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

VSEngineering 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

Engineering Contradiction:
Improveduration of actionVSAvoidpatient compliance
Core Design Contradiction:
Duration of action of stationary objectVSEase of operation

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.

Inventive Principle:
Principle #10Preliminary action

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.

Inventive Principle:
Principle #25Self-service

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

Engineering Contradiction:
Improveduration of actionVSAvoidrelease kinetics
Core Design Contradiction:
Duration of action of stationary objectVSManufacturing precision

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.

Inventive Principle:
Principle #35Parameter changes

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.

Inventive Principle:
Principle #40Composite materials

3Reliability

If potent drugs with poorer solubility are developed, then the therapeutic effect is enhanced, but the ease of delivery is reduced

Engineering Contradiction:
Improvetherapeutic effectVSAvoidease of delivery
Core Design Contradiction:
ReliabilityVSEase of manufacture

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.

Inventive Principle:
Principle #24Intermediary (Mediator)

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.

Inventive Principle:
Principle #35Parameter changes

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

Methodology Applied
Scientific EffectSurface tension reduction: Surfactant

Implementation Method 2

a liquid injectable composition that includes: (b) at least one gel strength enhancer

Methodology Applied
Scientific EffectGel formation: Gel

Data Source

PatentUS12409153B2Liquid injectable composition
Publication Date: 2025.09.09 AMATERASU LIFESCI LLP
  • US12409153B2 patent drawing
  • US12409153B2 patent drawing
  • US12409153B2 patent drawing

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.