12-Hour Matrix Tablet for Sustained Release of Tri-Oxy Agents
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Solution Overview
Problem
Current oral dosage forms for treating cough and cold symptoms often require frequent dosing due to short-acting combinations of active agents, leading to disrupted sleep and increased daytime grogginess, and there is a lack of effective combination matrix tablets that can release tri-oxy active agents optimally for twice-a-day dosing therapy.
Innovation Solution
A matrix tablet formulation containing a tri-oxy active agent and a second active agent, with a non-ionic oxyl-containing hydrophilic polymer, designed for 12-hour dosing, which maintains optimal blood levels and avoids food effects, using a specific oxyl content composition to control release rates and ensure consistent symptom relief.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If immediate release dosage forms are used, then symptom relief is achieved quickly, but frequent dosing is required which disrupts sleep and causes daytime grogginess
Solution Approach 1:
The patent changes the release rate parameter of the active agents by incorporating them into a hydrophilic polymer matrix, transforming the immediate release characteristic into sustained release. This allows the drug to be delivered at a controlled rate over 12 hours, maintaining therapeutic effect while enabling less frequent dosing.
Solution Approach 2:
The patent uses a composite material system consisting of active agents embedded in a hydrophilic polymer matrix. This composite structure enables sustained release by controlling the diffusion and erosion of the polymer, thereby extending the duration of action while maintaining adequate symptom relief speed.
2Reliability
If frequent dosing is required, then consistent symptom relief can be maintained, but patient compliance decreases and sleep is disrupted
Solution Approach 1:
The sustained release matrix tablet provides continuous delivery of active agents over a 12-hour period, eliminating the gaps between doses that occur with immediate release formulations. This continuous action maintains consistent symptom relief while requiring dosing only twice daily, significantly improving patient convenience and compliance.
3Adaptability or versatility
If combination products are formulated, then multiple symptoms can be treated simultaneously, but each active agent's unique pharmacokinetic requirements become difficult to meet
Solution Approach 1:
The patent applies local quality by creating distinct microenvironments within the matrix tablet for different active agents. Each agent can be associated with polymer regions having specific properties (such as different erosion rates or diffusion characteristics) that are tailored to meet its unique pharmacokinetic requirements, while still achieving sustained release overall.
4Duration of action of moving object
If sustained release formulations are developed, then dosing frequency can be reduced, but achieving optimal blood levels becomes challenging
Solution Approach 1:
The patent incorporates feedback mechanisms through the polymer matrix erosion and drug diffusion processes. The release rate automatically adjusts based on the remaining drug concentration and polymer degradation state, helping to maintain blood levels within the therapeutic window without requiring complex external control systems.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The 12-hour matrix tablet provides sustained release of active agents, maintaining 70-135% of peak plasma concentrations compared to immediate release dosing, with no significant food effect, allowing for uninterrupted sleep and reduced daytime grogginess while meeting regulatory requirements for blood level stability.
Implementation Method 1
A matrix tablet formulation containing a tri-oxy active agent and a second active agent, with a non-ionic oxyl-containing hydrophilic polymer, designed for 12-hour dosing
Implementation Method 2
using a specific oxyl content composition to control release rates and ensure consistent symptom relief
Implementation Method 3
The 12-hour matrix tablet provides sustained release of active agents, maintaining 70-135% of peak plasma concentrations compared to immediate release dosing
Data Source
AI summary
A pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The tablet is a matrix tablet and a single-dose administration of one or more tablets to a subject under fasted conditions provides a mean Cm˜ for each of the first active agent and the second active agent that is 70% to 135% of a respective mean Cm˜ provided by administering an immediate release oral dosage form to a subject under fasted conditions every 4 to 6 hours over a 12 hour time period, wherein cumulative dosage amounts administered over the 12 hour time period of each active agent is equivalent to the respective amount of each active agent in the pharmaceutical tablet.