Who holds the patent for Albuterol?

Introduction to Albuterol 
Albuterol (also known as salbutamol in many regions) is a well‐established β₂-adrenoreceptor agonist used extensively in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Its pharmacological action involves the relaxation of bronchial smooth muscles to facilitate easier breathing, and over the decades, a variety of formulations and administration methods have been developed to optimize its use in diverse clinical settings. The evolution of albuterol from early basic formulations to sophisticated aerosol and inhalation devices underscores both the drug’s pivotal role in respiratory therapy and the competitive innovations that drive its development.

Pharmacological Overview 
Albuterol’s mechanism of action is centered on its ability to stimulate β₂-adrenoreceptors, causing bronchodilation and reducing airway resistance. This pharmacodynamic profile makes it an essential rescue medication for acute bronchospasm, as well as a maintenance therapy in obstructive lung diseases. Its rapid onset of action and favorable safety profile compared with other sympathomimetic agents have contributed to its enduring clinical utility. The drug’s versatility is evident from its presence in multiple dosage forms such as tablets, aerosol inhalation solutions, and injectable formulations, each fine-tuned to meet specific patient needs and clinical indications.

Historical Development 
Since its introduction, albuterol has undergone significant refinement. Early reliance on simple formulations has gradually been supplanted by advanced delivery systems. Innovations span from oral solid dosage forms to complex inhalation systems that integrate metered dose delivery with sophisticated dosing indicators. The progression in formulation not only aimed at maximizing efficacy and convenience but also at addressing regulatory and competitive market dynamics. This evolution paved the way for a myriad of patents covering various aspects of albuterol, from its synthesis and formulation methods to specific delivery devices tailored for both pediatric and adult populations.

Patent Information 
The patent landscape for albuterol is notably complex and fragmented. It is important to understand that there is no single patent or single patent holder covering albuterol in its entirety. Instead, multiple patents cover a broad spectrum of innovations related to albuterol—from its chemical formulations and preparation methods to the design of inhalation devices and novel lipid aerosol forms.

Current Patent Holder 
Multiple entities hold patents related to albuterol (or salbutamol) reflecting the range of intellectual property that protects different facets of the drug: 

- Formulation and Composition Patents: 
- One patent, US11484513B2, is assigned to REKIK, RAOUF. This patent exemplifies the extension of albuterol’s use into ophthalmic applications, highlighting the drug’s versatility beyond respiratory indications. 
- Another patent, CN113456590B, the current assignee of this patent is China Pharmaceutical University Pharmaceutical, illustrating innovations in drug delivery where albuterol is encapsulated in liposomes to enhance stability and facilitate inhalation, particularly for vulnerable populations such as children and the elderly. 

- Process and Preparation Method Patents: 
- A preparation method for racemic salbutamol detailed in CN112592280B. This patent highlights innovation in chemical synthesis routes, utilizing novel intermediates and catalytic processes to reduce costs and improve yields. 
- Additional patents cover advanced preparation processes, such as the salbutamol sulfate aerosol inhalation solution by Shanghai Sine Pharmaceutical and Shanghai Xinyi Jinzhu Pharmaceutical. There are also patents from companies like Beijing Yunpeng Pengcheng Pharmaceutical Technology that focus on tablet formulations for albuterol sulfate. 

- Device and Inhalation System Patents: 
- Inhaler systems, which integrate both the medication and the device required for proper administration, are also covered under albuterol-related patents. For example, a patent granted to NORTON(WATERFORD) LIMITED describes an inhaler system that distinguishes types of medicament usage, addressing both rescue and maintenance therapies. 
- It should be noted that in the context of inhaler devices, a major case involving Teva Pharmaceuticals revealed that while Teva held patents related to the inhaler device (ProAir HFA), these patents did not extend to the albuterol sulfate formulation itself. This distinction emphasizes that even when a company appears to hold significant intellectual property in this space, it may be limited to delivery mechanisms rather than the drug substance per se.

- Other Notable Holders: 
- CARDIX THERAPEUTICS LLC holds patents focused on pharmaceutical compositions intended for treating cardiovascular diseases that incorporate albuterol as one of the active compounds. 
- Shanghai Fangyu Health Pharmaceutical Technology and Shijiazhuang No. 4 Pharmaceutical have contributed to the landscape with patents detailing intermediates and injection formulations, respectively, which are critical for ensuring the quality and stability of the final product. 
- Additionally, Sichuan Purity Pharmaceutical and Sichuan Ren'An Pharmaceutical hold patents for compound aerosol inhalation suspensions and efficient preparation methods of salbutamol sulfate, further illustrating the diversification of albuterol-related intellectual property.

Overall, the current patent holders for albuterol span academic institutions, specialized pharmaceutical companies, and larger commercial entities that have developed niche formulations or proprietary methods. This diverse ownership underlines the competitive nature of albuterol’s patent portfolio and the layered protection strategies employed by different stakeholders.

Patent Details and Claims 
The patents relating to albuterol are highly detailed and encompass multiple aspects of the drug’s formulation, method of use, and manufacturing process: 

- Chemical Composition and Synthesis Methods: 
These patents detail novel routes to synthesize albuterol or racemic salbutamol, using specific intermediates or catalysts. For example, the patent from CN112592280B discusses a preparation method using 5-bromosalicylaldehyde as the starting material, thereby reducing production costs and improving reaction selectivity. Similarly, other patents target the removal of impurities and control of residual elements such as boron through precise pH adjustments. 

- Formulation Enhancements: 
Formulation patents cover aerosol solutions, tablets, and injections. Each patent outlines methods to improve atomization, thermal stability, and delivery efficiency. For instance, the salbutamol sulfate aerosol inhalation solution patent (CN112402400B) describes a formulation with a pH range of 3.0 to 5.0, thereby achieving both efficacy and stability in the final product. Patent claims in this category thereby emphasize factors such as particle size distribution and the physical stability of the aerosol or tablet, ultimately influencing patient compliance and therapeutic outcomes.

- Device Integration and Delivery Technology: 
Patents related to inhaler systems focus on the integration of a drug delivery device with electronic features for usage monitoring. The system developed by NORTON(WATERFORD) LIMITED not only ensures proper drug administration but also incorporates encryption and usage parameter monitoring, which enhances regulatory compliance and patient adherence. Additionally, the Teva case highlighted that patents tied to device configurations do not automatically translate to exclusivity over the albuterol sulfate formulation itself. 

- Synergistic Compositions and Combination Therapies: 
Some patents extend albuterol’s utility into combination therapies, where it is combined with agents such as budesonide to create compound aerosol suspensions. Such patents, for instance by Sichuan Purity Pharmaceutical, claim innovative methods that lead to higher delivery efficiency and stability of the compound formulations. These patents are crucial from a market standpoint as they offer competitive advantages in therapeutic efficacy and patient convenience.

Market and Legal Implications 
The extensive and multifaceted patent portfolio related to albuterol has significant implications for market availability and legal frameworks within the pharmaceutical industry.

Impact on Market Availability 
The broad range of patents and the multiplicity of holders collectively contribute to prolonged market exclusivity for specific formulations and delivery systems of albuterol. This complex intellectual property landscape can delay the entry of generic competitors into the market, thereby maintaining higher price points for innovator products. For instance, even though the core molecule (albuterol sulfate) may have been researched and developed decades ago, the strategic layering of patents around novel formulations, manufacturing processes, and device technologies creates sustained protection that enhances market exclusivity.

In addition, patents targeting peripheral or incremental improvements to the original product, such as improved stability, enhanced delivery systems, or refined dosing mechanisms, extend the innovator companies’ ability to differentiate their products in a competitive market. This strategy is evident in the diversity of patented formulations ranging from ophthalmic medicaments to lipid aerosols, which cater to specific patient demographics and clinical needs.

Legal Considerations 
From a legal perspective, the albuterol patent landscape presents several noteworthy challenges and considerations: 

- Patent Scope and Validity: 
The scope of patents—whether they cover the active ingredient, the formulation process, or the delivery device—significantly influences their enforceability. Legal disputes such as the one involving Teva Pharmaceuticals emphasize that while a company might hold patents for certain aspects of a drug-device combination, these claims do not necessarily extend to the drug formulation itself. As evidenced by the Teva ruling, patents listed on the FDA's Orange Book may later be subject to legal scrutiny regarding their actual scope. 

- Patent Infringement and Litigation: 
The diversified nature of albuterol-related patents often leads to litigation over overlapping claims, particularly when different entities claim innovations on similar aspects of the drug or device. The dynamic interplay between various patent holders, such as those holding patents through academic institutions versus large pharmaceutical companies, can result in protracted legal battles over infringement and the validity of specific claims.

- Regulatory and Compliance Implications: 
The enforcement and maintenance of these patents are also governed by regulatory frameworks at national and international levels. Patent term extensions, compulsory licensing, and the nuances of patent term adjustments can influence both the strategy of the patent holders and the eventual market entry of generics. The detailed claims on manufacturing processes and formulation specifics must comply with strict FDA and international standards, which further complicate the legal environment.

Future Prospects 
Looking ahead, the evolving patent landscape for albuterol continues to shape market dynamics and innovation strategies.

Patent Expiration and Generic Entry 
While many patents related to albuterol are designed to ensure long-term exclusivity through incremental innovations and improved formulations, a number of these patents are approaching their expiration dates. As patents expire, generic manufacturers gain opportunities to enter the market, potentially leading to substantial price reductions. For example, patents such as those held by Shanghai Xinyi Jinzhu Pharmaceutical, Beijing Yunpeng Pengcheng Pharmaceutical Technology illustrate the strategy of securing exclusive rights for a finite period before facing generic competition. 

Moreover, the expiration of key patents related to specific formulations (e.g., aerosol inhalation solutions or tablets) may pave the way for diversified generic offerings. However, the fragmented nature of the patent holdings means that while one patent may expire, others covering different aspects (such as device design or novel preparation methods) may still be in effect, creating a staggered and complex timeline for generic entry.

Innovation and New Developments 
The intense competition in the albuterol market continues to drive further innovation. Companies remain invested in discovering new methods of formulation, improving delivery mechanisms, and integrating digital technologies into inhaler systems to provide enhanced patient data and compliance monitoring. These innovations are reflected in recent patents that not only address the core pharmacotherapy but also seek to merge therapeutic efficacy with patient-specific data analytics and enhanced usability. 

Furthermore, incremental improvements in process technology—such as the introduction of more cost-effective synthesis routes or methods to improve yield and purity—demonstrate that the patent landscape is not static but continually evolving. This evolution is supported by collaborative research efforts between academic institutions and commercial entities, ensuring that albuterol remains at the forefront of respiratory therapy innovation while also adapting to regulatory and market exigencies.

Conclusion 
In summary, the patent landscape for albuterol is exceedingly diverse and multifaceted. There is no single “patent for albuterol” or one patent holder that dominates the space. Instead, multiple entities hold patents covering a wide range of innovations—ranging from chemical synthesis and formulation methods to advanced delivery systems and digital monitoring devices. Key patent holders include REKIK, RAOUF (for an ophthalmic medicament formulation), China Pharmaceutical University Pharmaceutical (for a lipid aerosol formulation), various academic institutions , and other commercial entities like CARDIX THERAPEUTICS LLC, Shanghai Sine Pharmaceutical, and NORTON(WATERFORD) LIMITED, among others.

The legal implications of this diverse portfolio are significant, as litigation such as the Teva Pharmaceuticals case has shown that the precise scope of patent claims—whether they pertain to the formulation, the delivery device, or the overall combination product—has far-reaching effects on market exclusivity and generic entry. From a market and innovation perspective, the strategies employed by these various patent holders have both prolonged market exclusivity and spurred continuous innovation in delivery mechanisms and formulation enhancements, even as some patents approach expiration.

Ultimately, the future of albuterol’s patent portfolio will depend on ongoing advancements in pharmaceutical technology, legal frameworks addressing patent scope and term, and the competitive actions of both innovator and generic companies. This dynamic environment ensures that while some patents may expire, new ones will emerge, perpetuating a cycle of innovation that is critical for maintaining therapeutic excellence in respiratory medicine. The albuterol case thus serves as a prime example of how layered and strategic patenting can profoundly influence drug development, regulatory landscapes, and ultimately, patient access to essential medications.

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