Sumatriptan Salt Formulation with Permeation Enhancer
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Solution Overview
Problem
Existing triptan formulations for treating migraine have a slow onset of action, typically taking around 30 minutes or more to provide relief, which is not sufficient for rapid pain management.
Innovation Solution
A pharmaceutical composition comprising a salt of sumatriptan, such as citrate, phosphate, or sulphate salt, combined with a mucosal permeation enhancer like alkylglycoside or saccharide alkyl ester, which enhances the drug's absorption and reduces the time to maximum plasma concentration (Tmax) to less than 30 minutes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional triptan formulations are used, then the drug can be administered, but the onset of action is slow (30 minutes or more)
Solution Approach 1:
The patent introduces a mucosal permeation enhancer as an intermediary substance that facilitates the transport of sumatriptan across the nasal mucosa. This mediator component enables faster drug absorption and delivery to the bloodstream, achieving an onset of action in less than 30 minutes while maintaining the therapeutic function of the original drug.
2Productivity
If the nasal spray formulation is used, then the drug can be delivered intranasally, but the absorption and bioavailability are insufficient
Solution Approach 1:
The patent modifies the formulation parameters by incorporating a mucosal permeation enhancer that changes the physical-chemical properties of the drug-mucosa interface. This parameter change enhances the permeability and absorption characteristics of sumatriptan, improving both absorption rate and bioavailability while maintaining safe and effective drug delivery.
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 composition achieves a Tmax of less than 30 minutes, providing faster relief from migraine pain compared to existing formulations, with improved bioavailability and absorption due to the mucosal permeation enhancer.
Implementation Method 1
a mucosal permeation enhancer like alkylglycoside or saccharide alkyl ester, which enhances the drug's absorption and reduces the time to maximum plasma concentration (Tmax) to less than 30 minutes
Data Source
AI summary
The invention provides a pharmaceutical composition for intranasal administration comprising a salt of sumatriptan or a physiologically acceptable solvate thereof, an alkyl glycoside or saccharide alkyl ester and optionally at least one pharmaceutically acceptable excipient, wherein the said composition provides Tmax value of less than 30 minutes upon said administration. Other aspects and embodiments are contemplated and described.The invention also provides a pharmaceutical composition for intranasal administration comprising a triptan, a pharmaceutically acceptable vehicle and a mucosal permeation enhancer, wherein upon said administration said composition provides a Tmax substantially equivalent to subcutaneous administration of said triptan. Other aspects and embodiments are contemplated and described.