Oligomeric Lactic Acid Vaginal Compositions for Bacterial Vaginosis

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Solution Overview

Problem

Current treatments for bacterial vaginosis require frequent administration and often lead to recurrence, with existing formulations having issues with stability and duration of action, necessitating daily or more frequent application and failing to maintain a stable acidic environment effectively.

Innovation Solution

Development of oligomeric lactic acid compositions with specific molecular weight ranges and polydispersity indices, combined with a mucoadhesive agent, to gradually release lactic acid and maintain a weak acidic environment for extended periods, allowing for less frequent administration and improved therapeutic efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments for bacterial vaginosis are used, then therapeutic effect is achieved, but frequent administration is required and recurrence occurs

Engineering Contradiction:
Improvetherapeutic effectVSAvoidduration of action
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The treatment approach is segmented into multiple dosage forms with different release characteristics. The patent uses oligomeric lactic acid with controlled molecular weight distribution to create sustained-release formulations that maintain therapeutic effect over extended periods, reducing administration frequency while preventing recurrence through prolonged acidic environment maintenance.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The formulation is designed to preliminarily establish a stable acidic environment before pathogenic bacteria can recolonize. By using oligomeric lactic acid that gradually releases lactic acid over time, the treatment creates a preemptive protective acidic barrier that prevents recurrence rather than merely treating acute symptoms.

Inventive Principle:
Principle #10Preliminary action

2Object-affected harmful factors

If existing formulations are used, then pH lowering effect is achieved, but stability and duration of action are insufficient

Engineering Contradiction:
ImprovepH lowering effectVSAvoidstability
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent systematically optimizes critical parameters including oligomer molecular weight distribution (number average molecular weight 200-500), polydispersity index (1.45-6.0), and lactic acid content (30-80%) to achieve the desired balance between stability and duration of action. These parameter changes enable controlled hydrolysis rates and sustained pH lowering effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The formulation combines oligomeric lactic acid with specific excipients and mucoadhesive agents to create a composite system. This composite structure provides both structural stability for maintained pH levels and controlled release characteristics for extended duration of action, overcoming the limitations of simple lactic acid formulations.

Inventive Principle:
Principle #40Composite materials

3Duration of action of moving object

If oligomeric lactic acid with broad molecular weight distribution is used, then prolonged duration of action is achieved, but manufacturing complexity increases

Engineering Contradiction:
Improveduration of actionVSAvoidmanufacturing complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent defines specific parameter ranges for oligomeric lactic acid (number average molecular weight 200-500, polydispersity index 1.45-6.0) that balance prolonged duration of action with manufacturability. These standardized parameter specifications simplify quality control and manufacturing processes while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The oligomeric lactic acid structure with controlled molecular weight distribution creates a pseudo-porous release matrix that facilitates controlled hydrolysis and lactic acid release. This structural approach enables prolonged duration of action through gradual degradation without requiring complex controlled-release mechanisms.

Inventive Principle:
Principle #31Porous materials

4Reliability

If frequent administration is required, then therapeutic effect is maintained, but user compliance and convenience decrease

Engineering Contradiction:
Improvetherapeutic effectVSAvoidease of administration
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The formulation provides continuous therapeutic action through sustained lactic acid release from oligomeric precursors. This continuous acidic environment maintenance eliminates the need for frequent re-administration, improving user compliance while ensuring reliable therapeutic effect through uninterrupted pH control.

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The oligomeric lactic acid formulation acts as a self-sustaining treatment system where the degraded oligomers continuously release lactic acid without requiring external replenishment. This self-service characteristic reduces administration frequency and improves convenience while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #25Self-service

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 oligomeric lactic acid compositions effectively lower vaginal pH, reducing anaerobic bacteria and malodour, with a prolonged duration of action enabling administration once a week or less, and demonstrating improved stability and user-friendliness, as evidenced by clinical studies.

Implementation Method 1

The compositions release the active ingredient, lactic acid, in a prolonged matter

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Implementation Method 2

combined with a mucoadhesive agent, to gradually release lactic acid

Methodology Applied
Scientific EffectAdhesion: Adhesive

Data Source

PatentEP2872117B1Pharmaceutical compositions containing oligomeric lactic acid
Publication Date: 2017.09.27 LACCURE AB
  • EP2872117B1 patent drawingFigure 1
  • EP2872117B1 patent drawingFigure 2
  • EP2872117B1 patent drawingFigure 3

AI summary

A composition comprising i) oligomeric lactic acid with the following formula (I) wherein n is an integer from 2 to 20, from 2 to 19, or from 2 to 18, and wherein from about 10 to about 20% w/w of the total weight of the oligomeric lactic acid is a trimer, HL3, having n equal to 2, wherein the number average molecular weight Mn of the oligomeric lactic acid is from about 200 to about 500, and ii) a mucoadhesive agent.