Multimorphic ophthalmic preparations and treatments
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- UNIV OF UTAH RES FOUND
- Filing Date
- 2026-02-27
- Publication Date
- 2026-06-16
Smart Images
Figure 2026097904000001_ABST
Abstract
Claims
1. A method for treating or preventing the progression of myopia, The treatment includes the step of administering a therapeutically effective amount of the ophthalmic composition to the subject's eye during the treatment period. The aforementioned ophthalmic composition is A sufficient amount of corneal crosslinking agents and secondary treatment agents to treat myopic progression, and A method comprising the ophthalmic composition comprising a pharmaceutically acceptable carrier.
2. A method according to claim 1, wherein the ophthalmic composition is formulated as one of a solution, suspension, emulsion, gel, hydrogel, thermoresponsive gel, depot, film, gelled suspension, contact lens, or puncture plug.
3. A method according to claim 1, wherein the ophthalmic composition is formulated as a sustained-release composition configured to release the copper-containing agent and the secondary therapeutic agent over a period of about 2 days to about 6 months.
4. A method according to claim 3, wherein the administration is carried out by placing the composition in a sac-like portion of the eyeball, placing the composition in the conjunctival vestibule of the eyeball, and placing the composition in the subtenon space of the eyeball.
5. A method according to claim 3, wherein the ophthalmic composition is configured to deliver an average of about 0.0001 μg to about 5500 μg of copper per day to the eyes of the subject.
6. A method according to claim 3, wherein the ophthalmic composition is configured to deliver an average of about 0.01 μg to about 200 μg of the secondary therapeutic agent to the eyes of the subject per day.
7. The method according to claim 1, wherein the secondary therapeutic agent is present in the composition in an amount of about 0.0005 wt% to about 2 wt%.
8. The method according to claim 1, wherein the secondary therapeutic agent is present in the composition in an amount of about 0.001 wt% to about 1 wt%.
9. The composition according to claim 1, wherein the amount of the secondary therapeutic agent present in the composition is about 0.001 mg / ml to about 20 mg / ml.
10. The method according to claim 1, wherein the secondary therapeutic agent is a member selected from the group consisting of atropine, homatropine, cyclopentolate, pirenzepine, 7-methylxanthanine, and combinations thereof.
11. The method according to claim 1, wherein the corneal crosslinking agent is a copper-containing compound that provides copper in an amount of about 0.000001 wt% to about 15 wt% of the composition.
12. The method according to claim 1, wherein the corneal crosslinking agent is a copper-containing compound that provides an amount of copper of about 0.00001 mg / ml to about 1 mg / ml.
13. The method according to claim 1, wherein the corneal crosslinking agent is a copper-containing compound that provides copper in an amount of about 0.015 mg / ml to about 0.15 mg / ml.
14. The method according to claim 1, wherein the corneal crosslinking agent is a copper-containing compound selected from the group consisting of copper sulfate, copper carbonate, copper acetate, copper chloride, copper hydroxide, copper gluconate, copper bromide, copper fluoride, copper nitrate, copper iodide, copper perchlorate, copper molybdate, copper thiocyanate, copper tartrate, copper tetrafluoroborate, copper selenate, copper pyrophosphate, GHK-copper, copper tetraamine sulfate, copper histidine, copper glycinate, and combinations thereof.
15. The method according to claim 1, wherein the pharmaceutically acceptable carrier comprises at least one of a tonic, a solubilizer, a thickener, a polymer, a buffer, a preservative, a pH adjuster, and water.
16. A method according to claim 1, wherein the composition has a tonicity of about 200 mOsm / kg to about 600 mOsm / kg.
17. The method according to claim 1, wherein the composition has a pH of about 5.5 to about 8.
5.
18. The method according to claim 1, wherein the ophthalmic composition is formulated as eye drops and delivered in a container adapted to dispense the composition in a droppery manner in a droppery volume of about 5 μl to about 100 μl.
19. A method according to claim 18, wherein the dosage form provides about 0.0001 μg to about 500 μg of copper per drop of the ophthalmic composition.
20. The method according to claim 1, wherein the composition is administered to the eye in need at 1 to 4 time points per day.
21. A method according to claim 20, wherein about 5 μl to about 100 μl of the composition is administered at each time point.
22. A method according to claim 1, wherein the composition is administered in conjunction with an ophthalmoplasty device configured to reshape an elongated myopic eye.
23. The method according to claim 1, wherein the subject is a human subject having an age of approximately 3 to approximately 25 years.
24. The method according to claim 1, wherein the treatment period is approximately 6 months to approximately 5 years.
25. An ophthalmic composition for treating myopia progression, A sufficient amount of corneal crosslinking agents and secondary treatments to treat myopic progression, and A pharmaceutically acceptable carrier, An ophthalmic composition containing [the specified ingredient].
26. The composition according to claim 25, wherein the ophthalmic composition is formulated as one of a solution, suspension, emulsion, gel, hydrogel, thermoresponsive gel, depot, film, gelled suspension, contact lens, or puncture plug.
27. The composition according to claim 25, wherein the ophthalmic composition is formulated as a sustained-release composition configured to release the corneal crosslinking agent and the secondary therapeutic agent over a period of about 2 days to about 6 months.
28. The composition according to claim 27, wherein the ophthalmic composition is configured to deliver an average of about 0.0001 μg to about 500 μg of copper per day to the eyes of the subject.
29. The composition according to claim 27, wherein the ophthalmic composition is configured to deliver an average of about 0.0 μg to about 200 μg of the secondary therapeutic agent to the eyes of the subject per day.
30. The composition according to claim 25, wherein the secondary therapeutic agent is present in an amount of about 0.0005 wt% to about 2 wt%.
31. The composition according to claim 25, wherein the secondary therapeutic agent is present in an amount of about 0.001 wt% to about 1 wt%.
32. The composition according to claim 25, wherein the amount of the secondary therapeutic agent present in the composition is about 0.001 mg / ml to about 20 mg / ml.
33. The composition according to claim 25, wherein the secondary therapeutic agent is a member selected from the group consisting of atropine, homatropine, cyclopentolate, pirenzepine, 7-methylxanthanine, and combinations thereof.
34. The composition according to claim 25, wherein the corneal crosslinking agent is a copper-containing agent and is present in an amount of about 0.000001 wt% to about 15 wt%.
35. The composition according to claim 25, wherein the corneal crosslinking agent is a copper-containing agent that provides the composition with an amount of copper of about 0.00001 mg / ml to about 1 mg / ml.
36. The composition according to claim 25, wherein the corneal crosslinking agent is selected from the group consisting of copper sulfate, copper carbonate, copper acetate, copper chloride, copper hydroxide, copper gluconate, copper bromide, copper fluoride, copper nitrate, copper iodide, copper perchlorate, copper molybdate, copper thiocyanate, copper tartrate, copper tetrafluoroborate, copper selenate, copper pyrophosphate, GHK-copper, copper tetraamine sulfate, copper histidine, copper glycinate, and combinations thereof.
37. The composition according to claim 25, wherein the pharmaceutically acceptable carrier comprises at least one of a tonic, a solubilizer, a thickener, a polymer, a buffer, a preservative, a pH adjuster, and water.
38. The composition according to claim 25, wherein the composition has a tonicity of about 200 mOsm / kg to about 600 mOsm / kg.
39. The composition according to claim 25, wherein the composition has a pH of about 5.5 to about 7.
8.
40. A composition according to claim 25, wherein the composition further comprises an additional active ingredient.
41. It is a topical ophthalmic dosage form, An ophthalmic composition according to any one of claims 25 to 40, wherein the composition is formulated as eye drops and delivered in a container adapted to dispense the composition in a droppery manner in a droppery volume of about 5 μl to about 100 μl.
42. A dosage form according to claim 41, wherein each drop of the dosage form provides approximately 0.0001 μg to approximately 500 μg of copper.
43. The dosage form according to claim 41, wherein the dosage form provides a secondary therapeutic agent in an amount of about 0.01 μg to about 200 μg per drop of the ophthalmic composition.
44. The dosage form according to claim 41, wherein the container is adapted to dispense the composition in a dropper volume of about 5 μl to about 100 μl.
45. The use of corneal crosslinking agents and secondary therapeutic agents in the preparation of ophthalmic pharmaceuticals that treat myopia progression by increasing corneal lysyl oxidase activity, at least, when administered to the eyes of subjects in a therapeutically effective amount during the treatment period.
46. The use according to claim 45, wherein the ophthalmic drug is formulated as one of a solution, suspension, emulsion, gel, hydrogel, thermoresponsive gel, depot, film, gelled suspension, contact lens, or puncture plug.
47. The use according to claim 45, wherein the ophthalmic drug is formulated as a sustained-release composition configured to release the copper-containing agent and the secondary therapeutic agent over a period of about 2 days to about 6 months.
48. The use according to claim 47, wherein the administration is carried out by one or more of the following: placement of the composition in the sac-like portion of the eyeball, placement of the composition in the conjunctival vestibule of the eyeball, and placement of the composition in the subtenon space of the eyeball.
49. The use according to claim 47, wherein the ophthalmic composition is configured to deliver an average of about 0.0001 μg to about 5500 μg of copper per day to the eyes of the subject.
50. The use according to claim 47, wherein the ophthalmic composition is configured to administer an average of about 0.01 μg to about 200 μg of the secondary therapeutic agent to the eyes of the subject per day.
51. The use according to claim 47, wherein the secondary therapeutic agent is present in the composition in an amount of about 0.0005 wt% to about 2 wt%.
52. The use according to claim 45, wherein the secondary therapeutic agent is present in the composition in an amount of about 0.001 wt% to about 1 wt%.
53. The use described in claim 45, wherein the amount of the secondary therapeutic agent present in the composition is approximately 0.001 mg / ml to approximately 20 mg / ml.
54. The use according to claim 45, wherein the secondary therapeutic agent is a member selected from the group consisting of atropine, homatropine, cyclopentolate, pirenzepine, 7-methylxanthanine, and combinations thereof.
55. In the use described in claim 45, the corneal crosslinking agent is a copper-containing agent present in the composition in an amount of about 0.000001 wt% to about 15 wt%.
56. In the use described in claim 45, the corneal crosslinking agent is a copper-containing agent that provides an amount of copper of about 0.00001 mg / ml to about 1 mg / ml.
57. In the use according to claim 45, the corneal crosslinking agent is selected from the group consisting of copper sulfate, copper carbonate, copper acetate, copper chloride, copper hydroxide, copper gluconate, copper bromide, copper fluoride, copper nitrate, copper iodide, copper perchlorate, copper molybdate, copper thiocyanate, copper tartrate, copper tetrafluoroborate, copper selenate, copper pyrophosphate, GHK-copper, copper tetraamine sulfate, copper histidine, copper glycinate, and combinations thereof.
58. The use according to claim 45, wherein the pharmaceutically acceptable carrier comprises at least one of a tonic, a solubilizer, a thickener, a polymer, a buffer, a preservative, a pH adjuster, and water.
59. In the use described in claim 45, the agent has a tonic property of about 200 mOsm / kg to about 600 mOsm / kg.
60. The use according to claim 45, wherein the pH of the agent is approximately 5.5 to approximately 8.
5.
61. The use according to claim 45, wherein the agent further comprises an additional active ingredient.
62. In the use described in claim 45, the ophthalmic drug is formulated as eye drops and delivered in a container adapted to dispense the composition in a droppery manner at a droppery volume of approximately 5 μl to approximately 100 μl.
63. In the use described in claim 62, the dosage form provides about 0.0001 μg to about 500 μg of copper per drop of the ophthalmic composition.
64. The use according to claim 45, wherein the drug is administered to the eye in need at one to four time points per day.
65. The use according to claim 64, wherein about 5 μl to about 100 μl of the composition is administered at each time point.
66. The use according to claim 45, wherein the agent is administered in connection with an ophthalmoplastic device configured to reshape an elongated myopic eye.
67. The use described in claim 45, wherein the subject is a human subject aged approximately 3 to approximately 25 years.
68. The use described in claim 45, wherein the treatment period is approximately 6 months to approximately 5 years.
69. An ophthalmic composition used in a method for treating or preventing the progression of myopia, wherein the method is: The treatment includes the step of administering a therapeutically effective amount of the ophthalmic composition to the subject's eye during the treatment period. The aforementioned ophthalmic composition is A sufficient amount of corneal crosslinking agents and secondary treatment agents to treat myopic progression, and A pharmaceutically acceptable carrier, An ophthalmic composition containing [the specified ingredient].
70. An ophthalmic composition for use according to claim 69, wherein the ophthalmic composition is formulated as one of a solution, suspension, emulsion, gel, hydrogel, thermoresponsive gel, depot, film, gelled suspension, contact lens, or puncture plug.
71. An ophthalmic composition for use according to claim 69, wherein the ophthalmic composition is formulated as a sustained-release composition configured to release the copper-containing agent and the secondary therapeutic agent over a period of about 2 days to about 6 months.
72. An ophthalmic composition for use according to claim 71, wherein the administration is carried out by one or more of the following: placement of the composition in the sac-like portion of the eyeball, placement of the composition in the conjunctival vestibule of the eyeball, and placement of the composition in the subtenon space of the eyeball.
73. An ophthalmic composition for use according to claim 71, wherein the ophthalmic composition is configured to deliver, on average, about 0.0001 μg to about 5500 μg of copper per day to the eyes of the subject.
74. An ophthalmic composition for use according to claim 71, wherein the ophthalmic composition is configured to deliver an average of about 0.01 μg to about 200 μg of a secondary therapeutic agent per day to the eyes of the subject.
75. An ophthalmic composition for use according to claim 69, wherein the secondary therapeutic agent is present in the composition in an amount of about 0.0005 wt% to about 2 wt%.
76. An ophthalmic composition for use according to claim 69, wherein the secondary therapeutic agent is present in the composition in an amount of about 0.001 wt% to about 1 wt%.
77. An ophthalmic composition for use according to claim 69, wherein the amount of the secondary therapeutic agent present in the composition is about 0.001 mg / ml to about 20 mg / ml.
78. An ophthalmic composition for use according to claim 69, wherein the secondary therapeutic agent is a member selected from the group consisting of atropine, homatropine, cyclopentolate, pirenzepine, 7-methylxanthanine, and combinations thereof.
79. An ophthalmic composition for use according to claim 69, wherein the corneal crosslinking agent is a copper-containing compound that provides copper in an amount of about 0.000001 wt% to about 15 wt% of the composition.
80. An ophthalmic composition for use according to claim 69, wherein the corneal crosslinking agent is a copper-containing compound that provides copper in an amount of about 0.00001 mg / ml to about 1 mg / ml.
81. An ophthalmic composition for use according to claim 69, wherein the corneal crosslinking agent is a copper-containing compound that provides copper in an amount of about 0.015 mg / ml to about 0.15 mg / ml.
82. An ophthalmic composition for use according to claim 69, wherein the corneal crosslinking agent is a copper-containing compound selected from the group consisting of copper sulfate, copper carbonate, copper acetate, copper chloride, copper hydroxide, copper gluconate, copper bromide, copper fluoride, copper nitrate, copper iodide, copper perchlorate, copper molybdate, copper thiocyanate, copper tartrate, copper tetrafluoroborate, copper selenate, copper pyrophosphate, GHK-copper, copper tetraamine sulfate, copper histidine, copper glycinate, and combinations thereof.
83. An ophthalmic composition for use according to claim 69 of the pharmaceutical invention, wherein the pharmaceutically acceptable carrier comprises at least one of a tonic, a solubilizer, a thickener, a polymer, a buffer, a preservative, a pH adjuster, and water.
84. An ophthalmic composition for use according to claim 69, wherein the composition has a rigidity of about 200 mOsm / kg to about 600 mOsm / kg.
85. An ophthalmic composition for use according to claim 69, wherein the composition has a pH of about 5.5 to about 8.
5.
86. An ophthalmic composition for use according to claim 69, wherein the ophthalmic composition is formulated as eye drops and delivered in a container adapted to dispense the composition in a droppery manner in a droppery volume of about 5 μl to about 100 μl.
87. An ophthalmic composition for use according to claim 86, wherein the dosage form provides about 0.0001 μg to about 500 μg of copper per drop of the ophthalmic composition.
88. An ophthalmic composition for use according to claim 69, wherein the composition is administered at 1 to 4 time points per day to the eye in need.
89. An ophthalmic composition for use according to claim 88, wherein about 5 μl to about 100 μl of the composition is administered at each time point.
90. An ophthalmic composition for use according to claim 69, wherein the composition is administered in conjunction with an ophthalmoplastic device configured to reshape an elongated myopic eye.
91. An ophthalmic composition for use according to claim 69, wherein the subject is a human subject having an age of approximately 3 to approximately 25 years.
92. An ophthalmic composition for use according to claim 69, wherein the treatment period is approximately 6 months to approximately 5 years.