SNAC Salt PYY Composition Oral Bioavailability
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Solution Overview
Problem
Current pharmaceutical compositions for Peptide tyrosine tyrosine (PYY) compounds, particularly PYY(3-36), face challenges due to rapid degradation in the gastrointestinal system, leading to suboptimal pharmacokinetic properties and requiring frequent administration, and have low oral bioavailability, necessitating the development of optimized compositions for effective oral administration.
Innovation Solution
A pharmaceutical composition comprising a high content of the absorption enhancer sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC) with a minimal content of further excipients, which accelerates the dissolution and absorption of PYY compounds, enabling faster and more efficient uptake of the active pharmaceutical ingredient.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If PYY compounds are administered orally, then convenience of administration is improved, but oral bioavailability is low due to rapid degradation in the gastrointestinal system
Solution Approach 1:
The patent employs SNAC (sodium N-(8-(2-hydroxybenzoyl)amino)caprylate) as an intermediary substance to facilitate the absorption of PYY compounds across the gastrointestinal barrier. SNAC acts as a delivery agent that protects the peptide from degradation and enhances its transport through the gut wall, thereby improving oral bioavailability while maintaining the convenience of oral administration.
Solution Approach 2:
The patent modifies the formulation parameters by incorporating specific excipients and delivery agents that change the physical and chemical environment of the PYY compound in the gastrointestinal tract. This includes using SNAC to alter absorption kinetics and protecting the peptide from enzymatic degradation, thereby improving reliability of oral delivery without compromising ease of administration.
2Device complexity
If PYY compounds are administered without optimization, then formulation complexity is reduced, but pharmacokinetic properties are suboptimal requiring frequent administration
Solution Approach 1:
SNAC serves as a mediator that extends the duration of action of PYY compounds by protecting them from rapid clearance and degradation. This delivery agent enables sustained therapeutic effects, reducing the frequency of administration needed while maintaining a manageable formulation complexity.
Solution Approach 2:
The patent creates a composite pharmaceutical formulation combining PYY compounds with SNAC and other excipients. This composite material leverages the synergistic effects of its components to achieve improved pharmacokinetic properties, including extended duration of action and reduced clearance rate, without excessive formulation complexity.
3Speed
If high content of absorption enhancer SNAC is used, then dissolution and absorption of PYY is accelerated, but content of other excipients must be minimized
Solution Approach 1:
The patent extracts or removes unnecessary excipients from the formulation to make room for high concentrations of SNAC. By eliminating redundant components, the formulation achieves accelerated dissolution and absorption of PYY compounds through maximized SNAC content, thereby improving speed of drug release and uptake.
Solution Approach 2:
The patent optimizes the concentration parameters of formulation components by increasing SNAC content to high levels while minimizing other excipients. This parameter change strategy enhances the dissolution and absorption rate of PYY compounds, achieving faster therapeutic onset while maintaining a streamlined formulation composition.
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 composition provides improved exposure and bioavailability of PYY compounds, allowing for increased and sustained therapeutic effects, potentially enhancing treatment outcomes for obesity and diabetes by facilitating more effective oral administration.
Implementation Method 1
a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, wherein said salt constitutes at least 60 percent (w/w) of the composition
Implementation Method 2
Human PYY and analogues thereof have a low oral bioavailability. Human PYY and analogues thereof can only be detected in plasma after oral administration if formulated with certain absorption enhancers in a specific amount.
Data Source
Figure 1/1
AI summary
The present invention relates to a solid composition comprising a PYY compound and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and their use in medicine.