United States Patent 10,076,494: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 10,076,494, titled "Stable Orally Disintegrating Pharmaceutical Compositions," is a significant patent in the pharmaceutical industry, particularly in the development of orally disintegrating tablets (ODTs) containing proton pump inhibitors (PPIs). This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Scope of the Patent
Overview
The patent describes stable orally disintegrating tablets that contain a proton pump inhibitor, such as omeprazole, lansoprazole, pantoprazole, rabeprazole, tenatoprazole, or ilaprazole, or a combination thereof. These tablets are designed to disintegrate rapidly in the mouth, providing a convenient and patient-friendly dosage form[1].
Key Components
- Proton Pump Inhibitors (PPIs): The patent specifies various PPIs that can be used, each with its own therapeutic efficacy.
- Inert Seed: The inert seed can be a granule, pellet, bead, or powder, each representing a separate embodiment.
- Subcoating and Enteric Coating: The cores of the tablets are coated with a subcoating and an enteric coating. The subcoating can be made from materials like hydroxypropyl methylcellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, polyethylene glycol, or polyvinyl alcohol[1].
Claims of the Patent
Compressed Orally Disintegrating Tablets
The patent claims include:
- Composition: The tablets comprise a disintegrant in an amount of about 2% to about 25% by weight of the total tablet weight.
- Cores: The tablets include multiple cores containing a therapeutically effective amount of a PPI, making up about 5% to about 25% by weight of the total tablet weight.
- Enteric Coating: An enteric coating in an amount of about 10% to about 30% by weight of the total tablet weight.
- Reverse Enteric Polymer Coating: A coating comprising a reverse enteric polymer in an amount of about 5% to about 15% by weight of the total tablet weight[1].
Method for Increasing Compressibility
The patent also claims a method for increasing the compressibility of the tablets by applying a coating comprising a reverse enteric polymer over the enteric-coated cores. This method results in decreased friability (about 0.75% or less) and increased hardness (about 20 N to about 100 N) when a compression force of about 10 kN to about 50 kN is applied during manufacturing[1].
Patent Landscape
Related Patents and Technologies
- Orally Disintegrating Tablets: Other patents, such as US20050232988A1, also describe methods for manufacturing orally disintegrating tablets, highlighting the growing interest in this dosage form. These patents often focus on the use of disintegrants, binding agents, and specific manufacturing processes to achieve rapid disintegration[5].
- Pharmaceutical Formulations: Patents like those described in the District of Delaware case involving Heron Therapeutics and Fresenius Kabi USA, LLC, focus on stable injectable formulations of other drugs, such as aprepitant. These cases illustrate the broader efforts in pharmaceutical formulation to ensure stability and efficacy[2].
Intellectual Property Rights and Regulatory Exclusivities
- Patent Protection: The patent landscape is influenced by intellectual property rights, which provide exclusive rights to the patent holder for a period of 20 years from the filing date. This protection is crucial for pharmaceutical companies to recoup their investment in research and development[4].
- Regulatory Exclusivities: In addition to patent protection, pharmaceutical products may receive regulatory exclusivities, which can last from six months to 12 years. These exclusivities prevent the FDA from approving generic or biosimilar versions of the drug during this period, further protecting the original manufacturer's market position[4].
Impact on the Pharmaceutical Industry
Innovation and Competition
- The development of stable orally disintegrating tablets with PPIs enhances patient compliance and convenience, driving innovation in the pharmaceutical industry.
- The patent protection and regulatory exclusivities associated with these formulations can influence the market entry of generic and biosimilar products, affecting competition and drug pricing[4].
Manufacturing and Quality Control
- The methods described in the patent for increasing compressibility and reducing friability are significant for manufacturing processes. These improvements can lead to more consistent and reliable production of orally disintegrating tablets.
- The emphasis on stability and efficacy in these formulations aligns with regulatory requirements and industry standards, ensuring that the final product meets the necessary quality control criteria[1].
Key Takeaways
- Stable Formulations: The patent provides detailed compositions and methods for creating stable orally disintegrating tablets containing PPIs.
- Improved Manufacturing: The use of a reverse enteric polymer coating enhances the compressibility and reduces the friability of the tablets.
- Intellectual Property Protection: The patent and associated regulatory exclusivities play a crucial role in protecting the invention and influencing the market dynamics.
- Industry Impact: The innovation in orally disintegrating tablets contributes to better patient compliance and convenience, while also affecting competition and drug pricing in the pharmaceutical industry.
FAQs
What are the key components of the orally disintegrating tablets described in the patent?
The key components include a proton pump inhibitor, an inert seed, a subcoating, an enteric coating, and optionally a reverse enteric polymer coating.
How does the reverse enteric polymer coating improve the tablets?
The reverse enteric polymer coating increases the compressibility of the tablets, reducing friability and increasing hardness during manufacturing.
What is the significance of patent protection and regulatory exclusivities in this context?
Patent protection and regulatory exclusivities provide the patent holder with exclusive rights to manufacture and market the drug, protecting their investment and influencing market competition.
How do these formulations impact patient compliance?
The orally disintegrating tablets enhance patient compliance by providing a convenient and easy-to-use dosage form that disintegrates rapidly in the mouth.
What are some related technologies and patents in the pharmaceutical industry?
Other related patents focus on different pharmaceutical formulations, such as stable injectable formulations and other orally disintegrating tablets, highlighting ongoing innovation in drug delivery systems.
Sources
- US10076494B2 - Stable orally disintegrating pharmaceutical compositions - Google Patents
- 22-985.pdf - District of Delaware
- Patent Claims and Patent Scope - SSRN
- Drug Prices: The Role of Patents and Regulatory Exclusivities - Congressional Research Service
- US20050232988A1 - Orally disintegrating tablets and methods of manufacture - Google Patents
