Detailed Analysis of the Scope and Claims of United States Patent 10,376,470
Introduction
United States Patent 10,376,470, titled "Oral tablet formulation consisting of fixed combination of rosuvastatin and ezetimibe for treatment of hyperlipidemia and cardiovascular diseases," is a significant patent in the pharmaceutical industry. This patent, assigned to Althera Life Sciences, LLC, protects a novel formulation and method of manufacturing a combination of rosuvastatin and ezetimibe, two widely used drugs for treating hyperlipidemia and cardiovascular diseases.
Patent Overview
The patent was issued on August 13, 2019, and is set to expire on May 1, 2033, unless there are any changes due to legal activities such as term extensions or amendments[2][5].
Scope of the Patent
Active Ingredients
The patent focuses on the combination of rosuvastatin and ezetimibe, both of which are crucial for managing hyperlipidemia and reducing the risk of cardiovascular diseases. Rosuvastatin is a statin that lowers cholesterol levels, while ezetimibe works by inhibiting the absorption of cholesterol in the small intestine[1].
Formulation
The patent describes a novel approach to formulating these two active ingredients into a single bi-layer tablet. This formulation separates the two ingredients into almost completely separate parts or layers to enhance their bioavailability and efficacy. The rosuvastatin layer is formulated using microcrystalline cellulose, while the ezetimibe layer is formulated by dissolving ezetimibe and mounting it on lactose or mannitol to improve its solubility[1].
Claims of the Patent
Method of Manufacture
The patent claims a method of making the solid dosage bi-layer form of rosuvastatin and ezetimibe. This involves several steps:
- Blending rosuvastatin calcium with pre-gelatinized starch, calcium hydrogen phosphate, microcrystalline cellulose, and crospovidone, followed by lubrication with sodium stearyl fumarate.
- Mixing ezetimibe with a wetting agent and dispersing it in a mixture of isopropyl alcohol and dichloromethane.
- Absorbing the ezetimibe dispersion on lactose or mannitol and then granulating the mix with polyvinylpyrrolidone solution[1].
Solid Dosage Form
The preferred solid dosage form is a bi-layer tablet, which has one solid layer of ezetimibe composition and a solid layer of rosuvastatin composition. This formulation ensures that the combination is bioequivalent to taking two individual tablets of rosuvastatin and ezetimibe, with similar Cmax and area under the curve (AUC) values[1].
Pharmaceutically Acceptable Additives
The patent also includes claims for the use of pharmaceutically acceptable additives such as diluents, disintegrants, glidants, lubricants, and colorants. These additives are selected to ensure the stability and efficacy of the formulation[1].
Patent Landscape
Patent Protection
The patent is part of a broader patent landscape that includes multiple patents protecting various aspects of the drug, including dosage, mode of administration, and manufacturing processes. The protection extends beyond the United States, with patents filed in multiple countries to ensure global exclusivity[2].
Generic Launch Date
As of now, there are no approved generic versions of Roszet, and the estimated generic launch date is May 1, 2033, based on the expiry of the last outstanding patent. This date is subject to change due to ongoing legal activities or exclusivity additions[2][5].
Legal Activities
Recent legal activities on the patent include payments of maintenance fees, changes in power of attorney, and correspondence address changes. These activities are crucial for maintaining the patent's validity and ensuring that the exclusivity period is not compromised[2].
Impact on the Pharmaceutical Industry
Innovation and Competition
The patent's scope and claims highlight the innovative approach to formulating combination drugs, which can significantly impact the pharmaceutical industry. By protecting this specific formulation, Althera Life Sciences, LLC, can prevent competitors from developing similar products until the patent expires. This exclusivity period allows the company to recoup its investment in research and development[3].
Regulatory Compliance
The patent also underscores the importance of regulatory compliance. The formulation must meet bioequivalence standards set by regulatory bodies, ensuring that the combination drug is as effective as taking the two individual drugs. This compliance is crucial for gaining approval and maintaining market presence[5].
Challenges in Patent Claims
Genus Claims and Enablement
The pharmaceutical industry faces challenges in drafting patent claims that are neither too broad nor too narrow. The Federal Circuit's recent jurisprudence on genus claims and enablement has made it difficult to obtain meaningful patent protection. Innovators must balance the scope of their claims to avoid infringement issues while ensuring that their inventions are fully protected[3].
Key Takeaways
- Innovative Formulation: The patent protects a novel bi-layer tablet formulation of rosuvastatin and ezetimibe.
- Manufacturing Process: The method of manufacture involves separate steps for each active ingredient to enhance bioavailability.
- Patent Exclusivity: The patent is set to expire on May 1, 2033, with no approved generic versions currently available.
- Regulatory Compliance: The formulation must meet bioequivalence standards to ensure efficacy and regulatory approval.
- Industry Impact: The patent's exclusivity period affects competition and innovation in the pharmaceutical industry.
FAQs
What is the main focus of United States Patent 10,376,470?
The main focus of this patent is the formulation and method of manufacturing a fixed combination of rosuvastatin and ezetimibe in a bi-layer tablet for treating hyperlipidemia and cardiovascular diseases.
How does the bi-layer tablet formulation enhance the bioavailability of the drugs?
The bi-layer tablet formulation separates rosuvastatin and ezetimibe into distinct layers, with ezetimibe mounted on lactose or mannitol to improve its solubility, thus enhancing the bioavailability of both drugs.
When is the patent set to expire?
The patent is set to expire on May 1, 2033, unless there are any changes due to legal activities.
Are there any approved generic versions of Roszet available?
No, there are currently no approved generic versions of Roszet available.
What are the implications of the Federal Circuit's recent jurisprudence on genus claims for pharmaceutical patents?
The recent jurisprudence has made it challenging for pharmaceutical companies to draft patent claims that are neither too broad nor too narrow, affecting the scope of patent protection and innovation in the industry.
Cited Sources:
- US10376470B2 - Oral tablet formulation consisting of fixed combination of rosuvastatin and ezetimibe for treatment of hyperlipidemia and cardiovascular diseases - Google Patents
- Roszet patent expiration - Pharsight - GreyB
- Eviscerating Patent Scope - DigitalCommons@NYLS
- Formulation of Modified-Release Bilayer Tablets of Atorvastatin and ... - MDPI
- Generic Roszet Availability - Drugs.com
