Riluzole Solubility via Beta-Cyclodextrin Inclusion Complexes
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Solution Overview
Problem
Riluzole, used to treat amyotrophic lateral sclerosis (ALS), has limited solubility in water, leading to adverse events at higher oral doses, necessitating alternative administration methods with improved safety profiles.
Innovation Solution
Parenteral administration of riluzole dissolved in a ß-cyclodextrin solution, specifically intrathecal delivery, to achieve effective dosing without the adverse effects associated with oral administration, potentially combined with oral doses to enhance therapeutic outcomes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral administration of riluzole is used to treat ALS, then the drug can be delivered systemically, but the low water solubility limits the dose and causes adverse events
Solution Approach 1:
The patent uses cyclodextrins as intermediary molecules to solubilize riluzole in aqueous solutions. The cyclodextrin forms an inclusion complex with riluzole, acting as a mediator that enables the poorly water-soluble drug to be delivered via parenteral routes without causing precipitation or adverse events associated with high-dose oral administration.
2Reliability
If higher doses of riluzole are administered orally to improve treatment efficacy, then more drug reaches the target, but adverse events increase preventing dose escalation
Solution Approach 1:
The patent changes the physical-chemical parameters of the drug delivery system by using cyclodextrin inclusion complexes. This allows the drug to be administered via parenteral routes with controlled release, achieving effective therapeutic levels without the adverse events that limit oral dose escalation.
3Object-affected harmful factors
If parenteral administration of riluzole is implemented, then adverse events are reduced, but the drug's low solubility in water prevents effective dosing
Solution Approach 1:
The patent creates a composite pharmaceutical composition consisting of cyclodextrin and riluzole in aqueous solution. The cyclodextrin component provides water solubility while the riluzole component provides therapeutic activity, together enabling parenteral administration with both improved solubility and reduced adverse events.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The method allows for safe and effective administration of riluzole with reduced adverse events, achieving therapeutic levels in the spinal cord and brain while minimizing peripheral exposure, thus improving treatment efficacy and safety.
Implementation Method 1
Riluzole is used as the active ingredient in a formulation that comprises a ß-cyclodextrin solution. In particular, the riluzole is dissolved in the ß-cyclodextrin solution.
Data Source
AI summary
The present invention provides methods for parenterally administering riluzole to subjects in need of treatment.