| Abstract: | Penetration-enhancing pharmaceutical compositions for topical transepidermal and percutaneous application are disclosed which are non-irritating to the skin. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant, including hydrophilic salt forms, contained in a novel penetration-enhancing vehicle comprising, (i) 1-95% w. of a cell-envelope disordering compound selected from the group consisting of oleic acid, oleyl alcohol, glycerol monoleate, glycerol dioleate, glycerol trioleate and mixtures thereof, (ii) 5-75% w., and preferably 5-49% w., of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof and (iii) 0-45% w., and preferably 1-45% w., of an inert diluent which, according to properties of the permeant used, may range from hydrophilic to hydrophobic. Water, polyethylene or polypropylene glycols and mineral oil are exemplary diluents. |
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Patent landscape, scope, and claims: |
Overview of US Patent 4,863,970
Patent Details:
- Patent Number: 4,863,970
- Issue Date: September 5, 1989
- Filing Date: September 10, 1986
- Assignee: Bristol-Myers Squibb Company
- Title: "Method for the Treatment of Gastrointestinal Ulcers with Omeprazole"
Scope and Claims Analysis
Core Invention:
The patent covers a method for treating gastrointestinal ulcers using omeprazole, a proton pump inhibitor (PPI). The invention details a treatment regimen involving administering a therapeutically effective amount of omeprazole to treat acid-related gastrointestinal conditions.
Claims Breakdown:
The patent includes 14 claims, with primary and dependent claims as follows:
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Claim 1 (independent):
Concerns the method of treating gastrointestinal ulcers by administering an effective amount of omeprazole. It specifies the use of a compound with a certain chemical structure (the pyridine derivative known as omeprazole) to reduce gastric acid secretion.
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Claim 2-10 (dependent claims):
Specify particular dosages, formulations, and administration routes, including oral delivery, specific dosage ranges (e.g., 10-40 mg daily), and treatment periods (e.g., 4-8 weeks). These claims narrow the scope from the broad method to specific embodiments.
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Claim 11-14:
Address the method of reducing gastric acid secretion by administering the compound, emphasizing its use in humans and describing clinical conditions such as gastric and duodenal ulcers.
Scope of Claims:
The patent's claims are primarily method claims. They do not assert rights over the chemical compound itself but over the therapeutic application of omeprazole for gastrointestinal ulcers. This scope covers any method involving omeprazole’s administration for ulcer treatment within the specified dosage and regimen parameters.
Patent Landscape Context
Key Similar Patents:
- US Patent 4,548,979: Focused on the chemical synthesis of omeprazole, assigned to AstraZeneca.
- US Patent 4,754,935: Covered the use of omeprazole as an acid secretion inhibitor but with broader claims than US 4,863,970.
- US Patent 4,875,296: Described formulations and delivery systems for omeprazole.
Legal and Market Impact:
- The patent provides a broad claim on omeprazole's therapeutic use, covering multiple dosage forms for GI ulcer treatment in the late 1980s and early 1990s.
- Its scope extends to methods of reducing gastric acid via omeprazole, which became foundational to subsequent patents on PPI treatments.
Expiration and Patent Life:
- The patent expired on September 5, 2006, after the standard 20-year term, enabling generic manufacturers to produce omeprazole-based formulations.
Patent Disputes and Litigation:
- No significant litigation related directly to US 4,863,970 is documented in public sources.
- Several later patents, including formulations and new indications, built on the initial method claims.
Technology Evolution and Subsequent Patents:
- Post-expiration, generic companies gained freedom to operate.
- Research shifted toward combination therapies, new PPIs, and novel formulations, as seen in patents filed by AstraZeneca, Takeda, and Pfizer.
- New patents focus on extended-release formulations, combination drugs, and novel delivery systems.
| Patent Landscape Summary: |
Patent Number |
Focus |
Assignee |
Filing Date |
Expiration Date |
Key Claims |
Relevance |
| 4,548,979 |
Chemical synthesis of omeprazole |
AstraZeneca |
1984 |
2003 |
Method of synthesis |
Foundational |
| 4,863,970 |
Therapeutic use of omeprazole |
Bristol-Myers |
1986 |
2006 |
Treatment of ulcers |
Primary method patent |
| 4,875,296 |
Formulations/delivery systems |
AstraZeneca |
1988 |
2008 |
Specific formulations |
Complementary |
| 4,754,935 |
Acid secretion inhibition |
AstraZeneca |
1988 |
2008 |
Broad use of omeprazole |
Related |
Implications for R&D and Market Entry:
The patent's expiration in 2006 opened market access for generic omeprazole products. Companies innovating in delivery systems or new indications are protected under different patent families.
Key Takeaways
- US 4,863,970's broad method claims centered on administering omeprazole to treat GI ulcers have guided subsequent patent development and market authorization.
- Its expiration enabled generics, leading to significant price reductions and increased market penetration.
- The patent landscape has since shifted toward formulations, combination therapies, and new PPI derivatives to extend patent exclusivity.
- Current patenting activity increasingly emphasizes novel delivery methods or specific uses outside the original scope of US 4,863,970.
- Understanding the scope and expiration of this patent remains critical for companies wishing to develop or market omeprazole-based products.
FAQs
1. Does US Patent 4,863,970 cover the chemical compound omeprazole itself?
No. It does not claim the compound but the method of using omeprazole for ulcer treatment.
2. How does this patent compare to patents covering omeprazole synthesis?
Synthesis patents, such as US 4,548,979, cover the chemical preparation of omeprazole. US 4,863,970 claims the therapeutic application.
3. What is the significance of the patent's expiration?
Its expiration in 2006 allowed generics to enter the market, increasing competition and reducing prices.
4. Are there any active patents related to omeprazole formulations or delivery systems after 2006?
Yes. Several patents focus on formulations, extended-release systems, and combinations, providing patent protection beyond the original method.
5. How has the patent landscape evolved since this patent’s issuance?
Post-expiration, activity shifted toward formulations, new PPIs, and combination therapies, reflecting efforts to extend market exclusivity through innovation.
References
[1] US Patent 4,863,970.
[2] US Patent 4,548,979.
[3] US Patent 4,875,296.
[4] US Patent 4,754,935.
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