ARIPIPRAZOLE COMPOSITIONS AND METHODS FOR ITS TRANSDERMAL DELIVERY

• US 20130171237A1
• Filed: 11/05/2012
• Published: 07/04/2013
• Est. Priority Date: 10/28/2010
• Status: Abandoned Application

• Current Assignee: Aequus Pharmaceuticals, Inc.
• Original Assignee: Aequus Pharmaceuticals, Inc.
• Inventors: Plakogiannis, Fotios M., Hossain, Anwar Muhammed
• Application Number:
  US13/668,500
• Publication Number:
  US 20130171237A1
• Time in Patent Office: Days
• US Class Current: 424/450
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• 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
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61K 9/7023 Transdermal patches and similar drug-containing composite devices, e.g. cataplasms galenical aspects of iontophoretic devices A61K9/0009; microneedle arrays A61K9/0021; buccal patches A61K9/006
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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 pharmaceutical composition comprising aripiprazole in a dosage form for transdermal delivery, wherein the aripiprazole is in gel form, comprising:

aripiprazole in the amount of about 1 to 20% w/v;

a gelling agent in the range of about 0.1% to 5% w/v;

an enhancer selected from the group consisting of dimethylacetamide, dimethylformamide, decymethylsulfoxide, terpene and terpenoids, liposomes, niosomes, transferomes, ethanosomes, urea, lauric acid, myristc acid, and combinations thereof;

wherein the pH of the composition is maintained at approximately 6 to 7.

2. The pharmaceutical composition of claim 1 wherein the gelling agent is poloxamer.

3. The pharmaceutical composition of claim 1 wherein the form is a patch for transdermal delivery.

4. The pharmaceutical composition of claim 1 wherein the dosage form is an ointment, cream, emulsion, or liposome.

5. The pharmaceutical composition of claim 1 further comprising about 40% N-methyl-2-pyrrolidone, about 40% dimethylsulfoxide, about 15% alcohol, and about 5% water.

6. The pharmaceutical composition of claim 5, further comprising ingredients selected form the group consisting of isopropyl alcohol, isopropyl myristate, PEG, and combinations thereof.

7. A pharmaceutical composition comprising aripiprazole in a dosage form for transdermal delivery, wherein the aripiprazole is in liquid form, comprising:

aripiprazole present in the amount of 1 to 20% w/v;

an agent selected from the group consisting of an alcohol, glycol, mineral oil, vegetable oil, and combinations thereof,

an enhancer selected from the group consisting of dimethylacetamide, dimethylformamide, decymethylsulfoxide, terpene and terpenoids, liposomes, niosomes, transferomes, ethanosomes, urea, lauric acid, myristc acid, and combinations thereof;

wherein the pH of the composition is maintained at approximately 6 to 7.

8. The pharmaceutical composition of claim 7 wherein the form is a patch for transdermal delivery.

9. The pharmaceutical composition of claim 7 being in the dosage form of an ointment, cream, emulsion, or liposome.

10. The pharmaceutical composition of claim 7 further comprising about 40% N-methyl-2-pyrrolidone, about 40% dimethylsulfoxide, about 15% alcohol, and about 5% water.

11. The pharmaceutical composition of claim 10, further comprising ingredients selected form the group consisting of isopropyl alcohol, isopropyl myristate, PEG, and combinations thereof.

12. A pharmaceutical composition comprising aripiprazole in a dosage form for transdermal delivery, wherein the aripiprazole is in gel form, comprising:

aripiprazole in the amount of about 1 to 20% w/v;

a gelling agent in the range of about 0.1% to 5% w/v;

an enhancer selected from the group consisting of dimethylacetamide, dimethylformamide, decymethylsulfoxide, terpene and terpenoids, liposomes, niosomes, transferomes, ethanosomes, urea, lauric acid, myristc acid, and combinations thereof;

about 40% N-methyl-2-pyrrolidone, 40% dimethylsulfoxide, 15% alcohol and 5% water;

wherein the pH of the composition is maintained at approximately 6 to 7.

13. The pharmaceutical composition of claim 12, further comprising ingredients selected form the group consisting of isopropyl alcohol, isopropyl myristate, PEG, and combinations thereof.

14. A pharmaceutical composition comprising aripiprazole in a dosage form for transdermal delivery, wherein the aripiprazole is in liquid form, comprising:

aripiprazole present in the amount of 1 to 20% w/v;

an agent selected from the group consisting of an alcohol, glycol, mineral oil, vegetable oil, and combinations thereof,

an enhancer selected from the group consisting of dimethylacetamide, dimethylformamide, decymethylsulfoxide, terpene and terpenoids, liposomes, niosomes, transferomes, ethanosomes, urea, lauric acid, myristc acid, and combinations thereof;

about 40% N-methyl-2-pyrrolidone, about 40% dimethylsulfoxide, about 15% alcohol and about 5% water;

wherein the pH of the composition is maintained at approximately 6 to 7.

15. The pharmaceutical composition of claim 14, further comprising ingredients selected form the group consisting of isopropyl alcohol, isopropyl myristate, PEG, and combinations thereof.

16. A pharmaceutical composition comprising aripiprazole in a dosage form for transdermal delivery, wherein the aripiprazole is in gel form, comprising about 2% ARPZ;

about 25% DMSO;

about 10% NMP;

about 5% isopropyl alcohol (IPA);

about 40% Ethyl Alcohol;

about 15% PEG 400;

about 0.5% carbomer;

water q.s. to 100%.

17. The pharmaceutical composition of claim 16, wherein the pH of the composition is maintained at approximately 6 to 7.

18. A pharmaceutical composition comprising aripiprazole in a dosage form for transdermal delivery, wherein the aripiprazole is in liquid form, comprising about 2% ARPZ;

about 25% DMSO;

about 10% NMP;

about 5% isopropyl alcohol (IPA);

about 40% Ethyl Alcohol;

about 15% PEG 400;

about 0.5% carbomer;

water q.s. to 100%.

19. The pharmaceutical composition of claim 18, wherein the pH of the composition is maintained at approximately 6 to 7.