Totarol Vaginal Composition for Selective Antibacterial Action

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Solution Overview

Problem

Current treatments for bacterial vaginosis (BV) and aerobic vaginitis (AV) face challenges due to increasing antibiotic resistance, particularly in Gardnerella vaginalis, leading to recurrent infections and disruptions in vaginal flora, with existing antibiotics often harming beneficial Lactobacillus bacteria, causing secondary fungal infections and limited effectiveness.

Innovation Solution

A pharmaceutical composition containing totarol, a natural diterpene with broad-spectrum antibacterial activity, is developed, specifically formulated with methylcellulose, lactic acid, and a basic polymer to target pathogenic bacteria while sparing Lactobacillus species, ensuring selective antibacterial action and pH regulation to restore vaginal flora.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antibiotics are used to treat bacterial vaginosis, then pathogenic bacteria are eliminated, but beneficial Lactobacillus bacteria are also harmed causing secondary fungal infections

Engineering Contradiction:

Improveeffectiveness of treatmentVSAvoidsecondary fungal infections

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies selective antibacterial action where totarol exhibits different effects on different bacterial types. The composition targets pathogenic bacteria (Gardnerella vaginalis, Atopobium vaginae, Mobiluncus spp.) while sparing beneficial Lactobacillus species through specific concentration ranges and formulation characteristics that create local differences in biological activity.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent utilizes pH regulation as a key parameter to differentiate between pathogenic and beneficial bacteria. By maintaining vaginal pH below 4.5 through lactic acid and buffering systems, the composition creates conditions favorable for Lactobacillus growth while inhibiting pathogenic bacteria that thrive at higher pH levels.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If antibiotics are used to treat bacterial vaginosis, then bacterial infection is reduced, but recurrence of infections increases due to flora disruption

Engineering Contradiction:

Improveeffectiveness of treatmentVSAvoidrecurrence of infections

Core Design Contradiction:

ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The composition includes probiotic Lactobacillus species and prebiotic substances that prepare and restore the vaginal microflora before and during the antibacterial treatment. This preliminary restoration of beneficial flora prevents the ecological vacuum that would otherwise allow pathogenic bacteria to recur.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The composition creates a self-regulating system where restored Lactobacillus populations produce lactic acid that maintains pH below 4.5, which in turn continues to inhibit pathogenic bacteria. This feedback loop ensures long-term prevention of recurrence without requiring continuous antibiotic treatment.

Inventive Principle:

Principle #23Feedback

3Adaptability or versatility

If broad-spectrum antibiotics are used, then multiple pathogens are targeted, but the vaginal flora composition is disrupted

Engineering Contradiction:

Improvebroad-spectrum activityVSAvoidvaginal flora composition

Core Design Contradiction:

Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The composition combines multiple components with complementary functions: totarol for selective antibacterial activity, lactic acid for pH regulation, basic polymers for buffering capacity, and probiotic Lactobacillus species for flora restoration. This composite formulation achieves broad pathogen coverage while preserving and restoring beneficial flora through the synergistic interaction of its components.

Inventive Principle:

Principle #40Composite materials

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 effectively targets pathogenic bacteria with low Minimum Inhibitory Concentration (MIC) values, reducing recurrence of infections and maintaining the vaginal pH, thus preventing secondary fungal infections and promoting a healthy vaginal environment.

Implementation Method 1

lactic acid, in an amount of 0.5 to 5 parts by wt., wherein the stoichiometric ratio of lactic acid to the basic polymer is comprised in the range of 1:1 to 8:1

Methodology Applied

Scientific EffectpH regulation:

Data Source

PatentUS11534412B2Application of totarol and pharmaceutical composition containing totarol

Publication Date: 2022.12.27 EMERGOPHARM SP ZOO SPK

AI summary

The invention relates to application of totarol for production of a preparation for treatment of vaginal mucous membrane inflammations of bacterial origin, for alleviation of symptoms in such a treatment, and for prophylaxis and prevention of relapses of such inflammations. The invention includes also a pharmaceutical composition for treatment of vaginal mucous membrane inflammations of bacterial origin, for alleviation of symptoms in such a treatment and for prophylaxis and prevention of relapses of such inflammations, the composition containing from 75 to 95 parts by wt. of a cellulose derivative, from 0.5 to 5 parts by wt. of lactic acid, from 0.5 to 5 parts by wt. of a basic polymer, wherein the stoichiometric ratio of lactic acid to the basic polymer is comprised in the range of 1:1 to 8:1, and comprising totarol in an amount of 0.001 to 5 parts by wt. as the active substance.