United States Patent 7,182,958: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 7,182,958, titled "Pharmaceutical compositions comprising tadalafil," is a significant patent in the pharmaceutical industry, particularly in the realm of erectile dysfunction treatments and other related conditions. This patent, assigned to ICOS Corporation, covers various aspects of tadalafil formulations, preparation methods, and their applications.
Background of Tadalafil
Tadalafil, chemically known as (6R,12aR)-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a hexa hydro-2-methylpyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-dione, is a phosphodiesterase type 5 (PDE5) inhibitor. It is widely used to treat conditions such as male erectile dysfunction, benign prostatic hyperplasia, and pulmonary hypertension[1].
Scope of the Patent
The patent encompasses several key aspects:
Pharmaceutical Compositions
The patent describes pharmaceutical compositions that include tadalafil or its pharmaceutically acceptable salts. These compositions are formulated with various excipients such as diluents, lubricants, hydrophilic binders, and disintegrants. The particle size of tadalafil in these compositions is crucial, with at least 90% of the particles having a size of less than about 40 microns[1].
Preparation Process
The patent details a melt granulation process for preparing these compositions. This process involves blending tadalafil with melted excipients and then using hot melt extrusion technology to ensure uniform distribution. The temperature is maintained below 95°C to prevent drug decomposition and maintain tadalafil in its crystalline form[1].
Dosage Forms
The compositions can be formulated into various dosage forms, such as tablets or capsules, and may be optionally coated. The patent emphasizes the importance of maintaining the particle size within a specific range (between about 42 microns to less than about 200 microns) for optimal stability and in-vitro dissolution[1].
Claims of the Patent
The patent includes several claims that define its scope:
Composition Claims
- Claims related to the pharmaceutical composition comprising tadalafil or its pharmaceutically acceptable salts, along with specified excipients.
- Claims specifying the particle size distribution of tadalafil, ensuring at least 90% of the particles are below 40 microns[1].
Process Claims
- Claims detailing the melt granulation process and hot melt extrusion technology used to prepare the compositions.
- Claims outlining the steps involved in blending, extruding, and formulating the final dosage form[1].
Method of Administration Claims
- Claims related to the method of treating diseases such as male erectile dysfunction, female sexual arousal disorder, benign prostatic hyperplasia, and pulmonary hypertension by administering the described pharmaceutical compositions[1].
Patent Landscape
Related Patents
Other patents, such as U.S. Pat. No. 5,859,006 and U.S. Pat. No. 6,821,975, also relate to tadalafil formulations but focus on different aspects like the free drug particulate form and specific particle size distributions[1].
Litigation and IPR
The patent has been subject to inter partes review (IPR) decisions by the Patent Trial and Appeal Board. ICOS Corporation appealed these decisions, which held claims 1–32 of U.S. Patent No. 7,182,958 invalid. This highlights the ongoing legal battles and challenges in maintaining patent validity in the pharmaceutical sector[5].
Expiration and Generic Entry
The patent's expiration date and potential generic entry are critical for understanding the market landscape. As of the last update, detailed information on the patent's expiration and generic entry can be found through patent watch services[2].
Metrics for Patent Scope
The scope of a patent can be measured using various metrics, such as independent claim length and independent claim count. These metrics help in assessing the breadth and clarity of patent claims. For instance, narrower claims are associated with a higher probability of grant and a shorter examination process[3].
Impact on Innovation
The patent's scope and claims can significantly impact innovation in the pharmaceutical industry. Broad or unclear claims can lead to increased licensing and litigation costs, potentially diminishing incentives for innovation. Conversely, well-defined and narrow claims can facilitate clearer boundaries and encourage further research and development[3].
Conclusion
United States Patent 7,182,958 is a comprehensive patent that covers critical aspects of tadalafil formulations, including composition, preparation process, and method of administration. Understanding the scope and claims of this patent is essential for navigating the complex landscape of pharmaceutical patents.
Key Takeaways
- Pharmaceutical Compositions: The patent covers tadalafil compositions with specified excipients and particle size distributions.
- Preparation Process: A melt granulation process with hot melt extrusion technology is detailed.
- Dosage Forms: Various dosage forms are possible, with optional coating.
- Claims: Composition, process, and method of administration claims are included.
- Patent Landscape: Related patents, litigation, and expiration dates are important considerations.
- Impact on Innovation: The patent's scope affects innovation and legal challenges in the pharmaceutical industry.
FAQs
Q: What is the primary active ingredient in the pharmaceutical compositions described in U.S. Patent 7,182,958?
A: The primary active ingredient is tadalafil, a PDE5 inhibitor.
Q: What is the significance of the particle size of tadalafil in the compositions?
A: The particle size is crucial, with at least 90% of the particles needing to be less than about 40 microns for optimal stability and in-vitro dissolution.
Q: What process is used to prepare the pharmaceutical compositions?
A: A melt granulation process followed by hot melt extrusion technology is used.
Q: What conditions are treated by administering the described pharmaceutical compositions?
A: Conditions such as male erectile dysfunction, female sexual arousal disorder, benign prostatic hyperplasia, and pulmonary hypertension are treated.
Q: Has U.S. Patent 7,182,958 been subject to any legal challenges?
A: Yes, it has been subject to inter partes review (IPR) decisions by the Patent Trial and Appeal Board.
Sources:
- U.S. Pat. No. 7,182,958 - Pharmaceutical compositions comprising tadalafil - Google Patents
- DrugPatentWatch - Drugs covered by patent 7182958
- Hoover Institution - Patent Claims and Patent Scope
- U.S. Pat. No. 7182958B1 - β-carboline pharmaceutical compositions
- FindLaw - ICOS CORPORATION v. ACTELION PHARMACEUTICALS LTD[1][2][4][5]
