Liquid Injectable Composition with Gel-Based Controlled 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 frequent injections for sustained systemic levels, and there is a need for improved controlled release compositions to maintain therapeutic concentrations with minimal systemic exposure and patient compliance issues.
Innovation Solution
A liquid injectable composition comprising surfactants, gel strength enhancers, solvents, optional release retarding agents, stabilizing agents, and active pharmaceutical ingredients, designed to provide initial rapid release followed by sustained delivery, suitable for single or multiple dose therapies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If repeated injections are administered to maintain therapeutic levels, then the duration of action is extended, but patient compliance becomes difficult and systemic exposure increases
Solution Approach 1:
The patent formulates the active agent in a controlled release composition that is prepared in advance to automatically release the drug over an extended period. This preliminary action eliminates the need for repeated patient injections, as the single administered composition provides sustained therapeutic levels through its built-in controlled release mechanism.
Solution Approach 2:
The controlled release composition is designed to self-regulate drug release without requiring repeated patient intervention. The composition automatically maintains therapeutic levels through its controlled release properties, making the treatment system self-sufficient and eliminating the compliance burden of repeated injections.
2Duration of action of stationary object
If synthetic degradable polymers are used for controlled release, then the duration of action is extended, but the release kinetics may not match the desired profile
Solution Approach 1:
The patent modifies the polymer composition by incorporating natural biodegradable polymers (such as chitosan, alginate, or gelatin) alongside or instead of synthetic polymers. This parameter change in the material composition allows for tailored release kinetics that better match desired therapeutic profiles while maintaining extended duration of action.
Solution Approach 2:
The controlled release composition uses composite materials combining natural and/or synthetic biodegradable polymers. This composite approach enables fine-tuning of release kinetics by selecting and combining polymers with complementary degradation rates and release characteristics, achieving both extended duration and precise kinetic control.
3Reliability
If potent drugs with poorer solubility are developed, then the therapeutic effect is enhanced, but the ease of delivery is reduced
Solution Approach 1:
The patent uses solubility-enhancing excipients and surfactants as intermediaries to facilitate the delivery of potent but poorly soluble drugs. These auxiliary substances act as mediators that improve the solubility and dispersibility of the active agent in the injection medium, enabling effective delivery without compromising therapeutic potency.
Solution Approach 2:
The patent employs parameter changes in the formulation, including adjusting pH, using co-solvents, or modifying the physical state of the active agent (e.g., using amorphous forms or salt forms). These parameter modifications enhance solubility and deliverability while preserving the potent therapeutic effect of the active agent.
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 achieves controlled release of active agents, reducing the frequency of injections and maintaining therapeutic levels, with enhanced patient compliance and minimal systemic exposure, applicable for a wide range of diseases and disorders.
Implementation Method 1
a liquid injectable composition that includes: (a) at least one surfactant
Implementation Method 2
a liquid injectable composition that includes: (b) at least one gel strength enhancer
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.


