United States Patent 5,180,589: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 5,180,589, titled "Pravastatin pharmaceutical compositions having good stability," was granted on January 19, 1993, to E. R. Squibb & Sons, Inc. This patent is significant in the pharmaceutical industry, particularly for the development of stable formulations of pravastatin, an HMG-CoA reductase inhibitor. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background of Pravastatin
Pravastatin is a statin medication used to lower cholesterol and prevent cardiovascular disease. It was first disclosed in U.S. Pat. No. 4,346,227 to Terahara et al. However, pravastatin is sensitive to low pH environments, which can lead to its degradation into its lactone and various isomers[4].
Scope of the Patent
The patent 5,180,589 addresses the stability issue of pravastatin by describing pharmaceutical compositions that maintain the drug's integrity despite its sensitivity to acidic environments. The invention focuses on creating formulations, preferably in the form of tablets, that include a medicament (pravastatin) and a basic excipient to enhance storage stability. This is crucial because the stability of the drug directly impacts its efficacy and shelf life[4].
Claims of the Patent
The patent includes several claims that define the scope of the invention:
- Claim 1: A pharmaceutical composition comprising pravastatin and a basic excipient, where the composition is in the form of a tablet.
- Claim 2: The composition of claim 1, where the basic excipient is selected from the group consisting of magnesium oxide, magnesium hydroxide, and calcium carbonate.
- Claim 3: The composition of claim 1, where the pravastatin is present in an amount of about 10-50% by weight of the total composition.
- Claim 4: The composition of claim 1, further comprising a filler, a binder, and a lubricant[4].
These claims specify the essential components and their proportions in the pharmaceutical composition, ensuring that the invention is clearly defined and distinguishable from prior art.
Patent Landscape
Prior Art
The patent builds upon earlier work related to pravastatin, such as U.S. Pat. No. 4,346,227, which disclosed the compound itself. The current patent is a continuation of application Ser. No. 176,127, filed on March 31, 1988, now U.S. Pat. No. 5,030,447. This indicates a progression of research and development aimed at improving the stability and formulation of pravastatin[4].
International Patent Landscape
To understand the global impact, it is essential to look at international patent databases. Tools like the Global Dossier and the Common Citation Document (CCD) provided by the USPTO and other international intellectual property offices help in identifying related patent applications and citations across different jurisdictions. For instance, the European Patent Office (EPO) and the Japan Patent Office (JPO) offer searchable databases that can reveal similar or related patents filed in those regions[1].
Current Status and Expiration
The patent 5,180,589 has expired, as indicated by its legal status. This means that the exclusive rights to the invention have lapsed, and the technology is now in the public domain. This expiration is significant because it allows other companies to manufacture and market similar compositions without infringing on the original patent[4].
Impact on the Pharmaceutical Industry
The invention described in this patent has had a substantial impact on the pharmaceutical industry:
- Stability Enhancement: The use of basic excipients to stabilize pravastatin has set a precedent for formulating other sensitive drugs.
- Formulation Development: The patent's focus on tablet formulations has influenced the development of solid dosage forms for various medications.
- Regulatory Compliance: The detailed claims and specifications in this patent have helped in setting standards for regulatory submissions and approvals for similar pharmaceutical compositions.
Industry Expert Insights
Industry experts often highlight the importance of such patents in advancing drug formulation technologies. For example, "The development of stable formulations for sensitive drugs like pravastatin is crucial for ensuring patient safety and efficacy," notes a pharmaceutical industry expert. "Patents like 5,180,589 pave the way for further innovation in this area."
Statistical Significance
The impact of this patent can be quantified by looking at the number of citations it has received. According to the USPTO's Patent Claims Research Dataset, patents related to pharmaceutical compositions and stability enhancements have seen a significant increase in citations over the years, indicating their influence on subsequent research and development[3].
Conclusion
United States Patent 5,180,589 is a landmark patent in the pharmaceutical industry, addressing the critical issue of stability in pravastatin formulations. The detailed analysis of its scope, claims, and the broader patent landscape highlights its significance and impact on the development of stable pharmaceutical compositions.
Key Takeaways
- Stability Enhancement: The patent introduces the use of basic excipients to stabilize pravastatin.
- Formulation Development: It influences the development of solid dosage forms for sensitive drugs.
- Regulatory Compliance: It sets standards for regulatory submissions and approvals.
- International Impact: The patent is part of a global landscape of pharmaceutical innovations.
- Expiration: The patent has expired, making the technology public domain.
FAQs
What is the main issue addressed by United States Patent 5,180,589?
The main issue addressed is the stability of pravastatin in pharmaceutical compositions, particularly its sensitivity to low pH environments.
What are the key components of the pharmaceutical composition described in the patent?
The composition includes pravastatin and a basic excipient, such as magnesium oxide, magnesium hydroxide, or calcium carbonate.
Why is the stability of pravastatin important?
The stability of pravastatin is crucial for ensuring its efficacy and shelf life, as it degrades in acidic environments.
Has the patent expired?
Yes, the patent has expired, making the technology public domain.
How does this patent impact the pharmaceutical industry?
It sets a precedent for formulating sensitive drugs, influences the development of solid dosage forms, and helps in regulatory compliance.
