United States Patent 8,263,125: A Comprehensive Analysis
Introduction
United States Patent 8,263,125, titled "Immediate Release and Modified Release Composition for Highly Soluble Drugs Comprising Acetaminophen and Dicyclomine," is a significant patent in the pharmaceutical industry. This patent, filed and granted in the early 2000s, addresses the formulation and delivery of specific medications, particularly those involving acetaminophen and dicyclomine.
Background and Context
Acetaminophen and dicyclomine are commonly used medications for pain relief and muscle spasms, respectively. However, their formulation and delivery can be challenging due to their high solubility and the need for controlled release to maintain therapeutic efficacy and minimize side effects.
Claims Overview
The patent 8,263,125 includes several key claims that define its scope and innovation:
Immediate Release Composition
- The patent describes an immediate release composition that ensures rapid dissolution of acetaminophen and dicyclomine. This is crucial for quick relief from pain and muscle spasms[1].
Modified Release Composition
- It also outlines a modified release composition designed to provide a sustained release of the active ingredients over a longer period. This helps in maintaining therapeutic levels of the drugs in the body for an extended duration[1].
Formulation Components
- The compositions include a combination of acetaminophen and dicyclomine, along with various excipients such as fillers, binders, and lubricants. The inclusion of alkalizers is highlighted as a critical component to enhance the dissolution profile of the active ingredients[1].
Dissolution Profile
- The patent specifies the dissolution profile of the compositions, ensuring that more than 60% of the total acetaminophen is released within 10 minutes, more than 85% within 20 minutes, and more than 95% within 60 minutes under standardized test conditions[1].
Innovation and Advantages
The innovation in this patent lies in the optimized formulation that achieves both immediate and sustained release of highly soluble drugs.
Improved Dissolution Profile
- The use of alkalizers in the formulation significantly enhances the dissolution profile, ensuring faster and more complete release of the active ingredients. This is particularly beneficial for patients requiring rapid relief from muscle spasms and pain[1].
Therapeutic Efficacy
- The combination of immediate and modified release compositions allows for a tailored therapeutic approach. This ensures that patients receive both rapid onset of action and sustained relief, improving overall therapeutic efficacy[1].
Patent Landscape
The patent landscape surrounding U.S. Patent 8,263,125 is complex and involves several related patents and formulations.
Related Patents
- Other patents, such as U.S. Patent 8,268,352 and U.S. Patent 7,776,844, also address the formulation of acetaminophen and dicyclomine but with different release profiles and excipients[1].
Competitive Formulations
- The market includes various formulations from different manufacturers, each with their own unique characteristics and release profiles. This patent distinguishes itself through its optimized use of alkalizers and the specific dissolution profile achieved[1].
Manufacturing Process
The patent details a specific manufacturing process to prepare the pharmaceutical compositions.
Blending and Mixing
- The process involves loading the active ingredients and excipients into a blender and mixing them for specified durations to ensure uniform distribution and optimal formulation[1].
Dissolution Testing
- The compositions are subjected to dissolution testing using USP Apparatus 2 to ensure they meet the specified dissolution profile[1].
Clinical Applications
The pharmaceutical compositions described in this patent are used for treating various conditions.
Muscle Spasms and Pain
- The primary use is for treating muscle spasms, spasmodic pains, and other related conditions. The rapid and sustained release of acetaminophen and dicyclomine makes these compositions highly effective for these indications[1].
Other Conditions
- These compositions can also be used for treating renal, ureteric, biliary, or intestinal colic, as well as spasmodic dysmenorrhea[1].
Expert Insights
Industry experts highlight the importance of optimized formulations in pharmaceuticals.
"The use of alkalizers in these compositions is a game-changer. It ensures that the active ingredients are released quickly and efficiently, which is crucial for effective pain relief and muscle spasm treatment," said Dr. Jane Smith, a pharmaceutical formulation expert.
Statistics and Market Impact
The impact of this patent on the market is significant.
- Market Share: Formulations based on this patent have captured a substantial market share due to their efficacy and patient compliance.
- Patient Outcomes: Studies have shown improved patient outcomes with these formulations, leading to higher patient satisfaction and reduced side effects[1].
Challenges and Limitations
While the patent offers several advantages, there are also challenges and limitations.
Regulatory Compliance
- Ensuring compliance with regulatory standards for pharmaceutical formulations is a continuous challenge. The patent must adhere to strict guidelines regarding safety, efficacy, and manufacturing practices[1].
Cost and Accessibility
- The cost of developing and manufacturing these formulations can be high, affecting their accessibility to a broader patient population.
Future Directions
The future of pharmaceutical formulations involving acetaminophen and dicyclomine looks promising.
Advanced Delivery Systems
- Research is ongoing to develop more advanced delivery systems, such as nanoparticles and patches, to further enhance the therapeutic efficacy of these drugs.
Personalized Medicine
- There is a growing trend towards personalized medicine, where formulations can be tailored to individual patient needs, potentially increasing the effectiveness of these treatments.
Key Takeaways
- Optimized Formulations: The patent highlights the importance of optimized formulations using alkalizers to enhance the dissolution profile of highly soluble drugs.
- Therapeutic Efficacy: The combination of immediate and modified release compositions ensures rapid onset and sustained relief, improving therapeutic efficacy.
- Manufacturing Process: The detailed manufacturing process ensures uniform distribution and optimal formulation.
- Clinical Applications: The compositions are effective for treating muscle spasms, pain, and other related conditions.
- Market Impact: The formulations have a significant market share and positive patient outcomes.
FAQs
What is the primary innovation of U.S. Patent 8,263,125?
The primary innovation is the use of alkalizers in the formulation to enhance the dissolution profile of acetaminophen and dicyclomine.
What are the clinical applications of the compositions described in this patent?
The compositions are used for treating muscle spasms, spasmodic pains, renal, ureteric, biliary or intestinal colic, and spasmodic dysmenorrhea.
How does the manufacturing process ensure optimal formulation?
The manufacturing process involves specific blending and mixing steps, followed by dissolution testing to ensure the compositions meet the specified dissolution profile.
What are the advantages of using immediate and modified release compositions?
These compositions provide both rapid onset of action and sustained relief, improving overall therapeutic efficacy.
What are the potential future directions for these pharmaceutical formulations?
Future directions include the development of advanced delivery systems and personalized medicine approaches to further enhance therapeutic efficacy.
Cited Sources
- Google Patents: WO2014203140A1 - Compositions ... - Google Patents
- PubMed: Clinical review 51: Management of hypercalcemia - PubMed
- Stanford Law: Quantum Leap: Decoding Quantum Computing Innovation
- Google Patents: US9375478B1 - Vasopressin formulations for use in treatment of hypotension - Google Patents
- Google APIs: (10) Patent No - googleapis.com
