Peptide Compositions for Controlled Release in Aqueous Injection Media
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Solution Overview
Problem
Traditional parenteral drug delivery systems fail to account for drug solubility in both solid and liquid phases of the injection medium, leading to uncontrolled release and instability of pharmaceutically active compounds.
Innovation Solution
The use of novel peptides comprising specific combinations of acidic, basic, and neutral amino acids, which are non-covalently bonded with the pharmaceutically active compounds, to create a controlled release mechanism through nano or micro structures that modulate drug absorption, release, and clearance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If traditional depot approaches are used to achieve controlled release, then the duration of action is extended, but the drug solubility and stability in aqueous medium are compromised
Solution Approach 1:
The patent introduces a water-soluble polymer as an intermediary substance that mediates between the hydrophobic drug and the aqueous injection medium. The polymer forms a soluble complex with the drug, enabling stable dissolution in water while maintaining controlled release properties. This intermediary resolves the contradiction by allowing the drug to be both stable in aqueous medium and released over an extended period.
Solution Approach 2:
The patent changes the physical-chemical parameters of the drug delivery system by using a water-soluble polymer to alter the solubility characteristics. The polymer modifies the drug's apparent solubility and stability parameters in aqueous medium without changing the drug's intrinsic properties, enabling controlled release while maintaining stability.
2Ease of manufacture
If drug is highly soluble in the matrix, then the ease of manufacture is improved, but the release control is compromised as drug leaves matrix too quickly
Solution Approach 1:
The water-soluble polymer acts as an intermediary that controls the drug release rate. By forming a soluble complex, the polymer enables the drug to remain associated with the delivery system long enough to achieve controlled release, preventing premature release while maintaining manufacturability through simple mixing.
3Productivity
If traditional matrix systems are used to reduce number of injections, then the productivity is improved, but the device complexity increases due to multiple components
Solution Approach 1:
The patent creates a composite material system consisting of the drug and water-soluble polymer. This composite approach enables controlled release functionality while maintaining relative simplicity in composition and manufacturing, balancing the need for reduced injection frequency with acceptable system complexity.
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 peptide compositions provide controlled and sustained release of active compounds, reducing the need for multiple injections and maintaining stability in aqueous environments.
Implementation Method 1
The peptide, comprising a unique combination of acidic, neutral and basic amino acids, is non-covalently bonded with or used in combination with the pharmaceutically active compound
Implementation Method 2
transport of a drug within the matrix or depot is crucial for drug release kinetics and is related to the diffusivity and the solubility of drug dissolved in a homogeneous medium
Implementation Method 3
The traditional depot approach though considered the solubility of pharmaceutically active drug in the matrix but did not take the solubility of the drug in an aqueous medium where it got injected
Data Source
AI summary
Provided are novel peptides, methods of their preparation and their use in controlled release of pharmaceutically active compounds.