MOISTURE RESISTANT CONTAINER SYSTEMS FOR RAPIDLY BIOAVAILABLE DOSAGE FORMS

• US 20110105613A1
• Filed: 09/09/2009
• Published: 05/05/2011
• Est. Priority Date: 02/07/2006
• Status: Active Grant

• Current Assignee: APR Applied Pharma Research SA (RELIEF THERAPEUTICS Holding SA)
• Original Assignee: APR Applied Pharma Research SA (RELIEF THERAPEUTICS Holding SA)
• Inventors: Reiner, Giorgio, Reiner, Alberto
• Granted Patent: US 8,097,267 B2
• Time in Patent Office: Days
• US Class Current: 514/567
• CPC Class Codes: A61J 3/00 Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
• CPC Class Codes: A61K 31/195 having an amino group
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: B65B 1/04 Methods of, or means for, filling the material into the containers or receptacles

Abstract

Provided are rapidly bioavailable solid oral dosage forms of acute pain medications, and moisture resistant packaging that enables the formulation of such rapidly bioavailable dosage forms.

Claims

1. ) A method of packaging a rapidly bioavailable diclofenac potassium tablet comprising:

a) formulating a diclofenac potassium tablet dosage form for rapid bioavailability; and

b) packaging said dosage form in a moisture resistant bottle that prevents said doses from absorbing more than 4 wt. % moisture in three months when stored at 40°

C. and 75% relative humidity.

2. ) The method of claim 1 wherein said rapid bioavailability comprises a t_max of from about 5 to about 30 minutes, and a C_max of from about 1700 to about 2300 ng/ml.

3. ) The method of claim 1 wherein said rapid bioavailability comprises a t_max of from about 13 to about 27 minutes, and a C_max of from about 1500 to about 2500 ng/ml wherein said t_max exhibits an inter-subject variability of less than about 49%.

4. ) The method of claim 1 wherein said dosage form yields one C_max peak when orally ingested.

5. ) The method of claim 1 wherein said dosage form is characterized by a disintegration or 90% dissolution time of less than 10 minutes when tested according to USP 28 <

701>

or USP 28 <

711).

6. ) The method of claim 1 wherein said bottle comprises a foil seal at the cap and one or more dessicant pouches inside said bottle.

7. ) The method of claim 1 wherein said dosage form comprises about 50 mg. of diclofenac potassium.

8. ) The method of claim 1 wherein said dosage form comprises from about 7 to about 20 wt. % of an excipient that absorbs greater than about 1 wt. % water within a twenty four hour period in a humidity chamber maintained at 80% RH and 25 degrees Celcius.

9. ) The method of claim 1 wherein said dosage form absorbs greater than about 1 wt. % water within a twenty four hour period in a humidity chamber maintained at 80% RH and 25 degrees Celcius.

10. ) The method of claim 1 wherein said dosage form comprises at least 20 wt. % of one or more excipients that are freely soluble in water.

11. ) The method of claim 1 wherein said dosage form comprises at least 20 wt. % of mannitol, lactose, sucrose, or a combination thereof.

12. ) The method of claim 1 wherein said dosage form comprises a surfactant.

13. ) The method of claim 1 wherein said dosage form comprises a surfactant having an HLB greater than 14.

14. ) The method of claim 1 wherein said dosage form comprises sodium lauryl sulfate.

15. ) The method of claim 1 wherein said dosage form comprises from about 30 to about 80 wt. % of a hygroscopic diluent and a freely soluble diluent at a weight ratio of from about 1:

20 to about 5;

1.

16. ) The method of claim 1 wherein said dosage form comprises means for generating a gaseous and alkaline environment for said diclofenac potassium when orally ingested into the stomach.

17. ) The method of claim 1 wherein said dosage form comprises an alkali metal carbonate or bicarbonate.

18. ) The method of claim 1 wherein said dosage form comprises an excipient base that is characterized by an inverse relationship between disintegration rate and moisture uptake.

19. ) A method of packaging a rapidly bioavailable diclofenac potassium solid oral dosage form comprising:

a) formulating a diclofenac potassium solid oral dosage form for rapid bioavailability; and

b) packaging said dosage form in a moisture resistant bottle that prevents said dosage form from absorbing more than 4 wt. % moisture in three months when stored at 40°

C. and 75% relative humidity.

20. ) A method of treating acute pain comprising:

a) providing a diclofenac potassium solid oral dosage form that is characterized by;

i) rapid bioavailability; and

ii) a moisture resistant bottle that prevents said dosage form from absorbing more than 4 wt. % moisture in three months when stored at 40°

C. and 75% relative humidity; and

b) administering said dosage form to a patient suffering from acute pain.