Rifaximin Polymorphic Forms Modulating Bioavailability
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Rifaximin's polymorphic forms exhibit varying bioavailability and systemic absorption, leading to challenges in treating bacterial infections effectively while minimizing resistance induction and adverse events.
Innovation Solution
Discovery and characterization of new polymorphic forms of rifaximin, specifically Form Mu, which are characterized by distinct X-ray powder diffraction peaks, allowing for the modulation of therapeutic action by selecting appropriate forms for treatment based on infection type.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional rifaximin forms are used, then broad antibacterial activity is achieved, but bioavailability and systemic absorption vary leading to treatment inefficiency
Solution Approach 1:
The patent applies parameter changes by discovering and characterizing multiple polymorphic forms (α, β, γ, δ, ε, ζ, η, θ, ι, κ, λ, μ, ν, ξ, ο, π, ρ, σ, τ, υ, φ, χ, ω) of rifaximin, each with distinct crystal structures and X-ray diffraction patterns. These different polymorphic forms exhibit varying degrees of bioavailability and systemic absorption, allowing clinicians to select the most appropriate form for specific treatment scenarios, thereby resolving the contradiction between reliable treatment efficacy and adaptability in bioavailability modulation.
2Reliability
If rifaximin is administered to treat bacterial infections, then antibacterial activity is achieved, but resistance induction and adverse events occur
Solution Approach 1:
The patent applies local quality by enabling targeted selection of specific polymorphic forms based on infection type and desired therapeutic outcome. Different polymorphic forms can be selectively administered to achieve localized effects in the gastrointestinal tract with minimized systemic absorption, thereby maintaining effective antibacterial activity at the site of infection while reducing the risk of resistance induction and adverse events associated with systemic exposure.
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 new polymorphic forms of rifaximin, such as Form Mu, enable tailored bioavailability and absorption profiles, enhancing treatment efficacy for gastrointestinal disorders while reducing resistance and adverse effects.
Implementation Method 1
characterized by an X-ray powder diffraction comprising peaks, in terms of 2θ, at 4.72, 4.79, 7.84, 8.11, 8.36, 8.55, 8.70, 9.60, and 12.54
Data Source
Figure 1
Figure 2
Figure 3
AI summary
Embodiments relate to Rifaximin polymorphic, salt, and hydrate forms, methods of producing polymorphic forms and to their use in medicinal preparations and to therapeutic methods using them.