Buccal Delivery Matrix for Hormone Bioavailability
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current buccal delivery systems, such as troches, face challenges with bioavailability, side effects, and manufacturing complexity, particularly for hormones like progesterone and testosterone, which exhibit poor oral bioavailability and cause gastrointestinal irritation, leading to non-compliance issues and fluctuating hormone levels.
Innovation Solution
A buccal delivery system using a dry manufacturing process with a matrix comprising active ingredients, polyethylene glycols, suspending agents, flowing agents, and sweeteners, allowing for improved bioavailability and reduced gastrointestinal side effects, while being easier and more economical to produce, using a standard tabletting machine.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional troche formulations are used for buccal delivery, then the active ingredients can be delivered to the bloodstream, but the bioavailability is limited and gastrointestinal side effects occur due to swallowing
Solution Approach 1:
The patent modifies the physical and chemical parameters of the delivery system by using a dry powder compressed into a rigid tablet rather than a wet troche formulation. This parameter change in the delivery system's physical state prevents dissolution in saliva and subsequent swallowing, thereby eliminating gastrointestinal side effects while maintaining buccal absorption through direct contact with the buccal mucosa
Solution Approach 2:
The invention extracts the harmful pathway of drug delivery by preventing the drug from entering the gastrointestinal tract. By designing a dry compressed tablet that dissolves only in the buccal cavity and not in saliva, the patent removes the route that leads to gastrointestinal irritation and first-pass metabolism, isolating the therapeutic benefit from the harmful effects
2Ease of manufacture
If complex wet manufacturing processes are used for troches, then the formulation can be produced, but the manufacturing complexity and cost increase
Solution Approach 1:
The patent replaces the complex mechanical and thermal processing system used for traditional troche manufacturing with a simple compression mechanism. Instead of requiring melting, mixing, and molding equipment, the invention uses a dry powder compression process similar to standard tablet manufacturing, significantly simplifying the mechanical system required while maintaining production capability
Solution Approach 2:
The invention changes the manufacturing parameters from wet processing (melting, mixing, molding) to dry processing (compression). This parameter change in the manufacturing approach transforms a complex multi-step process into a simpler single-step compression process, reducing both equipment complexity and manufacturing difficulty
3Reliability
If frequent dosing is required to maintain hormone levels, then therapeutic effect is maintained, but patient compliance decreases
Solution Approach 1:
The patent enables continuous therapeutic action by providing sustained release of the active ingredient from the compressed tablet formulation. The dry compressed matrix allows for gradual dissolution and absorption over an extended period, maintaining stable hormone levels without requiring frequent re-dosing, thus improving patient compliance while preserving therapeutic efficacy
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 system achieves up to 85% bioavailability of active ingredients, reduces gastrointestinal side effects, and allows for less frequent dosing with more stable hormone levels, improving patient compliance and manufacturing efficiency.
Implementation Method 1
The buccal delivery system of the present invention is able to deliver up to and sometimes more than 85% of the active ingredient as it circumvents the action of the liver in 'first past metabolism'
Implementation Method 2
an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix
Data Source
AI summary
A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.