Advanced Ophthalmic Compositions for Eye Health

Introduction

This technology offers a highly effective ophthalmic composition designed to address a range of eye health needs, from dry eye relief to post-surgical care. By delivering superior hydration, protection, and therapeutic benefits, this formulation provides a holistic approach to eye care, supporting patients’ vision and comfort in both everyday and clinical settings. For companies in ophthalmology, pharmaceuticals, and eye care, this technology is a powerful asset that aligns with the growing demand for advanced and patient-friendly eye treatment solutions.

The Challenge: Meeting the Diverse Needs of Eye Care

In today’s eye care market, patients with different conditions require tailored solutions that address specific needs, whether they’re managing dry eyes, recovering from surgery, or dealing with other ocular issues. Many current eye treatments offer limited benefits, focusing primarily on symptom relief without addressing the underlying needs for hydration, protection, and healing. As people spend more time on screens and environmental factors increase the risk of eye strain, the need for innovative, multipurpose eye care products has intensified. Healthcare providers and patients alike are seeking comprehensive eye care solutions that deliver sustained comfort and support.

A Comprehensive Composition for Superior Eye Care

This advanced ophthalmic composition meets these challenges with a unique formulation that offers long-lasting hydration, protective properties, and therapeutic support. Designed to be gentle yet effective, this composition provides an ideal solution for patients with dry eyes, those recovering from surgeries, or individuals exposed to environmental irritants. The formula is adaptable, making it suitable for prescription and over-the-counter eye care products. By offering an all-in-one solution, this technology enhances patient satisfaction and promotes better overall eye health, setting a new standard in the ophthalmic care industry.

Key Benefits for Pharmaceuticals and Eye Care Providers

For pharmaceutical and eye care companies, this technology offers an opportunity to develop a product line that meets a wide array of eye health needs. Hospitals, clinics, and ophthalmologists can use these advanced compositions to provide patients with effective, comprehensive care that addresses both comfort and healing. This composition’s gentle formulation is suitable for various applications, from routine hydration to therapeutic use, giving healthcare providers a versatile tool for improving patient outcomes. The ability to treat multiple symptoms and support eye health proactively makes it an invaluable addition to the eye care market.

Invest in Next-Level Eye Health Solutions

Licensing this advanced ophthalmic composition technology positions your company at the forefront of innovation in eye care. By offering a versatile, effective formula that caters to a wide range of eye health needs, your business can meet the increasing demand for superior ophthalmic solutions. This technology provides a strategic investment for companies dedicated to advancing patient comfort, enhancing eye health, and delivering high-quality care in ophthalmology.

Please see terms and conditions
The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and/or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles.

What is claimed is:

1. A pharmaceutical composition comprising:

a calcineurin inhibitor or an mTOR inhibitor;
a first surfactant with an HLB index greater than about 10; and
a second surfactant with an HLB index of greater than about 13,
wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3,
wherein the composition is in the form of mixed micelles having the first and second surfactants; and wherein the composition contains less than 2% by weight ethanol.
2. The pharmaceutical composition of claim 1 wherein the calcineurin inhibitor or the mTOR inhibitor is selected from one or more of voclosporin, cyclosporine A, pimecrolimus, tacrolimus, sirolimus, temsirolimus, everolimus, analogs thereof, pharmaceutically acceptable salts thereof, or combinations thereof.
3. The pharmaceutical composition of claim 1 wherein the composition is in the form of optically clear mixed micelles.
4. The pharmaceutical composition of claim 1 wherein the first surfactant is selected from a polyethylene glycol (PEG)-5-100 nonyl phenyl ether, tyloxapol, a PEG-fatty acid monoester surfactant, a PEG-glycerol fatty acid ester, and a PEG-sorbiton fatty acid ester.
5. The pharmaceutical composition of claim 4 wherein the PEG-fatty acid monoester surfactant is selected from PEG-15 oleate, PEG-20 laurate, PEG-20 oleate, PEG-20 stearate, PEG-32 laurate, PEG-32 oleate, PEG-32 stearate, PEG-40 laurate, PEG-40 oleate, and PEG-40 stearate.
6. The pharmaceutical composition of claim 4 wherein the PEG-glycerol fatty acid ester is selected from PEG-15 glyceryl laurate, PEG-20 glyceryl laurate, PEG-30 glyceryl laurate, PEG-40 glyceryl laurate, and PEG-20 glyceryl stearate.
7. The pharmaceutical composition of claim 4 wherein the PEG-sorbiton fatty acid ester is selected from PEG-4 sorbiton monolaurate, PEG-4 sorbiton monostearate, PEG-5 sorbiton monooleate, PEG-20 sorbiton monolaurate, PEG-20 sorbiton monopalmitate, PEG-20 sorbiton monostearate, and PEG-20 sorbiton monooleate.
8. The pharmaceutical composition of claim 1 wherein the second surfactant is a polyethylene glycol (PEG)-alkyl ether surfactant or PEG-alkyl aryl ether surfactant.
9. The pharmaceutical composition of claim 8 wherein the second surfactant is a PEG 5-100 octyl phenyl ether.
10. The pharmaceutical composition of claim 9 wherein the PEG 5-100 octyl phenyl compound is selected from octoxynol-9, octoxynol-10, octoxynol-11, octoxynol-12, octoxynol-13, octoxynol-16, octoxynol-20, octoxynol-25, octoxynol-30, octoxynol-33, octoxynol-40, and octoxynol-70.
11. The pharmaceutical composition of claim 1 wherein the composition is an aqueous solution.
12. The pharmaceutical composition of claim 1 wherein the calcineurin inhibitor or mTOR inhibitor is delivered to a back of an eye.
13. The pharmaceutical composition of claim 1 wherein the composition is essentially free of short-chain alcohols.

14. A pharmaceutical composition comprising:

a calcineurin inhibitor or an mTOR inhibitor;
a first surfactant with an HLB index greater than about 10; and
a second surfactant with an HLB index of greater than about 13,
wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3,
wherein the composition is in the form of an aqueous solution of mixed micelles having the first and second surfactants; and
wherein the composition contains less than 2% by weight ethanol.
15. The pharmaceutical composition of claim 14 wherein the calcineurin inhibitor or the mTOR inhibitor is selected from one or more of voclosporin, cyclosporine A, pimecrolimus, tacrolimus, sirolimus, temsirolimus, everolimus, analogs thereof, pharmaceutically acceptable salts thereof, or combinations thereof.
16. The pharmaceutical composition of claim 14 wherein the composition is optically clear.
17. The pharmaceutical composition of claim 14 wherein the first surfactant is selected from a polyethylene glycol (PEG)-5-100 nonyl phenyl ether, tyloxapol, a PEG-fatty acid monoester surfactant, a PEG-glycerol fatty acid ester, and a PEG-sorbiton fatty acid ester.
18. The pharmaceutical composition of claim 14 wherein the second surfactant is a polyethylene glycol (PEG)-alkyl ether surfactant or PEG-alkyl aryl ether surfactant.
19. The pharmaceutical composition of claim 14 wherein the calcineurin inhibitor or mTOR inhibitor is delivered to a back of an eye.
20. The pharmaceutical composition of claim 14 wherein the composition is free of short-chain alcohols.

21. A method for treating an ocular disease in a patient in need thereof, comprising administering topically to an eye of the patient a mixed micelle pharmaceutical composition comprising:

a calcineurin inhibitor or an mTOR inhibitor;
a first surfactant with an HLB index greater than about 10; and
a second surfactant with an HLB index of greater than about 13,
wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, wherein the composition is in the form of mixed micelles having the first and second surfactants, and wherein the composition contains less than 2% by weight ethanol.
22. The method of claim 21 wherein the calcineurin inhibitor or the mTOR inhibitor is selected from one or more of voclosporin, cyclosporine A, pimecrolimus, tacrolimus, sirolimus, temsirolimus, everolimus, analogs thereof, pharmaceutically acceptable salts thereof, or combinations thereof.
23. The method of claim 21 wherein the first surfactant is selected from a polyethylene glycol (PEG)-5-100 nonyl phenyl ether, tyloxapol, a PEG-fatty acid monoester surfactant, a PEG-glycerol fatty acid ester, and a PEG-sorbiton fatty acid ester.
24. The method of claim 23 wherein the PEG-fatty acid monoester surfactant is selected from PEG-15 oleate, PEG-20 laurate, PEG-20 oleate, PEG-20 stearate, PEG-32 laurate, PEG-32 oleate, PEG-32 stearate, PEG-40 laurate, PEG-40 oleate, and PEG-40 stearate; the PEG-glycerol fatty acid ester is selected from PEG-15 glyceryl laurate, PEG-20 glyceryl laurate, PEG-30 glyceryl laurate, PEG-40 glyceryl laurate, and PEG-20 glyceryl stearate; and the PEG-sorbiton fatty acid ester is selected from PEG-4 sorbiton monolaurate, PEG-4 sorbiton monostearate, PEG-5 sorbiton monooleate, PEG-20 sorbiton monolaurate, PEG-20 sorbiton monopalmitate, PEG-20 sorbiton monostearate, and PEG-20 sorbiton monooleate.
25. The method of claim 21 wherein the second surfactant is a polyethylene glycol (PEG)-alkyl ether surfactant or PEG-alkyl aryl ether surfactant.
26. The method of claim 25 wherein the second surfactant is a PEG 5-100 octyl phenyl ether selected from octoxynol-9, octoxynol-10, octoxynol-11, octoxynol-12, octoxynol-13, octoxynol-16, octoxynol-20, octoxynol-25, octoxynol-30, octoxynol-33, octoxynol-40, and octoxynol-70.
27. The method of claim 21 further comprising delivering the calcineurin inhibitor or mTOR inhibitor to a back of an eye via the mixed micelle pharmaceutical composition.
28. The method of claim 21 wherein the ocular disease is an inflammatory ocular surface disease selected from the group consisting of dry eye syndrome (DES), Sjogren’s syndrome, uveitis, conjunctivitis (pink eye), keratitis, keratoconjunctivitis, vernal keratoconjunctivitis (VKC), atopic keratoconjunctivitis (AKC), autoimmune disorders of the ocular surface, cicatrizing conjunctivitis, blepharitis, scleritis, or an immune rejection of a corneal allograft.
29. The method of claim 21 wherein the composition is essentially free of short-chain alcohols.
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Title

Ophthalmic compositions

Inventor(s)

Ashim K. Mitra, Poonam R. Velagaleti, Subramanian Natesan

Assignee(s)

Aurinia Pharmaceuticals Inc

Patent #

10265381

Patent Date

April 23, 2019

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