Pharmaceutical delivery systems

• US 4,944,949 A
• Filed: 12/17/1987
• Issued: 07/31/1990
• Est. Priority Date: 12/18/1986
• Status: Expired due to Fees

• Current Assignee: Cortec Corporation
• Original Assignee: TIL Medical Limited
• Inventors: Flynn, Michael J., Story, Michael J.
• Primary Examiner(s): Chaudhuri, Olik
• Assistant Examiner(s): Griffis, Andrew
• Application Number:
  US07/134,243
• Time in Patent Office: 957 Days
• Field of Search: 424/450, 424/451, 424/455, 424/456, 514/825, 514/937, 514/941
• US Class Current: 424/451
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61K 9/4858 Organic compounds

Abstract

Non-steroidal anti-inflammatory drugs (NSAIDs) including diclofenac, flufenamic acid, flurbiprofen, ibuprofen, indomethacin, ketoprofen, naproxen, phenylbutazone, piroxicam and sulindac are administered in micelles to alleviate their adverse effects on the gastrointestinal tract. The drugs are formulated with surfactants such as polyethoxylated nonionics to give micelle-forming compositions.

Claims

1. A method for the treatment of prophylaxis of inflammatory arthropathy, the method comprising the steps of:

providing a non-aqueous formulation of a non-steroidal anti-inflammatory drug and a surfactant, the formulation forming micelles containing the drug on oral administration; and

orally administering said formulation to a patient to be treated.

2. The method of claim 1, further comprising selecting said non-steroidal anti-inflammatory drug from the class consisting of diclofenac, flufenamic acid, flurbiprofen, ibuprofen, indomethacin, ketoprofen, naproxen, phenylbutazone, piroxicam and sulindac and mixtures thereof.

3. The method of claim 1, further comprising selecting a nonionic surfactant as said surfactant.

4. The method of claim 3, further comprising selecting from a polyoxyethylated surfactant as said nonionic surfactant.

5. The method of claim 4 further comprising selecting said surfactant from the class consisting of polyoxyethylated glycol monoethers, polyoxyethylated fatty acids, polyoxyethylated sorbitan fatty esters and polyoxyethylated castor oils.

6. The method of claim 4, further comprising selecting said nonionic surfactant from the class consisting of sorbitan fatty acid esters, poloxamers, polyethylene glycol fatty acid esters and polyethyoxylated glyceryl fatty acid esters and mixtures thereof.

7. The method of claim 1, further comprising selecting a surfactant having an HLB of 10 or above.

8. The method of claim 1, further comprising selecting a surfactant having an HLB of 12 or above.

9. The method of claim 1, further comprising providing said formulation in the form of a capsule.

10. The method of claim 1, further comprising providing said formulation in the form of a liquid.

11. The method of claim 1, further comprising providing said drug and surfactant in a weight ratio in the formulation in a range of from 1:

5.7 to 1;

50.

12. The method of claim 1, further comprising providing said drug and surfactant in a weight ratio in the formulation is in a range from 1:

6 to 1;

25.

13. The method of claim 1, further comprising providing said drug and surfactant in a weight ratio in the formulation is in a range of from 1:

6 to 1;

20.

14. The method of claim 1, further comprising providing said drug and surfactant in a weight ratio in the formulation is in a range of from 1:

8 to 1;

30.

15. The method of claim 1, further comprising providing said drug and surfactant in a weight ratio in the formulation is in a range of from 1:

10 to 1;

27.5.