US2019240151A1PendingUtilityA1

Vasoconstriction compositions and methods of use

70
Assignee: EYE THERAPIES LLCPriority: Aug 1, 2008Filed: Nov 2, 2018Published: Aug 8, 2019
Est. expiryAug 1, 2028(~2 yrs left)· nominal 20-yr term from priority
Inventors:Gerald Horn
A61P 9/00A61P 9/10A61P 43/00A61P 27/02A61P 27/00A61P 23/02A61P 11/00A61K 31/498A61K 45/06A61K 9/08A61K 9/0048A61K 31/44A61K 9/0043
70
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Claims

Abstract

The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.

Claims

exact text as granted — not AI-modified
1 .- 13 . (canceled) 
     
     
         14 . A method of reducing ocular redness in a subject in need thereof comprising administering to the ocular surface a single drop of an ophthalmic formulation comprising brimonidine as the sole active ingredient at a concentration less than 0.07%, wherein the ophthalmic formulation is administered no more than 4 time a day. 
     
     
         15 . The method of  claim 14 , wherein the brimonidine is at a concentration less than 0.05%. 
     
     
         16 . The method of  claim 14 , wherein the brimonidine is at a concentration less than 0.03%. 
     
     
         17 . The method of  claim 14 , wherein the brimonidine is at a concentration of about between 0.005% to 0.05%. 
     
     
         18 . The method of  claim 14 , wherein the brimonidine is at a concentration of about between 0.001% to 0.05%. 
     
     
         19 . The method of  claim 14 , wherein the brimonidine is at a concentration of about between 0.001% to 0.025%. 
     
     
         20 . The method of  claim 14 , wherein the brimonidine is at a concentration of about 0.025%. 
     
     
         21 . The method of  claim 14 , wherein the ophthalmic formulation comprises an electrolyte or preservative. 
     
     
         22 . The method of  claim 14 , wherein the ophthalmic formulation comprises one or more of sodium chloride, magnesium ions, mannitol, carboxymethyl cellulose hyaluronic acid, glycerin, potassium chloride, calcium chloride, benzalkonium chloride, or water. 
     
     
         23 . The method of  claim 14 , wherein the ophthalmic formulation comprises glycerin, potassium chloride, calcium chloride, benzalkonium chloride, and water 
     
     
         24 . The method of  claim 14 , wherein the ophthalmic formulation comprises a buffering agent. 
     
     
         25 . The method of  claim 24 , wherein the buffering agent is citrate. 
     
     
         26 . The method of  claim 14 , wherein the ophthalmic formulation has a pH of about between 5.0-7.8. 
     
     
         27 . The method of  claim 14 , wherein the drop is no more than 50 μL. 
     
     
         28 . A method of reducing ocular redness in a subject in need thereof comprising administering to the ocular surface a single drop of an ophthalmic formulation comprising brimonidine as the sole active ingredient at a concentration less than 0.07%, wherein said administration does not result in ocular ischemia. 
     
     
         29 . The method of  claim 28 , wherein the brimonidine is at a concentration less than 0.05%. 
     
     
         30 . The method of  claim 28 , wherein the brimonidine is at a concentration less than 0.03%. 
     
     
         31 . The method of  claim 28 , wherein the brimonidine is at a concentration of about between 0.005% to 0.05%. 
     
     
         32 . The method of  claim 28 , wherein the brimonidine is at a concentration of about between 0.001% to 0.05%. 
     
     
         33 . The method of  claim 28 , wherein the brimonidine is at a concentration of about between 0.001% to 0.025%. 
     
     
         34 . The method of  claim 28 , wherein the brimonidine is at a concentration of about 0.025%. 
     
     
         35 . The method of  claim 28 , wherein the ophthalmic formulation is administered no more than 4 time a day. 
     
     
         36 . The method of  claim 28 , wherein the ophthalmic formulation comprises an electrolyte or preservative. 
     
     
         37 . The method of  claim 28 , wherein the ophthalmic formulation comprises one or more of sodium chloride, magnesium ions, mannitol, carboxymethyl cellulose hyaluronic acid, glycerin, potassium chloride, calcium chloride, benzalkonium chloride, or water. 
     
     
         38 . The method of  claim 28 , wherein the ophthalmic formulation comprises glycerin, potassium chloride, calcium chloride, benzalkonium chloride, and water 
     
     
         39 . The method of  claim 28 , wherein the ophthalmic formulation comprises a buffering agent. 
     
     
         40 . The method of  claim 39 , wherein the buffering agent is citrate. 
     
     
         41 . The method of  claim 28 , wherein the ophthalmic formulation has a pH of about between 5.0-7.8. 
     
     
         42 . The method of  claim 28 , wherein the drop is no more than 50 μL. 
     
     
         43 . A method of reducing ocular redness in a subject in need thereof comprising administering to the ocular surface a single drop of an ophthalmic formulation comprising as the sole active ingredient at a concentration less than 0.07% wherein said administration is not within 24 hrs. prior to or after the subject has had an ocular surgery. 
     
     
         44 . The method of  claim 43 , wherein the brimonidine is at a concentration less than 0.05%. 
     
     
         45 . The method of  claim 43 , wherein the brimonidine is at a concentration less than 0.03%. 
     
     
         46 . The method of  claim 43 , wherein the brimonidine is at a concentration of about between 0.005% to 0.05%. 
     
     
         47 . The method of  claim 43 , wherein the brimonidine is at a concentration of about between 0.001% to 0.05%. 
     
     
         48 . The method of  claim 43 , wherein the brimonidine is at a concentration of about between 0.001% to 0.025%. 
     
     
         49 . The method of  claim 43 , wherein the brimonidine is at a concentration of about 0.025%. 
     
     
         50 . The method of  claim 43 , wherein the ophthalmic formulation is administered no more than 4 time a day. 
     
     
         51 . The method of  claim 43 , wherein the ophthalmic formulation comprises an electrolyte or preservative. 
     
     
         52 . The method of  claim 43 , wherein the ophthalmic formulation comprises one or more of sodium chloride, magnesium ions, mannitol, carboxymethyl cellulose hyaluronic acid, glycerin, potassium chloride, calcium chloride, benzalkonium chloride, or water. 
     
     
         53 . The method of  claim 43 , wherein the ophthalmic formulation comprises a buffering agent. 
     
     
         54 . The method of  claim 53 , wherein the buffering agent is citrate. 
     
     
         55 . The method of  claim 43 , wherein the ophthalmic formulation has a pH of about between 5.0-7.8. 
     
     
         56 . The method of  claim 43 , wherein the drop is no more than 50 μL. 
     
     
         57 . A formulation comprising 0.025% brimonidine as the sole active ingredient, glycerin, potassium chloride, calcium chloride dehydrate, benzalkonium chloride, water wherein said formulation is suitable for administration to the ocular surface. 
     
     
         58 . The formulation of  claim 57 , wherein administration does not result in ocular ischemia. 
     
     
         59 . The formulation of  claim 57 , wherein the formulation has a pH of about between 5.0-7.8. 
     
     
         60 . A formulation comprising 0.09% or less brimonidine as the sole active ingredient and one or more of a surfactant, electrolyte, or preservative. 
     
     
         61 . A formulations of  claim 60 , wherein the formulation comprises 0.05% or less brimonidine. 
     
     
         62 . A formulations of  claim 60 , wherein the formulation comprises 0.025% or less brimonidine 
     
     
         63 . The formulation of  claim 60 , wherein the formulation comprises one or more of sodium chloride, magnesium ions, mannitol, carboxymethyl cellulose hyaluronic acid, glycerin, potassium chloride, calcium chloride, benzalkonium chloride, or water wherein said formulation is suitable for administration to the ocular surface. 
     
     
         64 . The formulation of  claim 60 , wherein the formulation comprises a buffering agent. 
     
     
         65 . The formulation of  claim 60 , wherein the buffering agent is citrate. 
     
     
         66 . The formulation of  claim 60 , wherein the formulation has a pH of about between 5.0-7.8.

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