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
Engineering 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
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
2Reliability
If orally or intravenously administered TXA is used, then bleeding reduction is achieved, but TXA does not concentrate effectively at the wound site
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
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
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
Data Source
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.
