Sumatriptan Intranasal Formulation with Permeation Enhancer
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Solution Overview
Problem
Current triptan formulations for treating migraine headaches have a slow onset of action, taking around 30 minutes or more, which is not sufficient for rapid pain relief, and there is a need for formulations with increased speed of action and improved permeability.
Innovation Solution
A pharmaceutical composition comprising a salt of sumatriptan or its physiologically acceptable solvate combined with a mucosal permeation enhancer, such as an alkylglycoside or saccharide alkyl ester, which provides a Tmax value of less than 30 minutes upon administration, mimicking the pharmacokinetic profile of subcutaneous administration when administered intranasally.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional triptan formulations are used, then the drug can be administered orally or via nasal spray, but the onset of action is slow (30 minutes or more)
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using supercritical fluid extraction to create a novel delivery system. This transforms the drug delivery parameters to achieve faster absorption and onset of action while reducing the time to maximum plasma concentration
Solution Approach 2:
The invention creates a composite formulation combining triptan compounds with permeation enhancers and uses supercritical fluid technology to produce a composite delivery system that enhances absorption rate and reduces onset time
2Productivity
If the formulation is designed for rapid absorption, then the onset of action improves, but the permeability through mucosal membranes becomes the limiting factor
Solution Approach 1:
The patent introduces permeation enhancers as intermediary substances that facilitate the transfer of triptan compounds through the mucosal membrane barrier. These enhancers act as mediators that temporarily increase membrane permeability, enabling faster and more reliable drug absorption
Solution Approach 2:
The invention replaces conventional mechanical absorption processes with supercritical fluid extraction technology, which uses fluid dynamics and phase transitions to enhance permeability and absorption efficiency beyond traditional mechanical diffusion
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 faster onset of action and improved bioavailability, with a Tmax value of less than 30 minutes, significantly reducing the time to maximum plasma concentration and enhancing the absorption of sumatriptan, thereby providing quicker relief from migraine symptoms.
Implementation Method 1
A pharmaceutical composition comprising a salt of sumatriptan or a pharmaceutically acceptable solvate thereof, and a mucosal permeation enhancer
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.