Anhydrous Soft Glycopyrrolate Formulation for Hyperhidrosis
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Solution Overview
Problem
Current topical anticholinergic agents used for treating hyperhidrosis suffer from undesirable systemic side effects and lack stable, pharmaceutically acceptable formulations with commercially viable shelf-life.
Innovation Solution
A stable, anhydrous topical composition comprising soft anticholinergic esters, such as glycopyrrolate esters, in anhydrous ethanol with optional gelling or viscosity-controlling agents, providing a formulation that minimizes systemic side effects and enhances stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If topical anticholinergic agents are administered to treat hyperhidrosis, then sweat production is reduced, but systemic side effects occur
Solution Approach 1:
The patent modifies the chemical parameters of anticholinergic compounds by creating ester derivatives (soft drugs) that change their metabolic properties. These modified compounds are rapidly metabolized by esterases in the skin and systemic circulation, converting them to inactive carboxylic acid forms, thereby reducing systemic side effects while maintaining local efficacy for sweat reduction
Solution Approach 2:
The patent introduces ester functional groups as intermediary chemical structures that facilitate rapid metabolic conversion. These ester groups act as metabolic handles that enable quick inactivation of the drug by endogenous esterases, serving as an intermediary mechanism between active drug administration and inactive metabolite elimination
2Stability of the object's composition
If aqueous formulations are used for soft anticholinergic esters, then the drug is stable in solution, but hydrolysis occurs reducing shelf-life
Solution Approach 1:
The patent employs anhydrous (water-free) alcoholic solvents to create an inert environment that prevents hydrolysis of the ester bonds. By eliminating water from the formulation matrix, the patent creates conditions where the soft anticholinergic esters remain chemically stable without undergoing hydrolytic degradation, thereby extending shelf-life while maintaining drug stability in solution
Data Source
AI summary
Topical formulations comprising soft glycopyrrolates are useful for treating excessive sweating conditions in subjects, such as humans suffering from hyperhidrosis. Preferably, at least one soft anticholinergic agent is provided in an effective amount or concentration in an anhydrous formulation that can inhibit excessive perspiration resulting from a condition such as hyperhidrosis.