Methods and means for drug administration

• US 5,952,378 A
• Filed: 06/05/1997
• Issued: 09/14/1999
• Est. Priority Date: 08/24/1994
• Status: Expired due to Fees

• Current Assignee: Pharmacia & Upjohn AB (Pharmacia Corp.)
• Original Assignee: Pharmacia & Upjohn AB (Pharmacia Corp.)
• Inventors: Selen, Goran, Stjernschantz, Johan
• Primary Examiner(s): FAY, ZOHREH A
• Application Number:
  US08/793,043
• Time in Patent Office: 831 Days
• Field of Search: 514/530, 514/573, 514/912
• US Class Current: 514/530
• CPC Class Codes: A61K 31/5575 having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics

Abstract

Method and means for delivery of drugs to the optic nerve head and the region surrounding it which comprises contacting the surface of the eye with an effective amount of a drug for treatment of said nerve head and a physiologically acceptable prostaglandin or prostaglandin derivative for enhancing delivery of the drug to the nerve head, in an opththalmologically acceptable carrier.

Claims

1. Method for delivery of drugs to the optic nerve head of an eye and its surrounding region, comprising contacting the surface of the eye with an effective amount of a drug for treatment of the optic nerve head and a physiologically acceptable prostaglandin or prostaglandin derivative for enhancing delivery of the drug to the optic nerve head, in opthalmologically acceptable carrier.

2. Method according to claim 1 wherein a composition comprising the prostaglandin or prostaglandin derivative is administered prior to a composition comprising the drug.

3. Method according to claim 1 wherein the prostaglandin or prostaglandin derivative is of the F-type.

4. Method according to claim 1 wherein the prostaglandin or prostaglandin derivative is an ester.

9. Method according to claim 1, wherein the prostaglandin is of class PGF₂α

.

10. Method according to claim 1, wherein the prostaglandin derivative is 13,14-dihydro-17-phenyl-18,19,20-trinor-PGF₂α

-isopropyl ester.

11. Method according to claim 1, wherein the drug for treatment of the optic nerve head comprises a neuroprotective agent, a growth factor or a vasoactive agent.

13. Method according to claim 1, wherein the drug for treatment of the optic nerve head is selected from the group consisting of calcium antagonists, angiotensin converting enzyme blockers, phosphodiesterase blockers, nitrates and nitric oxide generators, alpha 1-adrenergic receptor blockers, smooth muscle relaxing agents, agents for the treatment of vascular disease, beta adrenergic agonists, anticholinergic agents, central nervous system active agents, antioxidants, radical scavengers, dopaminergic agents, serotoninergic agents, monoamine oxidase inhibitors, anti-inflammatory agents, growth factors, neuropeptides and transglutaminase affecting agents.

15. Method according to claim 1, wherein the drug for treatment of the optic nerve head comprises a calcium antagonist.

17. Method according to claim 1, wherein the prostaglandin or prostaglandin derivative is administered in an amount of about 0.1-100 μ

g.

5. A method for enhancing delivery of a drug to the optic nerve head for treatment of diseases in the optic nerve head region in the eye, comprising contacting the eye with a physiologically acceptable prostaglandin or prostaglandin derivative and contacting the eye with the drug.

6. Method according to claim 5, wherein the prostaglandin is of class PGF₂α

.

7. Method according to claim 6, wherein the prostaglandin is an ester.

8. Method according to claim 7, wherein the prostaglandin derivative is 13,14-dihydro-17-phenyl-18,19,20-trinor-PGF₂α

-isopropyl ester.

12. Method according to claim 5, wherein the drug for treatment of the optic nerve head comprises a neuroprotective agent, a growth factor or a vasoactive agent.

14. Method according to claim 5, wherein the drug for treatment of the optic nerve head is selected from the group consisting of calcium antagonists, angiotensin converting enzyme blockers, phosphodiesterase blockers, nitrates and nitric oxide generators, alpha 1-adrenergic receptor blockers, smooth muscle relaxing agents, agents for the treatment of vascular disease, beta adrenergic agonists, anticholinergic agents, central nervous system active agents, antioxidants, radical scavengers, dopaminergic agents, serotoninergic agents, monoamine oxidase inhibitors, anti-inflammatory agents, growth factors, neuropeptides and transglutaminase affecting agents.

16. Method according to claim 5, wherein the drug for treatment of the optic nerve head comprises a calcium antagonist.

18. Method according to claim 5, wherein the prostaglandin or prostaglandin derivative is administered in an amount of about 0.1-100 μ

g.

19. A method for increasing the permeability of a drug in the ciliary muscle to enhance the diffusion of the drug into the suprachoroidal space of the eye to treat the optic nerve head, comprising contacting the surface of the eye with a psychologically acceptable prostaglandin or prostaglandin derivative and contacting the eye with the drug.