Meloxicam SBEβCD Inclusion Complex for Rapid Onset
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Solution Overview
Problem
Meloxicam, a nonsteroidal anti-inflammatory drug, has poor aqueous solubility, leading to reduced bioavailability and slow onset of pain relief, which is exacerbated in patients with inadequate responses to prior migraine treatments.
Innovation Solution
The use of a combination of meloxicam with sulfobutyl ether β-cyclodextrin (SBEβCD) and a bicarbonate, such as sodium bicarbonate, to form an inclusion complex that enhances solubility and bioavailability, often paired with rizatriptan for improved migraine treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If meloxicam is administered in conventional formulations, then the drug can be delivered to patients, but its poor aqueous solubility reduces bioavailability and slows onset of pain relief
Solution Approach 1:
The patent uses cyclodextrins as intermediary carriers to solubilize meloxicam. The cyclodextrin molecules form inclusion complexes with meloxicam, where the hydrophobic interior of the cyclodextrin cavity accommodates the meloxicam molecule while the hydrophilic exterior interacts with aqueous media, thereby enhancing solubility and bioavailability without altering the meloxicam molecule itself
Solution Approach 2:
The patent modifies the physical-chemical parameters of meloxicam by forming inclusion complexes with cyclodextrins. This complexation changes the apparent solubility parameters of meloxicam in aqueous solutions, transforming it from a poorly soluble compound to one with enhanced bioavailability while maintaining the original drug's pharmacological properties
2Speed
If meloxicam is administered in conventional formulations, then the drug can treat pain, but the onset of pain relief is slow
Solution Approach 1:
Cyclodextrins serve as mediators that facilitate rapid dissolution and absorption of meloxicam. By forming soluble inclusion complexes, the cyclodextrins enable faster drug release in the gastrointestinal tract, leading to quicker onset of pain relief compared to conventional formulations
3Reliability
If patients with inadequate response to prior migraine treatments receive conventional meloxicam, then standard treatment protocols are followed, but pain relief is insufficient and rescue medication is needed
Solution Approach 1:
The patent enhances treatment reliability by modifying the bioavailability parameter of meloxicam through cyclodextrin complexation. This results in more consistent and predictable pain relief outcomes, reducing the need for rescue medication in patients with inadequate responses to prior treatments
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
This combination significantly increases the oral bioavailability of meloxicam, leading to rapid and sustained pain relief in patients with a history of inadequate responses to prior treatments, reducing the need for rescue medication and providing longer-lasting pain freedom.
Implementation Method 1
In aqueous solutions, cyclodextrins can form complexes (i.e., an inclusion complex) with drugs by incorporating the drug into the center/hydrophobic portion of the cyclodextrin ring
Implementation Method 2
a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD)
Data Source
AI summary
Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.