Injectable Depot Composition for Controlled Drug Release
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Solution Overview
Problem
Existing biologically active agents face challenges in effective delivery through oral, transmucosal, or transdermal routes due to degradation or insufficient absorption, necessitating repeated injections for sustained effect, and there is a need for controlled release compositions that maintain therapeutic concentrations over time with minimal systemic exposure.
Innovation Solution
A liquid injectable composition comprising surfactants, gel strength enhancers, solvents, optional release retarding agents, stabilizing agents, and active pharmaceutical ingredients, which forms a depot in situ to provide initial rapid release followed by sustained delivery, allowing single or multiple dose therapy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If repeated injections are administered to maintain therapeutic effect, then the duration of action is extended, but patient compliance becomes difficult to ensure and systemic exposure increases
Solution Approach 1:
The patent applies preliminary action by formulating the drug in a controlled-release composition that pre-establishes a sustained release mechanism. The composition is designed to release the active agent over an extended period following a single injection, eliminating the need for repeated dosing and ensuring reliable therapeutic effect without depending on patient compliance.
Solution Approach 2:
The patent changes the release rate parameter of the active agent by incorporating it into a controlled-release matrix. This parameter change transforms the delivery profile from immediate-release requiring frequent dosing to sustained-release providing extended therapeutic effect, thereby resolving the contradiction between duration of action and patient compliance.
2Reliability
If controlled release compositions are used to reduce injection frequency, then patient compliance improves, but the release kinetics may not provide desired therapeutic profile
Solution Approach 1:
The patent optimizes the release kinetics by adjusting formulation parameters including the type and amount of polymer matrix, solvent composition, and drug-to-polymer ratio. These parameter changes enable control over the release rate to achieve the desired therapeutic profile while maintaining improved patient compliance through reduced injection frequency.
Solution Approach 2:
The patent employs composite materials by combining the active agent with specific polymers and solvents to create a controlled-release composition. This composite structure allows tuning of the release kinetics through selection of appropriate material combinations, achieving both improved compliance and desired therapeutic profile.
3Reliability
If potent drugs with poorer solubility are developed, then therapeutic efficacy is enhanced, but delivery effectiveness and efficiency decrease
Solution Approach 1:
The patent uses solvents and surfactants as intermediaries to enhance the solubility and delivery efficiency of potent drugs with poor aqueous solubility. These auxiliary substances facilitate the dissolution and dispersion of the active agent in the formulation, enabling effective delivery while maintaining high therapeutic efficacy.
Solution Approach 2:
The patent creates composite formulations by combining the potent drug with solubilizing agents, surfactants, and controlled-release matrices. This composite approach simultaneously addresses the solubility limitation and enables efficient delivery, resolving the contradiction between therapeutic efficacy and delivery efficiency.
4Duration of action of moving object
If synthetic degradable polymers are used for sustained release, then the duration of action is extended, but drug release becomes reliant on polymer breakdown rate which may not provide desired kinetic profile
Solution Approach 1:
The patent changes the release mechanism by incorporating solvents and adjusting formulation parameters to control drug release independently of polymer degradation rate. This allows achievement of desired release kinetics while maintaining extended duration of action through the controlled-release matrix.
Solution Approach 2:
The patent introduces solvents and other formulation components as intermediaries that facilitate drug release from the polymer matrix. These intermediaries enable control over release kinetics by modifying the diffusion and partitioning behavior of the active agent, decoupling release rate from polymer degradation rate.
Data Source
AI summary
A liquid injectable composition comprising (a) at least one surfactant; (b) at least one gel strength enhancer; (c) at least one solvent; (d) optionally release retarding agent(s); (e) optionally stabilizing agent(s); (f) optionally pharmaceutical excipient(s); and (g) active pharmaceutical ingredient(s) (API) and its use in treating a subject suffering from a disease or disorder.