Topical Tranexamic Acid Composition for Wound Bleeding Control

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Solution Overview

Problem

Systemically administered tranexamic acid formulations lead to significant bleeding reduction but cause systemic side effects and fail to concentrate effectively at wound sites, necessitating a topical formulation that minimizes systemic exposure while maintaining therapeutic efficacy.

Innovation Solution

Development of a topical aqueous composition containing tranexamic acid in a pharmaceutically acceptable vehicle, stabilized with hydroxyethyl cellulose as a viscosity modifying agent, and buffered with sodium citrate and citric acid, providing a therapeutically effective concentration of 200-300 mg/mL with a viscosity of 1-2000 cps for prolonged residence on wounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If orally or intravenously administered TXA is used, then bleeding reduction is achieved, but systemic side effects occur and systemic exposure is high

Engineering Contradiction:
Improvebleeding reductionVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by formulating TXA in a topical composition for localized application to wounds or lesions. This delivers the anti-fibrinolytic effect specifically at the site of bleeding without distributing the drug systemically, thereby achieving bleeding reduction while avoiding systemic side effects such as blood clots, seizures, and blurred vision

Inventive Principle:
Principle #3Local quality

2Reliability

If orally or intravenously administered TXA is used, then bleeding reduction is achieved, but TXA does not concentrate effectively at the wound site

Engineering Contradiction:
Improvebleeding reductionVSAvoidTXA concentration at wound site
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The topical formulation ensures that TXA is delivered in high concentration directly to the wound site rather than being distributed systemically at lower concentrations. The localized application method concentrates the therapeutic agent where it is needed most, improving efficacy at the target site

Inventive Principle:
Principle #3Local quality

3Object-affected harmful factors

If topical TXA composition is applied, then systemic exposure is minimized, but prolonged residence on wound is needed for sustained efficacy

Engineering Contradiction:
Improvesystemic exposureVSAvoidresidence time on wound
Core Design Contradiction:
Object-affected harmful factorsVSDuration of action of moving object

Solution Approach 1:

The patent modifies the physical parameters of the TXA formulation by adjusting viscosity (1-2000 cps) and pH (3-5) to optimize residence time on the wound. The viscosity-modified aqueous composition adheres better to the wound surface, prolonging contact time and sustaining the anti-fibrinolytic effect while maintaining minimal systemic absorption

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20240415794A1Topical tranexamic acid compositions and methods of use thereof
Publication Date: 2024.12.19 BIO 54 LLC
  • US20240415794A1 patent drawing

AI summary

The present disclosure relates to pharmaceutical compositions of tranexamic acid and methods of using the compositions. The pharmaceutical compositions of the present disclosure are stable and suitable for topical application.