Aripiprazole compositions and methods for its transdermal delivery

• US 9,757,374 B2
• Filed: 08/13/2015
• Issued: 09/12/2017
• Est. Priority Date: 10/28/2010
• Status: Active Grant

• Current Assignee: Alpha To Omega Pharmaceutical Consultants, Inc.
• Original Assignee: Aequus Pharmaceuticals, Inc.
• Inventors: Plakogiannis, Fotios M., Hossain, Muhammed Anwar
• Primary Examiner(s): Maewall, Snigdha
• Application Number:
  US14/825,318
• Publication Number:
  US 20150342949A1
• Time in Patent Office: 761 Days
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00

Abstract

The present invention discloses compositions of liquid and gel formulation containing aripiprazole in the form of a patch for transdermal delivery.

Claims

1. A transdermal pharmaceutical composition comprising aripiprazole about 7%, Carbopol about 5%, DMSO about 40%, Ethanol about 25%, Lactic acid about 5%, N-methyl-2-pyrrolidone (NMP) about 1.75%, Oleic acid about 4%, propylene glycol (PG) about 7.25%, and q.s. water.

2. The transdermal pharmaceutical composition of claim 1 wherein the aripiprazole is in a gel or liquid form.

3. The transdermal pharmaceutical composition of claim 1 wherein the pH of the composition is approximately 6 to 7.

16. A method of treating schizophrenia in patient in need of such treatment comprising:

selecting a patient in need of treatment for schizophrenia;

administering the pharmaceutical composition of claim 1,

thereby treating schizophrenia.

4. A transdermal pharmaceutical composition comprising aripiprazole about 7%, Klucel (hydroxypropylcellulose (HPC)) about 2%, DMSO about 40%, Ethanol about 25%, Lactic acid about 5%, N-methyl-2-pyrrolidone (NMP) about 1.75%, Oleic acid about 4%, propylene glycol about 10.25%, and q.s. water.

5. The transdermal pharmaceutical composition of claim 4 wherein the aripiprazole is in a gel or liquid form.

6. The transdermal pharmaceutical composition of claim 4 wherein the pH of the composition is approximately 6 to 7.

7. A transdermal pharmaceutical composition comprising aripiprazole about 7%, Klucel (hydroxypropylcellulose (HPC)) about 4%, DMSO about 5%, Ethanol about 5%, isopropyl myristate (IPM) about 1.5%, Oleic acid about 23%, Lactic acid about 6%, PG about 23.5%, Polyethylene glycol (PEG)—

20%, and Glycerin about 5%.

8. The transdermal pharmaceutical composition of claim 7 wherein the aripirazole is in a gel or liquid form.

9. The transdermal pharmaceutical composition of claim 7 wherein the pH of the composition is approximately 6 to 7.

10. A transdermal pharmaceutical composition comprising aripiprazole about 7%, DMSO about 40%, N-methyl-2-pyrrolidone (NMP) about 1.75%, propylene glycol (PG)—

10.25%, Ethanol about 16%, Lactic acid about 5%, Terpineol about 10%, Oleic acid about 2%, Water about 5%, and Carbopol about 3%.

11. The transdermal pharmaceutical composition of claim 10 wherein the aripiprazole is in a gel or liquid form.

12. The transdermal pharmaceutical composition of claim 10 wherein the pH of the composition is approximately 6 to 7.

13. A transdermal pharmaceutical composition comprising aripiprazole about 7%, DMSO about 40%, N-methyl-2-pyrrolidone (NMP) about 1.75%, propylene glycol (PG) about 9.25%, Ethanol about 25%, Lactic acid about 5%, Oleyl alcohol about 4%, Water about 5%, and Carbopol about 3%.

14. The transdermal pharmaceutical composition of claim 13 wherein the aripiprazole is in a gel or liquid form.

15. The transdermal pharmaceutical composition of claim 13 wherein the pH of the composition is approximately 6 to 7.