Vancomycin Hydrochloride Oral Liquid for Contamination Control

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Solution Overview

Problem

Current methods for administering vancomycin hydrochloride, such as mixing powder with sterile water for injection, are cumbersome, time-consuming, and prone to contamination, leading to potential infection and decreased patient compliance, especially in pediatric and geriatric populations.

Innovation Solution

A non-sterile stable liquid oral formulation of vancomycin hydrochloride, comprising vancomycin hydrochloride, citric acid, and a preservative, is developed, which is homogenous and stable for at least 30 days at ambient and refrigerated conditions, enhancing stability and patient compliance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If vancomycin hydrochloride powder is mixed with sterile water for injection, then the medication can be administered, but the process is cumbersome, time-consuming, and prone to contamination

Engineering Contradiction:
Improveease of administrationVSAvoidrisk of contamination
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent applies preliminary action by pre-formulating vancomycin hydrochloride in a stable liquid oral formulation that is ready for immediate administration. The formulation is prepared in advance with all necessary components (vancomycin hydrochloride, citric acid, and preservative) already mixed and stabilized, eliminating the need for bedside reconstitution and reducing contamination risk during administration.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent introduces an intermediary substance - a preservative system comprising citric acid and additional preservatives - that mediates between the vancomycin hydrochloride and the aqueous environment. This intermediary protects the formulation from contamination and degradation, enabling stable liquid formulation without requiring sterile water for injection.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Stability of the object's composition

If vancomycin hydrochloride is formulated as a stable liquid oral formulation with preservatives, then stability and ease of administration are improved, but the formulation complexity increases

Engineering Contradiction:
Improveformulation stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by optimizing the pH of the formulation through citric acid addition. By controlling the pH parameter within a specific range, the formulation achieves enhanced stability of vancomycin hydrochloride while maintaining palatability and preventing precipitation. This single parameter optimization enables a simpler formulation approach compared to multiple stabilizing agents.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite liquid oral formulation combining vancomycin hydrochloride with citric acid and preservatives in specific concentrations. This composite formulation achieves synergistic effects where the components work together to provide stability, prevent contamination, and maintain drug efficacy, resulting in a practically simple single-bottle ready-to-administer product.

Inventive Principle:
Principle #40Composite materials

3Quantity of substance

If intravenously-administered vancomycin is used, then systemic delivery is achieved, but it cannot penetrate the colon to reach therapeutic concentrations

Engineering Contradiction:
Improvesystemic deliveryVSAvoidtarget site concentration
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The patent applies the taking out principle by extracting vancomycin from the intravenous administration route and reformulating it specifically for oral delivery. The formulation is designed to be taken orally and delivered directly to the colon, bypassing the liver first-pass metabolism and achieving high local concentrations at the target site without requiring systemic circulation.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent utilizes the hydraulic principle of oral fluid delivery to transport the vancomycin formulation through the gastrointestinal tract. The liquid formulation is swallowed and moves through the digestive system via peristalsis, delivering the medication directly to the colon where C. difficile infections occur, achieving target site concentration without intravenous injection.

Inventive Principle:
Principle #29Pneumatics and hydraulics

Data Source

PatentEP4000628B1Composition and method for vancomycin oral liquid
Publication Date: 2025.09.24 AZURITY PHARMA INC
  • EP4000628B1 patent drawingFigure 1
  • EP4000628B1 patent drawingFigure 2
  • EP4000628B1 patent drawingFigure 3~4

AI summary

The invention relates to stable vancomycin hydrochloride powder for oral liquid formulations. Also provided herein are methods of using vancomycin oral liquid formulations for the treatment of certain diseases such as Clostridium difficile pseudomembranous colitis and Staphylococcal enterocolitis as well as kits and related products thereof.