United States Patent 10,376,505: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 10,376,505, titled "Oral formulations and lipophilic salts of methylnaltrexone," is a significant patent in the pharmaceutical field, particularly in the treatment of opioid-induced constipation. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background of Methylnaltrexone
Methylnaltrexone is a potent opioid antagonist that has been clinically approved in the United States for the treatment of opioid-induced constipation in patients with advanced illness or those receiving palliative care. The subcutaneous injection form of methylnaltrexone has been effective, but the development of oral formulations has been a focus to enhance patient compliance and convenience[1].
Scope of the Patent
The patent US10376505B2 covers several key aspects of methylnaltrexone formulations:
Oral Dosage Forms
The patent describes the development of oral dosage forms of methylnaltrexone, which is crucial because opioid antagonists like methylnaltrexone are not always suitable for immediate release due to dose-limiting side effects. The oral formulations are designed to release the compound over the entire gastrointestinal tract, addressing the local effects of opioids on the GI tract[1].
Lipophilic Salts and Ion Pairs
The invention includes the formation of ion pairs of methylnaltrexone with amphiphilic pharmaceutically acceptable excipients. These ion pairs enhance the solubility and stability of methylnaltrexone, making it more suitable for oral administration. The patent also details methods for forming, selecting, and using these ion pairs[1].
Controlled-Release Formulations
To mitigate the side effects associated with immediate release, the patent suggests controlled-release dosage forms. This approach ensures that methylnaltrexone is delivered at acceptable doses locally across the entire gastrointestinal tract, providing effective treatment without inducing immediate laxation[1].
Claims of the Patent
The patent includes several claims that define the scope of the invention:
Composition Claims
- Claims related to pharmaceutical compositions containing methylnaltrexone and an amphiphilic pharmaceutically acceptable excipient.
- Specific formulations, including those with rapid-acting disintegrants such as effervescent or carbon dioxide-producing disintegrants[1].
Method Claims
- Methods for forming ion pairs of methylnaltrexone and selecting appropriate excipients.
- Methods for using these compositions and formulations for treating opioid-induced constipation[1].
Formulation Claims
- Claims covering solid oral formulations, including tablets, pills, and other galenical forms characterized by their shape, structure, or size[1].
Patent Landscape
Related Patents and Prior Art
The patent US10376505B2 is part of a broader landscape of pharmaceutical patents related to opioid antagonists and their formulations. Prior art includes other patents and publications discussing the use of opioid antagonists in treating opioid-induced constipation. For example, the '959 patent mentioned in the background of US10376505B2 suggests dosing certain opioid antagonists in a controlled-release dosage form[1].
Classification and Categories
The patent is classified under various categories in the International Patent Classification (IPC) system, including A61K47/06 and A61K47/20, which pertain to organic compounds and their pharmaceutical applications. It also falls under A61K9/00, which covers medicinal preparations characterized by special physical forms[1].
Litigation and Examination
While the patent US10376505B2 itself is not directly involved in the litigation discussed in other sources, the broader context of patent litigation and examination is relevant. Factors such as patent scope, claim length, and claim count can influence the likelihood of patent infringement litigation and the validity of patents during examination processes[3][4].
Industry Impact and Clinical Relevance
Clinical Benefits
The oral formulations of methylnaltrexone described in this patent offer significant clinical benefits, including improved patient compliance and reduced side effects compared to subcutaneous injections. This is particularly important for patients with advanced illnesses who may have difficulty with injectable treatments[1].
Market and Competitive Landscape
The development of oral methylnaltrexone formulations positions the patent holder competitively in the market for treatments of opioid-induced constipation. This market is growing due to the increasing use of opioids for pain management and the subsequent need for effective treatments for opioid-induced side effects.
Key Takeaways
- Oral Formulations: The patent covers the development of oral dosage forms of methylnaltrexone, enhancing patient compliance and convenience.
- Lipophilic Salts and Ion Pairs: The invention includes ion pairs with amphiphilic excipients to improve solubility and stability.
- Controlled-Release: Controlled-release formulations are designed to deliver methylnaltrexone across the entire gastrointestinal tract.
- Clinical Benefits: Oral formulations offer improved compliance and reduced side effects.
- Market Impact: The patent positions the holder competitively in the growing market for opioid-induced constipation treatments.
FAQs
What is the primary focus of United States Patent 10,376,505?
The primary focus is on the development of oral formulations and lipophilic salts of methylnaltrexone for treating opioid-induced constipation.
How do the oral formulations of methylnaltrexone improve patient treatment?
The oral formulations improve patient compliance and convenience compared to subcutaneous injections and are designed to release the compound over the entire gastrointestinal tract, reducing side effects.
What is the significance of ion pairs in this patent?
Ion pairs of methylnaltrexone with amphiphilic pharmaceutically acceptable excipients enhance the solubility and stability of methylnaltrexone, making it more suitable for oral administration.
How does the controlled-release formulation work?
The controlled-release formulation ensures that methylnaltrexone is delivered at acceptable doses locally across the entire gastrointestinal tract, providing effective treatment without immediate laxation.
What is the market impact of this patent?
The patent positions the holder competitively in the growing market for treatments of opioid-induced constipation, driven by the increasing use of opioids for pain management.
Sources
- US10376505B2 - Oral formulations and lipophilic salts of methylnaltrexone - Google Patents
- In re Cellect - United States Court of Appeals for the Federal Circuit - CAFC
- Patent Claims and Patent Scope - SSRN
- Assessing Factors That Affect Patent Infringement Litigation - GAO
