Topical compositions and methods of using the same

Patent metadata

Field	Value
Publication number	US-2016199295-A1
Application number	US-201414910207-A
Country	US
Kind code	A1
Filing date	Aug 8, 2014
Priority date	Aug 8, 2013
Publication date	Jul 14, 2016
Grant date	—

Abstract

The present invention generally relates to topical compositions and methods of using the same. A preferred topical pharmaceutical composition comprises a nitric oxide-releasing active pharmaceutical ingredient in admixture with a hydrophilic composition and a hydrophobic composition wherein the nitric oxide-releasing active pharmaceutical ingredient comprises a nitric oxide-releasing compound having a diazeniumdiolate functional group.

First claim

1 . A topical pharmaceutical composition comprising a nitric oxide-releasing active pharmaceutical ingredient in admixture with a hydrophilic composition and a hydrophobic composition,
wherein the hydrophobic composition comprises the nitric oxide-releasing active pharmaceutical ingredient and the nitric oxide-releasing active pharmaceutical ingredient comprises a nitric oxide-releasing compound having a diazeniumdiolate functional group.

2 . The topical pharmaceutical composition of claim 1 , wherein the hydrophilic composition comprises a solution, suspension, lotion, gel, cream, or hydrogel.

3 . (canceled)

4 . The topical pharmaceutical composition of claim 1 , wherein the hydrophilic composition has a pH of about 3 to about 8.

5 . The topical pharmaceutical composition of claim 1 , wherein the hydrophilic composition comprises a buffer, optionally a phosphate buffer.

6 . The topical pharmaceutical composition of claim 1 , wherein the hydrophilic composition comprises a polymer, optionally cellulose or a pharmaceutically acceptable salt thereof, chitosan, an acrylic acid polymer, or any combination thereof.

7 . The topical pharmaceutical composition of claim 1 , wherein the hydrophilic composition comprises a polyhydric alcohol.

8 - 9 . (canceled)

10 . The topical pharmaceutical composition of claim 1 , wherein the topical pharmaceutical composition is self-emulsifying.

11 . The topical pharmaceutical composition of claim 1 , wherein the composition has a viscosity of about 5000 cP to about 100,000 cP.

12 . (canceled)

13 . The topical pharmaceutical composition of claim 1 , wherein the topical pharmaceutical composition is continuous.

14 . The topical pharmaceutical composition of claim 1 , wherein the nitric oxide-releasing compound comprises a NO-releasing co-condensed silica particle.

15 . The topical pharmaceutical composition of claim 1 , wherein the topical pharmaceutical composition has a pH of about 3 to about 9.

16 . The topical composition of claim 1 , wherein the composition further comprises
a hydrophobic base; at least one of an amphiphilic compound or an emulsifying agent; a buffer; a polymer; a polyhydric alcohol; and water, and wherein the composition is buffered to a pH of about 3 to about 9.

17 . The topical pharmaceutical composition of claim 16 , wherein the nitric oxide-releasing active pharmaceutical ingredient, the hydrophobic base, and the at least one of the amphiphilic compound or the emulsifying agent are present in the hydrophobic composition and the buffer, the polymer, the polyhydric alcohol, and the water are present in the hydrophilic composition.

18 - 34 . (canceled)

35 . A kit comprising:
a first composition comprising a hydrophilic composition; and a second composition comprising an active pharmaceutical ingredient, wherein the active pharmaceutical ingredient comprises a nitric oxide-releasing compound having a diazeniumdiolate functional group.

36 . The kit of claim 35 , wherein the hydrophilic composition has a pH of about 4 to about 8.

37 . The kit of claim 35 , wherein the hydrophilic composition is a hydrogel, optionally a buffered hydrogel.

38 . The kit of claim 35 , wherein the hydrophilic composition comprises:
a phosphate buffer; a cellulose or a pharmaceutically acceptable salt thereof; a polyhydric alcohol; and water.

39 . The kit of claim 35 , wherein the second composition further comprises:
a hydrophobic base; and an amphiphilic compound.

40 . The kit of claim 35 , wherein the first composition and second composition are separately stored.

41 . A method of stably storing a diazeniumdiolate modified macromolecule in a hydrophobic composition and releasing nitric oxide from the diazeniumdiolate modified macromolecule, the method comprising:
admixing the hydrophobic composition with a hydrophilic composition to form an admixture, wherein the hydrophobic composition comprises the diazeniumdiolate modified macromolecule and the hydrophilic composition has a pH of about 4 to about 8.

42 - 48 . (canceled)

Assignees

• Novan Inc

Inventors

• Doxey Ryan
• Bao Jian

Classifications

• A61P31/00

  Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics · CPC title

• A61P17/02

  for treating wounds, ulcers, burns, scars, keloids, or the like · CPC title

• A61P17/00

  Drugs for dermatological disorders · CPC title

• A61K9/0014 Primary

  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 title

• A61K33/00 Primary

  Medicinal preparations containing inorganic active ingredients · CPC title