United States Patent 10,918,694: A Comprehensive Analysis
Introduction
The United States Patent 10,918,694, titled "Topical cyclosporine-containing formulations and uses thereof," is a significant patent in the field of ophthalmic formulations. This patent, issued on February 28, 2022, and set to expire on February 28, 2037, outlines innovative formulations and methods for the topical administration of cyclosporine, particularly in ophthalmic applications.
Background and Context
Cyclosporine is an immunosuppressive agent widely used in treating various ocular conditions, including dry eye syndrome, keratitis, and other inflammatory eye diseases. The development of effective topical formulations is crucial for maximizing the drug's efficacy while minimizing systemic side effects.
Scope of the Patent
Formulations
The patent describes formulations containing 0.087-0.093 wt % of cyclosporine, which is a narrow and specific concentration range. These formulations are designed for topical ophthalmic use and may include various components such as polyoxyl lipids, fatty acids, polyalkoxylated alcohols, and nanomicelles[1][2][5].
Components and Ingredients
- Polyoxyl Lipids and Fatty Acids: These components are integral to the formulation, enhancing the stability and bioavailability of cyclosporine.
- Polyalkoxylated Alcohols: These help in solubilizing the drug and improving its delivery.
- Nanomicelles: These are microscopic vesicles that encapsulate the drug, facilitating targeted and efficient delivery to the ocular tissues[2][5].
Methods of Preparation
The patent details methods of preparing these formulations, including stirring, filling, and buffering processes. The formulations may involve the use of preservative agents, bioadhesives, and other excipients to ensure stability and patient compliance[1].
Claims
The patent includes several claims that define the scope of the invention:
Composition Claims
- The patent claims formulations containing specific concentrations of cyclosporine and other ingredients like polyoxyl lipids, fatty acids, and polyalkoxylated alcohols.
- It also claims the use of nanomicelles in these formulations to enhance drug delivery[1][2].
Method Claims
- The patent claims methods of making these formulations, including the steps involved in preparing and stabilizing the cyclosporine-containing solutions.
- It also includes claims related to the methods of using these formulations for treating or preventing ocular diseases[1][2].
Patent Landscape
Related Patents
The patent landscape surrounding US 10,918,694 includes several related patents that also deal with topical ophthalmic formulations:
- Patent 10,441,630: Issued to SUN PHARMA GLOBAL FZE, this patent also covers formulations for topical administration, including ophthalmic formulations, and methods of using such formulations[2].
- Patent 8,980,839: This patent, issued to Ocular Technologies SARL, describes formulations for topical administration, including ophthalmic formulations, and methods of treating or preventing ocular diseases[2].
Expiration Dates
The patent is set to expire on February 28, 2037, which is a typical 20-year term from the date of filing. Other related patents, such as Patent 10,441,630, expire on August 23, 2033[2].
Competitive Analysis
The patent landscape indicates significant activity in the development of ophthalmic formulations by various pharmaceutical companies and research institutions. Major players include SUN PHARMA GLOBAL FZE and Ocular Technologies SARL, among others. This competitive environment drives innovation and improves the efficacy and safety of ophthalmic treatments[2][3].
Therapeutic Applications
Ocular Diseases
The formulations described in the patent are intended for treating a range of ocular diseases and conditions, including:
- Dry eye syndrome
- Keratitis
- Inflammatory eye diseases
- Proliferative vitreoretinopathy
- Retinopathy[1][2].
Mechanism of Action
Cyclosporine works by modulating the immune response, reducing inflammation, and promoting healing in the ocular tissues. The use of nanomicelles and other delivery systems enhances the drug's bioavailability and reduces side effects[4].
Technical and Analytical Aspects
Characterization Methods
The patent and related research involve various characterization methods to ensure the quality and efficacy of the formulations. These include:
- Transmission Electron Microscopy (TEM) to study the ultrastructure of the nanomicelles.
- Surface tension and contact angle measurements to assess the physical properties of the formulations[4].
In Vitro Drug Release Studies
These studies are crucial for understanding the release kinetics of cyclosporine from the formulations, ensuring that the drug is delivered effectively and consistently over time[4].
Regulatory and Commercial Implications
Patent Exclusivity
The patent grants exclusive rights to the patent holder until its expiration in 2037. This exclusivity period allows the patent holder to market the drug without generic competition, which can be a significant commercial advantage[2].
Generic Availability
After the patent expires, generic versions of the drug may become available, subject to FDA approval and bioequivalence testing. The Reference Listed Drug (RLD) designation will be crucial in this process, ensuring that generic versions meet the same standards as the brand-name drug[2].
Key Takeaways
- The patent describes specific formulations of cyclosporine for ophthalmic use, including the use of nanomicelles.
- The formulations are designed to treat various ocular diseases and conditions.
- The patent landscape shows significant activity in ophthalmic formulation development by several pharmaceutical companies.
- The patent expires on February 28, 2037, after which generic versions may become available.
- Characterization and in vitro studies are essential for ensuring the quality and efficacy of these formulations.
Frequently Asked Questions (FAQs)
What is the primary active ingredient in the formulations described in US 10,918,694?
The primary active ingredient is cyclosporine, an immunosuppressive agent.
What is the concentration range of cyclosporine in these formulations?
The concentration range is 0.087-0.093 wt %.
What role do nanomicelles play in these formulations?
Nanomicelles enhance the bioavailability and targeted delivery of cyclosporine to ocular tissues.
What are some of the ocular diseases treated by these formulations?
These formulations are used to treat dry eye syndrome, keratitis, inflammatory eye diseases, proliferative vitreoretinopathy, and retinopathy.
When does the patent expire?
The patent expires on February 28, 2037.
Cited Sources:
- US10918694B2 - Topical cyclosporine-containing formulations and uses thereof - Google Patents
- Generic Cequa Availability - Drugs.com
- A novel approach to understand patents from the drug discovery ... - bioRxiv
- Cationic Hyaluronic Acid-Modified Cyclosporin Micelles Used for ... - International Journal of Pharmaceutics
- CN117957011A - Stable cyclosporin ophthalmic ... - Google Patents
