Cyclobenzaprine Mannitol Eutectic Formulation
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Solution Overview
Problem
Current formulations of Cyclobenzaprine HCl, particularly those containing basifying agents, face stability issues and slow absorption, which are exacerbated in fibromyalgia treatment where disturbed sleep and fatigue are not adequately addressed by FDA-approved treatments.
Innovation Solution
A pharmaceutical composition comprising a eutectic of Cyclobenzaprine HCl and mannitol, with specific weight ratios and molar ratios, which includes micronized Cyclobenzaprine HCl and optional basifying agents like K2HPO4, Na2HPO4, or trisodium citrate, to enhance stability and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If Cyclobenzaprine HCl is formulated with basifying agents to improve absorption, then absorption rate is improved, but stability deteriorates
Solution Approach 1:
Mannitol is introduced as an intermediary substance that mediates between Cyclobenzaprine HCl and basifying agents. The mannitol-Cyclobenzaprine HCl eutectic composition allows basifying agents to be present without causing degradation, enabling improved absorption while maintaining stability through the protective eutectic matrix.
Solution Approach 2:
The invention creates a composite material system consisting of the eutectic mixture of mannitol and Cyclobenzaprine HCl, optionally combined with basifying agents. This composite structure provides both the stability of the eutectic and the absorption-enhancing properties of basifying agents, resolving the contradiction between stability and absorption rate.
2Stability of the object's composition
If conventional formulations are used to maintain stability, then stability is maintained, but absorption rate deteriorates
Solution Approach 1:
The invention changes the physical-chemical parameters of the formulation by creating a eutectic composition with specific weight ratios (60-90% Cyclobenzaprine HCl and 40-10% mannitol) and molar ratios (1.76±0.1). This parameter change enables both high stability and improved absorption rate, reversing the conventional trade-off.
3Stability of the object's composition
If oral formulations are used to ensure stability, then stability is maintained, but absorption speed deteriorates
Solution Approach 1:
The invention utilizes the phase transition properties of the mannitol-Cyclobenzaprine HCl eutectic system. The eutectic composition undergoes specific phase transitions that enhance dissolution and absorption rates while maintaining the stability advantages of solid oral formulations, thereby resolving the contradiction between stability and absorption speed.
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 eutectic composition improves the stability and absorption of Cyclobenzaprine HCl, providing effective treatment for fibromyalgia-related sleep disturbances and fatigue, with enhanced bioavailability and increased dissolution rates, even in the presence of basifying agents.
Implementation Method 1
A eutectic composition is formed by combining Cyclobenzaprine HCl and mannitol in specific weight ratios and molar ratios. The eutectic composition melts at a lower temperature than the individual components, enhancing dissolution and absorption.
Implementation Method 2
The Cyclobenzaprine HCl is micronized to increase its surface area and improve dissolution rate, thereby enhancing bioavailability when administered orally or sublingually.
Data Source
AI summary
The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol.