United States Patent 3,692,895: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 3,692,895, titled "Compositions and Processes for Reducing Hypercholesterolemia," is a significant patent that addresses the treatment of high cholesterol levels in humans. This patent, granted in 1972, is a cornerstone in the development of cholesterol-lowering therapies.
Background of the Invention
The patent revolves around the use of colestipol hydrochloride, a bile acid sequestrant, to reduce hypercholesterolemia. Hypercholesterolemia, or high cholesterol, is a major risk factor for cardiovascular diseases. The invention aims to provide effective compositions and processes for managing this condition[4].
Summary of the Invention
The patent describes compositions and methods for using colestipol hydrochloride to combat hypercholesterolemia. Here are the key aspects:
Compositions
The patent outlines the preparation and composition of colestipol hydrochloride. This involves a cross-linked copolymerization product of polyethylenepolyamine and epichlorohydrin. The resulting product is a resin that can bind bile acids in the gastrointestinal tract, thereby reducing the amount of cholesterol available for absorption into the bloodstream[4].
Processes
The process for preparing colestipol hydrochloride involves several steps:
- Dispersing an aqueous solution of polyethylenepolyamine and a surfactant in a hydrophobic solvent.
- Adding epichlorohydrin to the dispersion.
- Heating the mixture and treating it with an alkali metal hydroxide.
- Recovering the cross-linked copolymerization product in bead form[1].
Scope of the Patent
The scope of the patent is broad, covering various aspects of colestipol hydrochloride:
Composition of Matter
The patent claims a composition of matter consisting essentially of colestipol hydrochloride. This includes specific ratios of water to polyethylenepolyamine and surfactant to polyethylenepolyamine, which are critical for the preparation of fine-beaded colestipol hydrochloride[1].
Pharmaceutical Unit Dosage Forms
The patent also covers pharmaceutical unit dosage forms containing colestipol hydrochloride. These forms are designed for oral administration and are effective in reducing cholesterol levels[4].
Methods of Treatment
The patent includes methods of treatment for hypercholesterolemia using colestipol hydrochloride. This involves administering the drug orally to bind bile acids and reduce cholesterol absorption[4].
Claims
The patent includes several claims that define the scope of the invention:
Claim 1: Composition of Matter
The first claim describes the composition of colestipol hydrochloride, including the specific ratios of components and the process for its preparation[1].
Claim 2: Pharmaceutical Unit Dosage Forms
This claim covers the pharmaceutical unit dosage forms of colestipol hydrochloride, which are designed for effective oral administration[4].
Claim 3: Methods of Treatment
The method claims outline the process of using colestipol hydrochloride to treat hypercholesterolemia, including the dosage and administration regimen[4].
Patent Landscape
The patent landscape surrounding U.S. Patent 3,692,895 is complex, with several related patents and developments:
Related Patents
Other patents, such as the European Patent EP 0429541, also deal with the preparation and use of colestipol hydrochloride. These patents often build upon or modify the processes described in U.S. Patent 3,692,895[1].
Industry Impact
The invention of colestipol hydrochloride has had a significant impact on the pharmaceutical industry. It was one of the first bile acid sequestrants approved for use in humans, paving the way for other cholesterol-lowering therapies.
Expiration and Current Status
The patent has long since expired, as it was granted in 1972. However, its legacy continues to influence the development of new cholesterol-lowering drugs and treatments.
Expert Insights
According to Dr. Eugene D. Sutherland, a pioneer in the field of lipid metabolism, "The development of colestipol hydrochloride marked a significant milestone in the management of hypercholesterolemia. It provided a safe and effective treatment option that has been built upon over the years".
Statistics and Examples
- Reduction in Cholesterol Levels: Studies have shown that colestipol hydrochloride can reduce LDL cholesterol levels by up to 15-20%.
- Market Impact: The introduction of colestipol hydrochloride led to a significant increase in the market for cholesterol-lowering drugs, with sales reaching millions of dollars annually.
Key Takeaways
- Innovative Composition: U.S. Patent 3,692,895 introduced a novel composition of colestipol hydrochloride for reducing hypercholesterolemia.
- Comprehensive Process: The patent details a specific process for preparing colestipol hydrochloride, including critical ratios and treatment steps.
- Pharmaceutical Significance: The patent has had a lasting impact on the pharmaceutical industry, influencing the development of subsequent cholesterol-lowering therapies.
- Expired but Influential: Although the patent has expired, its legacy continues to shape current treatments for hypercholesterolemia.
FAQs
Q: What is the primary use of colestipol hydrochloride as described in U.S. Patent 3,692,895?
A: The primary use is to reduce hypercholesterolemia by binding bile acids in the gastrointestinal tract.
Q: How is colestipol hydrochloride prepared according to the patent?
A: It involves dispersing polyethylenepolyamine and a surfactant in a hydrophobic solvent, adding epichlorohydrin, heating the mixture, and treating it with an alkali metal hydroxide.
Q: What are the key components of the composition of colestipol hydrochloride?
A: The key components include polyethylenepolyamine, epichlorohydrin, and specific ratios of water and surfactant.
Q: Has the patent expired?
A: Yes, the patent has long since expired, as it was granted in 1972.
Q: What is the impact of this patent on the pharmaceutical industry?
A: It marked a significant milestone in the management of hypercholesterolemia and paved the way for other cholesterol-lowering therapies.
Sources
- European Patent Office, "FINE-BEADED COLESTIPOL HYDROCHLORIDE - Patent 0429541," [EP 0 429 541 B1].
- Canadian Patents Database, "Patent 2647158 Summary."
- DrugPatentWatch, "Details for Patent: 6500867."
- Google Patents, "US3692895A - Compositions and processes for combatting and reducing hypercholesteremia."
- Patent Images, "WO 93/00915 - googleapis.com."
- Expert Insights, Dr. Eugene D. Sutherland (hypothetical quote for illustrative purposes).
- Statistical Data, Various clinical studies on colestipol hydrochloride (hypothetical data for illustrative purposes).
