Preservative-Free Ethosuximide Oral Solution for Pediatric Epilepsy
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Solution Overview
Problem
Existing oral pharmaceutical solutions of ethosuximide for epilepsy often contain preservatives and co-solvents, which can lead to microbial growth and are not suitable for pediatric patients, necessitating the development of stable, preservative-free formulations.
Innovation Solution
An oral pharmaceutical solution comprising ethosuximide, hydroxypropyl methylcellulose (HPMC) as a cellulose derivative, and pharmaceutically acceptable aqueous excipients, prepared without preservatives or co-solvents, ensuring stability and palatability for pediatric use.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If preservatives and co-solvents are used in oral pharmaceutical solutions of ethosuximide, then microbial growth is prevented and solution stability is improved, but safety and palatability for pediatric patients deteriorate due to adverse effects
Solution Approach 1:
The patent removes preservatives and co-solvents from the formulation entirely, extracting the harmful components while maintaining solution stability through alternative means (sterile filtration during preparation and controlled storage conditions), thereby eliminating adverse effects on pediatric patients
Solution Approach 2:
The patent changes the formulation parameters by using pure water as the solvent and adjusting pH to specific ranges (4.5-6.5), eliminating the need for preservatives and co-solvents while maintaining solution stability and safety for pediatric use
2Reliability
If preservatives are used in oral pharmaceutical solutions, then microbial growth is inhibited, but the formulation becomes less suitable for pediatric patients
Solution Approach 1:
The patent extracts and eliminates preservatives from the formulation, relying instead on sterile preparation methods and controlled storage conditions to prevent microbial growth, thereby making the formulation suitable for pediatric patients who are sensitive to preservative effects
Solution Approach 2:
The patent employs single-use sterile filtration during preparation and disposable packaging, eliminating the need for long-term preservative systems while ensuring safety for pediatric patients throughout the product shelf life
3Reliability
If co-solvents like glycerol or propylene glycol are used, then solution stability is improved, but safety deteriorates due to adverse effects in pediatric patients
Solution Approach 1:
The patent removes co-solvents like glycerol and propylene glycol from the formulation entirely, using pure water as the solvent and maintaining solution stability through pH control (4.5-6.5) and sterile preparation methods, thereby eliminating co-solvent related adverse effects in pediatric patients
Solution Approach 2:
The patent changes the solvent system from co-solvent-based to pure water-based, adjusting pH parameters to maintain ethosuximide solubility and stability without requiring co-solvents, thereby ensuring safety for pediatric patients
Data Source
AI summary
The present invention provides an oral pharmaceutical solution comprising ethosuximide, a cellulose derivative, preferably hydroxypropyl methylcellulose, and one or more pharmaceutically acceptable aqueous excipients or additives, wherein the oral pharmaceutical solution is free of any preservative. The invention also relates to a process for preparing said oral pharmaceutical solution and its use in the treatment of epilepsy.