STIMULATION OF OCULAR RETROBULBAR BLOOD FLOW USING OCULAR IRRITANTS

• US 20110014294A1
• Filed: 03/02/2009
• Published: 01/20/2011
• Est. Priority Date: 03/03/2008
• Status: Abandoned Application

• Current Assignee: PharmaLight Inc.
• Original Assignee: PharmaLight Inc.
• Inventors: Koevary, Steve B., Gross, Yossi
• Application Number:
  US12/920,458
• Publication Number:
  US 20110014294A1
• Time in Patent Office: Days
• US Class Current: 424/489
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/704 attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin digitoxin A61K31/7048
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• 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: A61P 3/02 Nutrients, e.g. vitamins, minerals
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives

Abstract

Disclosed are uses of an ocular irritant such as saponin in stimulating the retrobulbar blood flow of an eye. Disclosed are also methods of treatment including administration of a pharmaceutical composition including an ocular irritant to an eye, for example as a mist, in order to stimulate the retrobulbar blood flow. In some embodiments, the stimulation of the retrobulbar blood flow has a beneficial effect.

Claims

1-21. -21. (canceled)

22. A method of treating a condition associated with insufficient retrobulbar blood flow, the method comprising administering to an eye of a subject suffering from a condition associated with insufficient retrobulbar blood flow an effective amount of a pharmaceutical composition in the form of a mist consisting essentially of an ocular irritant and an ophthalmically-acceptable carrier, whereby the ocular irritant stimulates retrobulbar blood flow, thereby treating the condition.

23. The method of claim 22, wherein administering of the pharmaceutical composition in the form of a mist occurs with reduced, minimal or no irritation to the eye.

24. The method of claim 22, wherein administering comprises contacting an anterior surface of the eye with the mist.

25. The method of claim 24, wherein administering the mist leads to depositing an amount of the ocular irritant on a posterior surface of the eye effective in stimulating the retrobulbar blood flow.

26. The method of claim 22, wherein the pharmaceutical composition is substantially devoid of an active pharmaceutical ingredient other than the ocular irritant.

27. The method of claim 22, wherein the condition is selected from diabetic retinopathy, open angle glaucoma, ocular hypertension, macular degeneration, ocular ischemic syndrome, giant cell arteritis, eye occlusions, central retinal artery occlusion (CRAO), central retinal vein occlusion (CRVA), ischemic optic neuropathy, optic neuritis, neuromyelitis optica and neuroretinitis.

28. The method of claim 22, wherein the ocular irritant is selected from saponin, benzalkonium chloride or both.

29. The method of claim 22, wherein the mist comprises particles having a mean particle diameter of less than about 20 microns.

30. The method of claim 22, wherein the mist comprises particles having a mean particle diameter of less than about 5 microns.

31. A method of treatment, comprising:

a) providing a pharmaceutical composition consisting essentially of an ocular irritant and an ophthalmically-acceptable carrier;

b) generating a mist of said pharmaceutical composition; and

c) contacting said mist with a posterior surface of an eye of a subject in need thereof.

32. A pharmaceutical composition consisting essentially of an ocular irritant in an ophthalmically-acceptable carrier, the composition being adapted for administration to an eye as a mist and further adapted for stimulating retrobulbar blood flow.

33. The composition of claim 32, further adapted to cause reduced, minimal or no irritation to the eye.

34. The composition of claim 32, substantially devoid of an active pharmaceutical ingredient other than the ocular irritant.

35. The composition of claim 32, wherein the ocular irritant comprises saponin, benzalkonium chloride or both.

36. The composition of claim 32, wherein the mist comprises particles having a mean particle diameter of less than about 20 microns.

37. The composition of claim 32, wherein the mist comprises particles having a mean particle diameter of less than about 5 microns.

38. The composition of claim 32, further comprising at least one component selected from bioadhesives, buffering agents, chelating agents, humectants, pH-adjusting agents, preservatives, solubilizers, viscosity modifiers and vitamins.

39. A device for ophthalmic administration of a pharmaceutical composition as a mist, the device comprising:

a) a composition-reservoir configured to be functionally associated with a nebulizer; and

b) a pharmaceutical composition consisting essentially of an ocular irritant and an ophthalmically-acceptable carrier contained within said reservoir, said composition is adapted for stimulating retrobulbar blood flow in an eye to which administered as a mist.

40. The device of claim 39, further comprising:

c) a nebulizer configured to nebulize said composition contained in said composition-reservoir and to generate an ophthalmically administrable mist.

41. The device of claim 39, configured to produce a mist comprising particles having a mean particle diameter of less than about 20 microns.

42. The device of claim 39, configured to produce a mist comprising particles having a mean particle diameter of less than about 5 microns.

43. The device of claim 39, wherein said composition is further adapted to cause reduced, minimal or no irritation to the eye.

44. The device of claim 39, wherein said composition is substantially devoid of an active pharmaceutical ingredient other than the ocular irritant.

45. The device of claim 39, wherein said ocular irritant comprises saponin, benzalkonium chloride or both.