Vaginal Delivery System Using High Internal Phase Emulsion

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Solution Overview

Problem

Current pharmaceutical delivery systems for the vaginal cavity fail to provide controlled release of active agents for extended periods, often leading to inadequate bioadherence and stability issues due to high systemic absorption and physical instability, particularly with high propylene glycol concentrations.

Innovation Solution

A delivery system with a high internal to external phase ratio of 70% or greater, utilizing an emulsion formulation with reduced propylene glycol content and an applicator design for controlled release of imidazole derivatives, ensuring prolonged bioadherence and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional delivery systems with high propylene glycol content are used, then drug availability and penetration potential are improved, but systemic absorption increases and physical stability deteriorates

Engineering Contradiction:
Improvedrug availabilityVSAvoidphysical stability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent changes the concentration parameter of propylene glycol from conventional high levels (50-80%) to a reduced level (10-40%), and adjusts the water content accordingly (60-90%). This parameter change resolves the contradiction by reducing systemic absorption and improving physical stability while maintaining adequate drug availability through the optimized emulsion formulation.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If conventional delivery systems are used, then immediate solubilization occurs enhancing drug availability, but bioadherence becomes minimal and controlled release for extended periods cannot be achieved

Engineering Contradiction:
Improvedrug availabilityVSAvoidcontrolled release duration
Core Design Contradiction:
Quantity of substanceVSDuration of action of moving object

Solution Approach 1:

The patent employs a composite emulsion system combining hydrophilic propylene glycol with hydrophobic oils (mineral oil, vegetable oils, or animal fats) in a specific ratio. This composite structure creates a controlled release matrix that maintains drug availability while enabling sustained release for 3-6 hours, resolving the contradiction between immediate availability and extended controlled release.

Inventive Principle:
Principle #40Composite materials

3Speed

If high concentrations of solubilizing compounds are used, then drug penetration potential increases, but treatment duration must be prolonged due to systemic absorption

Engineering Contradiction:
Improvepenetration rateVSAvoidtreatment duration
Core Design Contradiction:
SpeedVSDuration of action of moving object

Solution Approach 1:

The patent optimizes the propylene glycol concentration parameter to a reduced level (10-40% range) rather than conventional high levels, which maintains adequate drug penetration and availability while significantly reducing systemic absorption. This parameter optimization allows treatment to be completed within 3-6 hours rather than requiring prolonged treatment regimes.

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 system achieves controlled release of active agents for at least three hours, maintaining stability and bioadherence, reducing systemic absorption, and extending shelf life, while effectively treating vaginal infections with improved diffusion rates and physical stability.

Implementation Method 1

the delivery system is an emulsion that exhibits an internal to external phase ratio of greater than 70%... allow the active agent to be released in a controlled manner

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 2

The advantage being taken of both the potential solubilization of the active pharmaceutical compound in a solvent like molecule such as propylene glycol and the increased penetration potential afforded by propylene glycol through biological membranes

Methodology Applied
Scientific EffectSolubilization: Solvation

Data Source

PatentUS8057433B2Delivery system
Publication Date: 2011.11.15 PADAGIS US LLC
  • US8057433B2 patent drawing
  • US8057433B2 patent drawing
  • US8057433B2 patent drawing

AI summary

A pharmaceutical delivery system that releases an active agent in a controlled manner for an extended period in the vaginal cavity to treat or cure ailments associated with the vaginal cavity or proximal areas. The delivery system includes an applicator which is composed of a high internal phase emulsion, allowing the delivery system to adhere to the mueosal surfaces of the body, primarily the lining of vaginal cavity. The delivery system can maintain the high internal phase emulsion at a temperature of 86° F. for at least one month, without decomposition or instability of the emulsion.