/2015
Published: 04/14/2016
Est. Priority Date: 06/09/2014
Status: Active Grant

First Claim

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1. A unit dosage form of a pharmaceutical composition comprising 5 mg of meloxicam, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma AUC (0-∞

) of 7500-20000 h*ng/ml.

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Abstract

Unit dosage forms of meloxicam containing either 5 mg or 10 mg of meloxicam that provide effective pain relief and have desirable pharmacokinetic properties are described. The unit dosage forms can provide pain relief when a single unit dose is administered to a patient and useful for treating pain such as osteoarthritis pain at a relatively low systemic exposure to meloxicam.

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1. A unit dosage form of a pharmaceutical composition comprising 5 mg of meloxicam, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma AUC (0-∞
- ) of 7500-20000 h*ng/ml.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
- - 2. The unit dosage form of claim 1, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma Cmax of 350-950 ng/ml.
  - 3. The unit dosage form of claim 1, wherein the particles of meloxicam have a median particle size, on a volume average basis, between 100 nm and 5000 nm.
  - 4. The unit dosage form of claim 1, wherein the D(0.9) of the particles of meloxicam is less than 3000 nm.
  - 5. The unit dosage form of claim 1, wherein the surface weighted mean diameter (D[3,2]) of the particles of meloxicam is between 100 nm and 800 nm.
  - 6. The unit dosage form of claim 1 wherein the volume weighted mean diameter (D[4,3]) of the particles of meloxicam is between 400 nm and 1300 nm.
  - 7. The unit dosage form of claim 1 wherein the dissolution rate is such that, when tested using USP Apparatus 1 (baskets) set to rotation speed of 100 RPM in 500 mL of pH 6.1 phosphate buffer with 0.1% sodium lauryl sulfate (SLS) at 37°
    - C.±
      
      0.5°
      
      C., at least 80% of the meloxicam dissolves in a time period selected from;
      
      30 minutes or less;
      
      20 minutes or less;
      
      10 minutes or less;
      
      8 minutes or less;
      
      7 minutes or less;
      
      6 minutes or less; and
      
      5 minutes or less.
  - 8. The unit dosage form of claim 1 wherein the dissolution rate is such that, when tested using USP Apparatus 1 (baskets) set to rotation speed of 100 RPM in 500 mL of pH 6.1 phosphate buffer with 0.1% sodium lauryl sulfate (SLS) at 37°
    - C.±
      
      0.5°
      
      C., at least 90% of the meloxicam dissolves in a time period selected from;
      
      30 minutes or less;
      
      20 minutes or less;
      
      10 minutes or less;
      
      8 minutes or less;
      
      7 minutes or less;
      
      6 minutes or less; and
      
      5 minutes or less.
  - 9. The unit dosage form of claim 1, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a median plasma tmax of 1 to 3 hrs.
  - 10. The unit dosage form of claim 1, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma AUC (0-∞
    - ) that is 80% to 125% of 13610 ng-h/ml.
  - 11. The unit dosage form of claim 1, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma AUC (0-∞
    - ) that is 60% to 80% of the AUC (0-∞
      
      ) of 7.5 mg Mobic tablets.
  - 12. The unit dosage form of claim 1, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma Cmax that is 80% to 125% of the Cmax of 7.5 mg Mobic tablets.

13. A unit dosage form comprising 10 mg of meloxicam, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma AUC (0-∞
- ) of 16000-44000 h*ng/ml.
- View Dependent Claims (14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25)
- - 14. The unit dosage form of a claim 13, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean blood plasma Cmax of 700-1900 ng/ml.
  - 15. The unit dosage form of claim 13, wherein the particles of meloxicam have a median particle size, on a volume average basis, between 100 nm and 5000 nm.
  - 16. The unit dosage form of claim 13, wherein the D(0.9) of the particles of meloxicam is less than 3000 nm.
  - 17. The unit dosage form of claim 13, wherein the surface weighted mean diameter (D[3,2]) of the particles of meloxicam is between 100 nm and 800 nm.
  - 18. The unit dosage form of claim 13 wherein the volume weighted mean diameter (D[4,3]) of the particles of meloxicam is between 400 nm and 1300 nm.
  - 19. The unit dosage form of claim 13 wherein the dissolution rate is such that, when tested using USP Apparatus 1 (baskets) set to rotation speed of 100 RPM in 1000 mL of pH 6.1 phosphate buffer with 0.1% sodium lauryl sulfate (SLS) at 37°
    - C.±
      
      0.5°
      
      C., at least 80% of the meloxicam dissolves in a time period selected from;
      
      30 minutes or less;
      
      20 minutes or less;
      
      15 minutes or less;
      
      14 minutes or less;
      
      13 minutes or less;
      
      12 minutes or less;
      
      11 minutes or less;
      
      10 minutes or less; and
      
      5 minutes or less.
  - 20. The unit dosage form of claim 13 wherein the dissolution rate is such that, when tested using USP Apparatus 1 (baskets) set to rotation speed of 100 RPM in 1000 mL of pH 6.1 phosphate buffer with 0.1% sodium lauryl sulfate (SLS) at 37°
    - C.±
      
      0.5°
      
      C., at least 90% of the meloxicam dissolves in a time period selected from;
      
      30 minutes or less;
      
      20 minutes or less;
      
      15 minutes or less;
      
      14 minutes or less;
      
      13 minutes or less;
      
      12 minutes or less;
      
      11 minutes or less;
      
      10 minutes or less; and
      
      5 minutes or less.
  - 21. The unit dosage form of claim 13, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a median plasma tmax of 1 to 3 hrs.
  - 22. The unit dosage form of claim 13, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma AUC (0-∞
    - ) that is 80% to 125% of 29,173 ng-h/ml.
  - 23. The unit dosage form of claim 13, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma Cmax that is 80% to 125% of 1253 ng/ml.
  - 24. The unit dosage form of claim 13, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma AUC (0-∞
    - ) that is 60%-80% of the mean plasma AUC (0-∞
      
      ) of 15 mg Mobic tablets.
  - 25. The unit dosage form of claim 13, wherein a single dose, upon oral administration to a population of healthy adults in the fasted state, provides a mean plasma Cmax that is 80%-125% of the mean plasma Cmax of 15 mg Mobic tablets.

26. A unit dosage form of a pharmaceutical composition comprising 10 mg of meloxicam, wherein a single dose, upon oral administration to a population of healthy adults in the fed state, provides a mean plasma Cmax of 525-1500 ng/ml.
- View Dependent Claims (27, 28, 29, 30)
- - 27. The unit dosage form of claim 26, wherein a single dose, upon oral administration to a population of healthy adults in the fed state, provides a median plasma Tmax of 3 to 7 hrs.
  - 28. The unit dosage form of claim 26, wherein a single dose, upon oral administration to a population healthy adults in the fed state, provides a mean plasma AUC (0-∞
    - ) of 15000-42000 h*ng/ml.
  - 29. The unit oral dosage form of claim 26, wherein a single dose, upon oral administration to a population of healthy adults in the fed state, provides a mean plasma Cmax that is 80% to 125% of 974 ng/ml.
  - 30. The unit oral dosage form of claim 26, wherein a single dose, upon oral administration to a population of healthy adults in the fed state, provides a mean plasma AUC (0-∞
    - ) that is 80% to 125% of 27,146 ng/ml.

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Current Assignee
Iceutica Pty Limited (Assertio Holdings, Inc.)
Original Assignee
Iceutica Pty Limited (Assertio Holdings, Inc.)
Inventors
Bosch, H. William

Granted Patent

US 9,649,318 B2
Time in Patent Office

Days
Field of Search
US Class Current

1/1
CPC Class Codes

A61K 31/00   Medicinal preparations cont...

A61K 31/5415   ortho- or peri-condensed wi...

A61K 9/0053   Mouth and digestive tract, ...

A61K 9/14   Particulate form, e.g. powd...

A61K 9/145   with organic compounds

A61K 9/1617   Organic compounds, e.g. pho...

A61K 9/1623   Sugars or sugar alcohols, e...

A61K 9/1652   Polysaccharides, e.g. algin...

A61K 9/4858   Organic compounds

A61P 19/02   for joint disorders, e.g. a...

A61P 25/04   Centrally acting analgesics...

A61P 29/00   Non-central analgesic, anti...

Y10T 428/2982   Particulate matter [e.g., s...

Novel Formulation of Meloxicam

First Claim

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Novel Formulation of Meloxicam

First Claim

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Abstract

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