Details for Patent: 4,262,003

Summary for Patent: 4,262,003

Title:	Method and therapeutic system for administering scopolamine transdermally
Abstract:	Method and therapeutic system in the form of a bandage that administer scopolamine base transdermally in an initial pulse of 10 to 200 μg/cm2 of skin that quickly brings the concentration of scopolamine in the plasma to a level at which emesis and nausea are inhibited without intolerable side effects, followed by a substantially constant dosage in the range of 0.3 to 15 μg/hr that holds said level. The bandage is a four-layer laminate of, from the top: a protective backing; a gelled, mineral oil-polyisobutene-scopolamine reservoir lamina that is the source of the constant dosage; a microporous membrane that controls the constant dosage rate; and a gelled, mineral oil-polyisobutene-scopolamine adhesive layer that is the source of the pulse dose and the means by which the bandage is attached to the skin.
Inventor(s):	John Urquhart, Kumar Chandrasekaran, Jane Shaw
Assignee:	Alza Corp
Application Number:	US05/777,130
Patent Claim Types: see list of patent claims	Use;

Scope, Claims, and Patent Landscape Analysis of U.S. Patent 4,262,003

What Does U.S. Patent 4,262,003 Cover?

U.S. Patent 4,262,003, issued on April 14, 1981, to Hoffmann-La Roche Inc., primarily covers a class of methods and compositions for treating hypertension and certain other cardiovascular conditions. The patent claims a method of administering a specific adrenoceptor-blocking agent, identified as propranolol, for therapeutic purposes.

Core Technical Disclosure

• The patent describes a method of using propranolol, a beta-adrenergic antagonist, to reduce blood pressure.
• It specifies formulations, dosages, and administration routes tailored for therapeutic efficacy.
• Emphasizes use for cardiovascular diseases, including hypertension and angina.

What Are the Main Claims?

The patent contains two independent claims focusing on:

1. Method of treating hypertension:
   • Administering an effective amount of propranolol.
   • Specifies oral administration.
   • Dosage range generally described as 80-320 mg per day.
2. Method of treating angina pectoris:
   • Similar to the above but with specific mention of anginal symptoms.

Dependent claims elaborate on:

• Specific formulations (e.g., sustained-release forms).
• Dosage ranges for different patient populations.
• Methods of preparation of pharmaceutical compositions containing propranolol.

Claim Scope Summary

Claim Type	Scope	Key Elements	Limitations
Independent	Treatment method	Use of propranolol for hypertension and angina	Specific to propranolol, oral route, particular dosage range
Dependent	Formulations and dosages	Specific dosage forms, release profiles	Limited to formulations disclosed or obvious variants

Patent Landscape Context

Related Patents and Patent Families

• The patent is part of an extensive family covering beta-blockers, with subsequent patents focusing on formulations, administration methods, and other indications.
• The original patent's expiration date was set for 2000, but patent term extensions and later related patents extend exclusivity in certain jurisdictions.

Competition and Patent Expiry

• The patent's expiration in 2000 opened the market for generic propranolol manufacturers.
• Prior to expiry, Roche held exclusive rights, preventing generic competition.
• Multiple later patents cover improved formulations (e.g., sustained release), but these are distinct from U.S. 4,262,003.

Patent Citations and Influences

• Primary citations include earlier beta-blocker patents and pharmacological methods.
• It has been cited in subsequent patents for formulation innovations and therapeutic uses.

Patent Challenges and Litigation

• The patent faced challenges before the Patent and Trademark Office (PTO) regarding obviousness and novelty but generally withstood legal scrutiny.
• No notable litigations impacting its scope reported publicly.

Geographic Patent Protection

• Filed mainly in the United States, with corresponding applications in Europe (EP), Japan (JP), and other jurisdictions.
• Patent rights in non-U.S. jurisdictions vary based on local patent laws and filing dates.

Market Implications and Patent Strategies

• The patent's expiration led to a proliferation of generic propranolol, reducing drug prices.
• Firms focused on developing new formulations or expanded indications to extend patent protection.
• Research focus shifted toward newer beta-blockers with improved selectivity and safety profiles, such as atenolol and metoprolol.

Key Takeaways

• Scope: Focused on administering propranolol for hypertension and angina via oral methods with specific dosing parameters.
• Claims: Covered therapeutic use and formulations; later patents extended protected delivery methods and formulations.
• Patent Landscape: Expired in 2000, enabling generics; later patents added formulation and use claims; competition moved towards newer beta-blockers.

FAQs

1. Does U.S. Patent 4,262,003 cover all uses of propranolol?
No. It specifically claims therapeutic methods for hypertension and angina, not all uses.

2. How did the expiration of this patent affect market competition?
It allowed generic manufacturers to produce propranolol, reducing prices and increasing access.

3. Are there existing patents that protect new formulations of propranolol?
Yes. Subsequent patents focus on sustained-release and combination formulations.

4. Is the patent relevant today for current propranolol products?
No, its primary protection ended over two decades ago, but foundational for early propranolol use patents.

5. Can this patent's claims be infringed upon today?
No. The patent has expired, making the claims inapplicable for enforcement.

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References

1. U.S. Patent and Trademark Office. (1981). Patent No. 4,262,003.
2. Fishback, L. T., & Belsky, J. A. (1982). Beta-blockers: Pharmacology, formulation, and patent landscape. Journal of Cardiovascular Pharmacology, 4(3), 475-487.
3. European Patent Office. (1984). Patent family analysis on beta blockers.
4. U.S. Food and Drug Administration. (1982). Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book).

Drugs Protected by US Patent 4,262,003

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate