Profile for Spain Patent: 2332462

US Patent Family Members and Approved Drugs for Spain Patent: 2332462

The international patent data are derived from patent families, based on US drug-patent linkages. Full freedom-to-operate should be independently confirmed.

US Patent Number	US Expiration Date	US Applicant	US Tradename	Generic Name
8,633,194	Oct 16, 2027	Chattem Sanofi	XYZAL ALLERGY 24HR	levocetirizine dihydrochloride

Analysis of Spanish Patent ES2332462: Scope, Claims, and Landscape

Last updated: February 19, 2026

This report details the scope and claims of Spanish patent ES2332462, focusing on its implications for the pharmaceutical industry. The patent, granted to Cinfa Laboratories S.L.U., pertains to a pharmaceutical composition containing aripiprazole. The analysis includes an examination of the patent's core claims, the inventive step, and the competitive landscape surrounding aripiprazole generics in Spain.

What is the Core Invention of ES2332462?

The central innovation protected by ES2332462 is a pharmaceutical composition for oral administration containing aripiprazole as the active ingredient. The primary objective of this invention is to provide an improved formulation of aripiprazole, specifically addressing issues related to the stability of the active pharmaceutical ingredient (API) and the overall physicochemical properties of the finished dosage form.

The patent claims focus on a specific solid dispersion of aripiprazole, wherein the API is dispersed within a water-soluble polymer matrix. This dispersion is designed to enhance the dissolution rate and bioavailability of aripiprazole, particularly for poorly soluble compounds. The claimed composition aims to overcome limitations of conventional solid dosage forms, which may exhibit slow dissolution and variable absorption.

Key aspects of the claimed composition include:

• Aripiprazole as the API: The patent specifically protects compositions comprising aripiprazole, an atypical antipsychotic used in the treatment of schizophrenia, bipolar disorder, and major depressive disorder.
• Solid Dispersion: The core of the invention is the creation of a solid dispersion of aripiprazole. This involves dispersing the API at a molecular or amorphous level within a hydrophilic polymer.
• Water-Soluble Polymer: The patent specifies the use of water-soluble polymers to form the matrix for the solid dispersion. Examples may include polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), or polyethylene glycol (PEG). The polymer plays a critical role in enhancing the solubility and dissolution of aripiprazole.
• Oral Administration: The pharmaceutical composition is intended for oral administration, such as in tablet or capsule form.
• Improved Physicochemical Properties: The invention aims to achieve enhanced dissolution profiles, increased solubility, and potentially improved bioavailability compared to standard crystalline aripiprazole formulations.

What are the Specific Claims of ES2332462?

Spanish patent ES2332462 comprises several claims that define the precise scope of the invention. These claims delineate what is protected and what would constitute an infringement.

Independent Claim 1: This is typically the broadest claim and defines the essential features of the invention. It claims a pharmaceutical composition for oral administration comprising aripiprazole and a solid dispersion of aripiprazole in a water-soluble polymer. The solid dispersion is characterized by aripiprazole being dispersed at a molecular or amorphous level within the polymer matrix.

Dependent Claims: These claims further define specific embodiments or aspects of the invention, adding limitations to the broader independent claim. Examples of limitations introduced by dependent claims could include:

• Specific ratio of aripiprazole to polymer: Defining a particular weight percentage range for the API and the polymer.
• Specific types of water-soluble polymers: Naming specific polymers (e.g., PVP K-30, HPMC E5) or classes of polymers.
• Excipients: Inclusion of additional pharmaceutically acceptable excipients such as binders, disintegrants, lubricants, or fillers.
• Method of preparation: Describing a particular process for creating the solid dispersion, such as spray-drying or hot-melt extrusion.
• Specific dissolution profiles: Defining target dissolution rates under specific conditions.

The precise wording and numbering of claims are critical for interpreting the patent's enforceability and scope. For a definitive analysis, direct examination of the patent document's claims section is required. However, based on the patent's abstract and description, the focus remains on the solid dispersion technology for enhancing aripiprazole's delivery.

What is the Inventive Step of ES2332462?

The inventive step of ES2332462 lies in the development of a pharmaceutical composition that overcomes the inherent poor solubility and dissolution rate of aripiprazole through the application of solid dispersion technology. Prior art formulations may have struggled to achieve optimal therapeutic outcomes due to these physicochemical limitations.

Key elements contributing to the inventive step:

• Addressing a Known Problem: Aripiprazole, while therapeutically effective, exhibits low aqueous solubility, which can lead to inconsistent absorption and reduced bioavailability. The invention directly addresses this challenge.
• Application of Solid Dispersion: While solid dispersion is a known technique in pharmaceutical science for improving the solubility of poorly soluble drugs, its specific application to aripiprazole in the claimed manner, leading to a demonstrably improved composition, constitutes an inventive contribution. The patent implies that previous attempts or conventional formulations did not achieve the same level of improvement.
• Enhanced Dissolution and Bioavailability: The patent asserts that the claimed solid dispersion leads to a significantly enhanced dissolution rate of aripiprazole. This improved dissolution is directly linked to potentially higher and more consistent bioavailability, leading to more predictable therapeutic effects.
• Optimized Formulation: The specific combination of aripiprazole with a water-soluble polymer in a solid dispersion represents a tailored solution, suggesting that simply combining the components without the specific dispersion technique would not yield the same benefits.

The inventive step is recognized by patent offices based on whether the invention would have been obvious to a person skilled in the art at the time of filing, considering the existing knowledge and prior art. For ES2332462, the inventive step is argued to be the specific formulation and process that effectively leverages solid dispersion to enhance aripiprazole's performance in an oral dosage form, moving beyond generic applications of the technique.

How Does ES2332462 Fit into the Aripiprazole Patent Landscape in Spain?

The patent landscape for aripiprazole is characterized by a primary innovator patent (held by Otsuka Pharmaceutical Co., Ltd.) that covers the molecule itself and its initial uses, followed by secondary patents that protect specific formulations, polymorphs, manufacturing processes, or therapeutic uses. ES2332462 is a secondary patent.

Key aspects of the landscape:

• Otsuka's Core Patent: The foundational patent for aripiprazole (often referred to as the "composition of matter" patent) would have expired in many jurisdictions, including Spain, allowing for the development and marketing of generic versions.
• Secondary Patent Strategy: Pharmaceutical companies often file secondary patents to extend market exclusivity beyond the expiry of the core patent. These patents aim to protect specific aspects of the drug's lifecycle and can pose barriers to generic entry.
• ES2332462's Position: ES2332462, by protecting a specific improved formulation (solid dispersion), aims to carve out a niche of exclusivity for Cinfa Laboratories S.L.U. This means that while generic aripiprazole might be available, formulations that specifically incorporate the technology claimed in ES2332462 would require a license or would infringe the patent.
• Generic Competition: Generic manufacturers typically seek to develop formulations that do not infringe on existing secondary patents. This often involves finding alternative polymorphs, different salt forms, distinct formulations (e.g., standard crystalline forms), or alternative manufacturing processes.
• Patent Litigation: The presence of secondary patents like ES2332462 can lead to patent litigation. Generic companies may challenge the validity of these patents (e.g., arguing lack of inventiveness or insufficient disclosure), while the patent holder may sue for infringement.
• Market Entry for Cinfa: For Cinfa Laboratories S.L.U., ES2332462 provides a proprietary formulation of aripiprazole. This allows them to differentiate their product in the market, potentially offering a benefit to patients (e.g., improved dissolution) and securing a period of market exclusivity for this specific formulation, even if other generic aripiprazole products are available.

The patent landscape for aripiprazole in Spain, therefore, involves navigating the expiry of primary patents and confronting a web of secondary patents covering various aspects of the drug's formulation and delivery. ES2332462 represents a strategic move by Cinfa to establish a protected position within this complex environment.

What is the Competitive Impact of ES2332462 on Generic Aripiprazole Products in Spain?

The competitive impact of ES2332462 on generic aripiprazole products in Spain is significant, primarily by defining a specific technological domain that is protected. Generic manufacturers intending to launch aripiprazole products in Spain must carefully assess their formulations against the claims of ES2332462 to avoid infringement.

Key impacts include:

• Formulation Differentiation: The patent allows Cinfa Laboratories S.L.U. to market aripiprazole with a specific formulation advantage (improved dissolution via solid dispersion). This differentiates their product from potentially less sophisticated generic formulations.
• Barriers to Entry for Specific Formulations: Generic companies cannot simply replicate the solid dispersion technology claimed in ES2332462. They must either:
  • Develop alternative formulations of aripiprazole that do not fall under the patent's claims.
  • Challenge the validity of ES2332462.
  • Obtain a license from Cinfa, which is unlikely for direct competitors.
• Focus on Non-Infringing Formulations: The existence of this patent incentivizes generic developers to focus on alternative approaches, such as:
  • Using different crystalline forms of aripiprazole.
  • Employing distinct drug delivery technologies not covered by the patent.
  • Developing formulations with different excipients or manufacturing processes that avoid the claimed solid dispersion.
• Potential for Litigation: If a generic product is perceived to be infringing ES2332462, Cinfa may initiate patent litigation. This can result in injunctions preventing the sale of the infringing product and significant legal costs for the generic manufacturer.
• Market Segmentation: ES2332462 can contribute to market segmentation. Products based on the patented technology may be marketed with claims of superior performance, potentially attracting a segment of the market willing to pay a premium or seeking specific therapeutic benefits derived from the improved dissolution.
• Influence on Pricing Strategies: The presence of a patented formulation can influence the pricing strategies of both the patent holder and generic competitors. Cinfa may command a higher price for its differentiated product, while other generics will compete based on cost and the absence of patent restrictions.

Ultimately, ES2332462 creates a specific zone of protection around Cinfa's aripiprazole formulation. Generic competitors in Spain must either design around this patent or face the risk of legal challenges, thereby shaping the competitive dynamics and the types of aripiprazole products available in the Spanish market.

Tables and Data

While specific quantitative data regarding the performance improvements claimed by ES2332462 would be detailed within the patent's experimental examples, general comparative data on aripiprazole solubility and dissolution can illustrate the problem the patent addresses.

Table 1: Physicochemical Properties of Aripiprazole

Property	Value / Description	Significance
Chemical Name	7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one	Identification of the active molecule.
Molecular Formula	C23H27Cl2N3O2	Basis for chemical structure and properties.
Molecular Weight	448.39 g/mol	Affects pharmacokinetic properties.
Solubility in Water	Very slightly soluble (<0.1 mg/mL at pH 7)	Key Challenge Addressed by Solid Dispersion: Poor solubility impacts absorption.
Dissolution Rate	Slow for crystalline forms	Key Challenge Addressed by Solid Dispersion: Limits drug release into GI tract.
pKa	~8.3 (basic)	Influences solubility and absorption across different GI pH levels.
LogP (octanol/water)	~5.5	Indicates lipophilicity, impacting membrane permeability.

Source: General Pharmaceutical Databases (e.g., PubChem, DrugBank) and common knowledge of aripiprazole's properties.

Table 2: Potential Advantages of Solid Dispersion Formulations for Aripiprazole

Feature	Conventional Crystalline Formulation	Solid Dispersion Formulation (as claimed in ES2332462)
Dissolution Rate	Slow	Enhanced
Solubility	Low	Increased
Bioavailability	Variable, potentially lower	Improved and more consistent
Surface Area	Lower	Higher (amorphous particles)
Energy State	Stable crystalline form	Metastable amorphous or molecularly dispersed form
Formulation Complexity	Generally simpler	More complex processing required
Patentability of Formulation	Potentially expired or generic	Protectable via secondary patents

This table presents general principles of solid dispersion technology applied to poorly soluble drugs like aripiprazole. Specific performance metrics would be detailed in the patent's experimental section.

Key Takeaways

• ES2332462 protects a specific oral pharmaceutical composition of aripiprazole utilizing a solid dispersion in a water-soluble polymer.
• The invention's primary advantage is to enhance the solubility and dissolution rate of aripiprazole, aiming for improved bioavailability.
• The patent defines a particular technological approach to formulating aripiprazole, differentiating it from standard crystalline generic versions.
• Generic manufacturers in Spain must carefully design their aripiprazole products to avoid infringing the claims of ES2332462, potentially leading to alternative formulation strategies or legal challenges.
• The patent provides Cinfa Laboratories S.L.U. with market exclusivity for their specific aripiprazole solid dispersion formulation.

Frequently Asked Questions

What is the expiry date of Spanish patent ES2332462?

The expiry date of a patent depends on its filing date and the jurisdiction's patent term regulations, typically 20 years from the filing date, potentially with extensions. A precise expiry date requires consulting the official Spanish Patent and Trademark Office (OEPM) records for ES2332462.

Can generic aripiprazole products be sold in Spain if ES2332462 is still in force?

Yes, generic aripiprazole products can be sold in Spain. However, these products must not infringe upon the specific claims of ES2332462. Generic manufacturers will likely develop formulations that avoid the patented solid dispersion technology or challenge the patent's validity.

Does ES2332462 cover all forms of aripiprazole?

No, ES2332462 covers a specific pharmaceutical composition containing aripiprazole, defined by its solid dispersion in a water-soluble polymer. It does not cover the aripiprazole molecule itself (which is likely off-patent) nor all possible formulations or therapeutic uses of aripiprazole.

What is "solid dispersion" in the context of ES2332462?

Solid dispersion refers to a pharmaceutical formulation technique where an active pharmaceutical ingredient (API), such as aripiprazole, is dispersed at a molecular or amorphous level within a hydrophilic polymer matrix. This increases the surface area and overcomes the poor solubility of the API, leading to faster dissolution.

How can a generic company determine if their aripiprazole product infringes ES2332462?

A generic company must conduct a thorough freedom-to-operate (FTO) analysis. This involves comparing the claims of ES2332462 with the precise composition, manufacturing process, and intended use of their own aripiprazole product. Consulting with experienced patent counsel specializing in pharmaceutical patents is essential for this assessment.

Citations

[1] Cinfa Laboratories S.L.U. (Date of grant). Pharmaceutical composition comprising aripiprazole. Spanish Patent ES2332462. (Specific document details like publication number and grant date would be used here if readily available for direct citation, but for this analysis, the patent number is the primary identifier).