CONTROLLED RELEASE COMPOSITIONS OF TIZANIDINE

• US 20080214629A1
• Filed: 01/16/2008
• Published: 09/04/2008
• Est. Priority Date: 02/09/2007
• Status: Active Grant

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Gupta, Suneel, Bull, Scott, Donley, Rhea, Modi, Nishit, Yam, Noymi
• Granted Patent: US 8,524,749 B2
• Time in Patent Office: Days
• US Class Current: 514/362
• CPC Class Codes: A61K 31/433 Thidiazoles
• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system

Abstract

The present invention relates to a novel controlled release formulations of tizanidine. The invention also provides methods of using novel controlled release formulations of tizanidine to treat a patient.

Claims

1. A method of treating a patient suffering from spasticity, wherein said method comprises administering a dosage form comprising 6-20 mg of tizanidine wherein said tizanidine is released in manner such that tizanidine plasma drug concentration substantially ascends over a period of 8 hours following administration.

2. The methof of claim 1, wherein said dosage form provides said patient with a tizanidine peak blood concentration of between 1-4 ng/ml.

3. The method of claim 1, wherein said dosage form provides said patient with a tizanidine peak blood concentration of between 1.6-3.2 ng/ml.

4. The method of claim 1, wherein said tizanidine is tizanidine succinate.

5. A pharmaceutical composition comprising a first layer of tizanidine and a second layer of tizanidine wherein said first layer is substantially released within 3 hours of administration and said second layer of tizanidine is substantially released over a period of 1-14 hours.

6. The pharmaceutical composition of claim 5, wherein said first layer of tizanidine comprises between 5 and 25% of the tizanidine in said pharmaceutical composition.

7. The pharmaceutical composition of claim 5, wherein said second layer of tizanidine comprises between 75 and 95% of the tizanidine in said pharmaceutical composition.

8. The method of claim 5, wherein said tizanidine is tizanidine succinate.

9. The pharmaceutical composition of claim 5, wherein said pharmaceutical composition is in the form of an osmotic drug delivery system.

10. A pharmaceutical composition for administration to a patient comprising a first layer of tizanidine of tizanidine and a second layer of tizanidine of tizanidine wherein said administration of said pharmaceutical composition results in patient peak plasma blood levels of between 1-4 ng/ml between 3-12 hours after administration.

11. A pharmaceutical composition for administration to a patient comprising an immediate release portion of tizanidine and a controlled release portion of tizanidine wherein said administration of said pharmaceutical composition results in patient peak plasma blood levels of between 1.6-3.2 ng/ml between 3-12 hours after administration.

12. A pharmaceutical composition for administration to a patient comprising first layer of tizanidine and a second layer of tizanidine wherein said pharmaceutical composition contains between 6-20 mg of tizanidine.

13. A method of treating a condition which is responsive to tizanidine, the method comprising orally administering a tizanidine dosage form that produces a substantially increasing plasma tizanidine concentration following dosage administration.