Vaginal Tablet Composition Using GDL for Stable Slow Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for vaginal infections, such as vaginal capsules, tablets, and creams, suffer from high recurrence of infections, side effects, risks during pregnancy, and potential drug resistance, and are not suitable for stable solid formulations like tablets or rings due to the use of gluconic acid in liquid form.
Innovation Solution
A solid pharmaceutical composition comprising glucono-δ-lactone (GDL) and hypromellose (HPMC) is developed for vaginal administration, providing a slow-release formulation that maintains stability and efficacy over an extended period.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If gluconic acid is used in liquid form (50% water solution) for vaginal treatment, then antimicrobial efficacy is achieved, but the formulation cannot be made into a stable solid pharmaceutical form (tablet, suppository, ring)
Solution Approach 1:
The patent changes the physical state parameter of the active ingredient from liquid (gluconic acid 50% water solution) to solid (GDL crystalline form). This parameter change enables the formulation to be manufactured as stable solid dosage forms while maintaining the antimicrobial efficacy through the lactone form's bioactivity.
Solution Approach 2:
The patent creates a composite formulation combining GDL (active ingredient) with excipients such as HPMC (hydroxypropyl methylcellulose) to formulate stable solid pharmaceutical products. The composite material approach allows the solid GDL to maintain stability while releasing active gluconic acid in situ.
2Reliability
If conventional antimicrobial treatments (econazol, clotrimazole, miconazole, etc.) are used, then infection treatment is achieved, but high recurrence rates and side effects occur
Solution Approach 1:
The patent employs a biocompatible, naturally metabolizable substance (GDL) that acts locally and temporarily, converting to gluconic acid which is naturally present in the body. This disposable-like approach avoids accumulation and long-term side effects associated with conventional azole antifungals.
Solution Approach 2:
The patent converts the typically harmful alkaline environment created by infections into a beneficial condition by using GDL, which acidifies the vaginal environment (lowering pH), thereby creating an unfavorable condition for pathogenic bacteria and fungi that thrive in alkaline conditions.
3Ease of operation
If pharmaceutical fat-based pessaries are used for vaginal treatment, then delivery is achieved, but stability at elevated temperatures is poor
Solution Approach 1:
The patent replaces the fat-based mechanical carrier system with a water-soluble polymer matrix system (HPMC and similar excipients). This substitution eliminates the thermal instability of fats while maintaining the desired dissolution and release properties in the vaginal environment.
4Duration of action of stationary object
If the product needs to be stable during transport and storage (shaking, temperature changes), then shelf life is extended, but the product may become slippery or shiny affecting application
Solution Approach 1:
The patent applies different quality characteristics to different aspects of the product: the external surface is formulated to be non-slippery and non-shiny for easy handling and application, while the internal composition maintains stability against shaking and temperature changes. The tablet surface treatment and coating techniques provide the desired external properties without compromising internal stability.
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 reduces biofilm formation by Candida species and bacteria, offering a stable, safe, and effective treatment option with minimal side effects and reduced risk of resistance, suitable for use during pregnancy and daily activities.
Implementation Method 1
GDL is a solid at room temperature and body temperature and is therefore suitable to use as the active ingredient in e.g. a vaginal tablet
Implementation Method 2
Gluconic acid is known to reduce the presence of biofilm. The present inventors have found that GDL as such has an effect on the formation of biofilm of different Candida species as well as bacteria
Implementation Method 3
The vaginal microbiome is a dynamic system with a complex mixture of various microorganisms in different ratios and quantities, which depends upon lactic acid producing bacteria to maintain a weakly acidic environment
Data Source
AI summary
The present invention concerns a pharmaceutical composition comprising glucono-δ-lactone, which is suitable for use in the treatment of vaginal microbial infections.