United States Patent 7,226,614: A Detailed Analysis
Overview of the Patent
United States Patent 7,226,614, titled "Tablet comprising cetirizine and pseudoephedrine," is a pharmaceutical patent that describes a specific formulation and method of treatment for allergic disorders. Here is a detailed analysis of its scope, claims, and the surrounding patent landscape.
Background and Objectives
The patent, filed by UCB, Inc., aims to provide a combination of cetirizine and pseudoephedrine in a single tablet, enhancing the treatment efficacy for conditions such as rhinitis, cold, flu, and similar symptoms. The primary objectives include increasing treatment efficiency while minimizing adverse effects[1].
Patent Scope
Pharmaceutical Composition
The patent describes a tablet composed of two distinct segments, each containing a different active ingredient: cetirizine and pseudoephedrine. Cetirizine is an antihistamine, while pseudoephedrine is a sympathomimetic drug known for its decongestant properties. The segments are designed to maintain the pharmacokinetic profiles of each drug as if they were administered separately[1].
Segment Design
The tablet can be formulated in various ways, such as a bilayer tablet, where each layer contains a different active ingredient. The segments may also be particles fully or partially covered by a coating. The weight ratio of the pseudoephedrine layer to the cetirizine layer is specified to be between 0.25 to 10, with a preferred range of 2 to 6[1].
Excipients and Stability
The cetirizine segment includes excipients like lactose, a polyhydroxyl compound, to enhance stability. The pseudoephedrine segment may include disintegrants such as sodium starch glycolate or cross-linked carboxy methyl cellulose. The presence of an alkalinizing agent can improve the stability profile of the composition[1].
Claims
The patent includes several key claims:
- A method of treating allergic disorders by administering a tablet with distinct segments containing cetirizine and pseudoephedrine.
- The tablet design ensures that the pharmacokinetic profiles of both drugs are maintained as if they were administered separately.
- Specific weight ratios and excipient compositions are claimed to optimize the formulation[1].
Patent Landscape
Related Patents
The patent is part of a broader portfolio related to the combination of cetirizine and pseudoephedrine. Other relevant patents include U.S. Patent Nos. 6,469,009 and 7,014,867, which also cover aspects of this combination and its use. These patents were involved in litigation regarding generic versions of the product, highlighting their importance in the pharmaceutical landscape[2][4].
Litigation and Enforcement
The patent was central to a legal dispute involving UCB, Inc., and InvaGen, where InvaGen sought to market a generic version of the product before the patent's expiration. UCB, Inc., alleged infringement and sought an injunction to prevent InvaGen from commercializing the product until the patent expired[2].
Expiration and Generic Competition
The patent expired on June 10, 2022, allowing for the entry of generic versions into the market. Generic drug manufacturers had to submit ANDAs (Abbreviated New Drug Applications) with Paragraph IV certifications, stating that the patent was invalid, unenforceable, or would not be infringed by their products[4].
Impact on Pharmaceutical Industry
The combination of cetirizine and pseudoephedrine in a single tablet has been significant in treating allergic disorders. The patent's expiration has opened the market to generic competition, potentially reducing costs and increasing accessibility for patients.
Key Takeaways
- Combination Therapy: The patent describes a combination of cetirizine and pseudoephedrine in a single tablet, enhancing treatment efficacy for allergic disorders.
- Segment Design: The tablet is designed with distinct segments to maintain the pharmacokinetic profiles of each drug.
- Excipients and Stability: Specific excipients and an alkalinizing agent are used to enhance stability.
- Patent Landscape: The patent is part of a broader portfolio and was involved in significant litigation regarding generic competition.
- Expiration and Generic Competition: The patent's expiration has allowed for the entry of generic versions into the market.
FAQs
Q: What are the active ingredients in the tablet described by U.S. Patent 7,226,614?
A: The active ingredients are cetirizine, an antihistamine, and pseudoephedrine, a sympathomimetic drug.
Q: What is the design of the tablet according to the patent?
A: The tablet is composed of two distinct segments, each containing one of the active ingredients, and can be formulated as a bilayer tablet or particles with coatings.
Q: What is the significance of the weight ratio between the pseudoephedrine and cetirizine segments?
A: The weight ratio is specified to be between 0.25 to 10, with a preferred range of 2 to 6, to optimize the pharmacokinetic profiles of both drugs.
Q: Why is the presence of an alkalinizing agent important in this formulation?
A: The alkalinizing agent improves the stability profile of the pharmaceutical composition.
Q: When did the patent expire, and what was the impact on the market?
A: The patent expired on June 10, 2022, allowing generic versions of the product to enter the market, potentially reducing costs and increasing accessibility for patients.
Cited Sources
- US7226614B2 - Tablet comprising cetirizine and pseudoephedrine - Google Patents
- IN THE UNITED STATES DISTRICT COURT FOR THE EASTERN DISTRICT OF NEW YORK - Insight.RPXcorp
- A novel approach to understand patents from the drug discovery perspective - bioRxiv
- ANDA 090922 - accessdata.fda.gov - FDA
