United States Patent 5,198,226: A Detailed Analysis
Introduction
United States Patent 5,198,226, titled "Pharmaceutical Dosage Form," is a significant patent in the field of pharmaceuticals, particularly focusing on the formulation and delivery of dihydropyridine calcium channel blockers. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background
Calcium channel blockers are a class of medications used to treat hypertension and other cardiovascular conditions. Dihydropyridines are a subset of these blockers, known for their efficacy in relaxing vascular smooth muscle and reducing blood pressure. The patent in question addresses the formulation of these compounds into a pharmaceutical dosage form.
Inventors and Assignees
The patent was granted to inventors who developed a novel formulation for dihydropyridine calcium channel blockers. The assignee of the patent is typically a pharmaceutical company or research institution that funded the development of this technology.
Claims
The patent includes several claims that define the scope of the invention:
Claim 1: Pharmaceutical Dosage Form
The first claim describes a pharmaceutical dosage form comprising spheroids containing a dihydropyridine calcium channel blocker. These spheroids are designed to provide a controlled release of the active ingredient.
Claim 2: Composition of Spheroids
This claim specifies the composition of the spheroids, including the dihydropyridine compound, a binder, and optionally other excipients to enhance the formulation's stability and release profile.
Claim 3: Method of Preparation
The method of preparing these spheroids is outlined, involving the steps of mixing the active ingredient with a binder, forming the mixture into spheroids, and optionally applying a coating to control the release rate.
Description of the Invention
The patent provides a detailed description of the invention, including the materials used, the process of manufacturing, and the characteristics of the final product.
Materials
The dihydropyridine calcium channel blockers are the primary active ingredients. The binder and other excipients are chosen to ensure the stability and controlled release of the spheroids.
Manufacturing Process
The process involves mixing the active ingredient with a binder, followed by the formation of spheroids. This can be achieved through various techniques such as extrusion, spheronization, or other granulation methods.
Characteristics of the Spheroids
The spheroids are designed to have specific physical and pharmacokinetic properties. They must have a uniform size and shape to ensure consistent drug release. The coating applied to the spheroids can be tailored to achieve the desired release profile.
Advantages of the Invention
The invention offers several advantages over existing formulations:
Controlled Release
The spheroids provide a controlled release of the dihydropyridine compound, which can improve patient compliance by reducing the frequency of dosing.
Stability
The formulation enhances the stability of the active ingredient, protecting it from degradation and ensuring a consistent therapeutic effect.
Bioavailability
The design of the spheroids can improve the bioavailability of the dihydropyridine compound, ensuring that more of the drug is absorbed by the body.
Patent Landscape
The patent landscape surrounding United States Patent 5,198,226 includes other patents related to pharmaceutical dosage forms and controlled release formulations.
Related Patents
Other patents, such as U.S. Patent 4,940,556, also disclose spheroids containing dihydropyridine calcium channel blockers but may differ in their specific formulations or manufacturing processes[5].
Competing Technologies
Competing technologies include other types of controlled release formulations, such as tablets or capsules, which may offer different advantages and disadvantages compared to the spheroid formulation.
Impact on the Pharmaceutical Industry
This patent has had a significant impact on the pharmaceutical industry by providing a novel and effective way to deliver dihydropyridine calcium channel blockers.
Clinical Use
The controlled release formulation has improved the management of hypertension and other cardiovascular conditions by providing a more consistent and reliable therapeutic effect.
Economic Impact
The patent has also had economic implications, as it has allowed pharmaceutical companies to develop and market new products that offer improved patient outcomes and compliance.
Challenges and Limitations
While the patent offers several advantages, there are also challenges and limitations associated with its implementation.
Manufacturing Complexity
The process of manufacturing spheroids can be complex and may require specialized equipment and expertise.
Regulatory Approval
Obtaining regulatory approval for new pharmaceutical formulations can be a lengthy and costly process.
Future Developments
The field of pharmaceutical dosage forms is continuously evolving, with new technologies and formulations being developed.
Advanced Materials
New materials and excipients are being researched to further enhance the stability and release profile of pharmaceutical formulations.
Personalized Medicine
There is a growing trend towards personalized medicine, where formulations are tailored to individual patient needs.
Key Takeaways
- Controlled Release: The patent provides a controlled release formulation of dihydropyridine calcium channel blockers.
- Spheroid Formulation: The use of spheroids ensures uniform size and shape, leading to consistent drug release.
- Stability and Bioavailability: The formulation enhances the stability and bioavailability of the active ingredient.
- Impact on Industry: The patent has significantly impacted the pharmaceutical industry by offering improved patient outcomes and compliance.
- Future Developments: The field is evolving with new materials, technologies, and personalized medicine approaches.
FAQs
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What is the primary active ingredient in the pharmaceutical dosage form described in U.S. Patent 5,198,226?
- The primary active ingredient is a dihydropyridine calcium channel blocker.
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What is the advantage of using spheroids in this formulation?
- Spheroids provide a controlled release of the active ingredient, ensuring consistent drug delivery.
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How are the spheroids manufactured?
- The spheroids are manufactured through a process involving mixing the active ingredient with a binder, followed by formation into spheroids, and optionally applying a coating.
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What are the key characteristics of the spheroids?
- The spheroids must have a uniform size and shape, and the coating can be tailored to achieve the desired release profile.
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How has this patent impacted the pharmaceutical industry?
- The patent has improved the management of hypertension and other cardiovascular conditions by providing a more consistent and reliable therapeutic effect.
Citations
[5] https://patents.justia.com/patent/20130251759
This analysis provides a comprehensive overview of United States Patent 5,198,226, highlighting its significance in the pharmaceutical industry and its contributions to the field of controlled release formulations.
