Levodopa-Tyrosine Polymorphs for Solubility and Bioavailability
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Solution Overview
Problem
There is a need for additional therapeutic agents to treat degenerative disorders such as Parkinson's disease, as some patients become less responsive to levodopa over time, and preparing liquid formulations of levodopa can be difficult.
Innovation Solution
The development of crystalline forms of ((S)-2-amino-3-(3,4-dihydroxyphenyl) propanoyl)-L-tyrosine, including crystalline forms and their anhydrates and hydrates, which are characterized by specific powder X-ray diffraction patterns and thermal properties, and their use in pharmaceutical compositions for treating conditions associated with reduced dopamine levels in the brain.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If levodopa is used as a therapeutic agent for Parkinson's disease, then dopamine concentration in the brain is restored, but patients become less responsive after 3-4 years of therapy
Solution Approach 1:
The patent applies parameter changes by modifying the crystalline structure of levodopa to create different polymorphic forms with distinct physical and chemical properties. These structural parameter changes result in variations in solubility, dissolution rate, and bioavailability, thereby altering the therapeutic response profile and potentially extending the duration of effective therapy
Solution Approach 2:
The patent utilizes composite material principles by creating levodopa polymorphs that combine the active pharmaceutical ingredient with specific crystal lattice arrangements. These composite crystalline structures provide enhanced stability and controlled release characteristics, addressing the issue of diminished therapeutic response over time
2Ease of operation
If liquid formulations of levodopa are prepared, then therapeutic delivery is improved, but formulation preparation becomes difficult
Solution Approach 1:
The patent applies parameter changes by controlling the crystallization conditions to produce polymorphic forms with specific solubility characteristics. By adjusting parameters such as solvent type, temperature, and pH during formulation preparation, the patent enables easier creation of liquid formulations with improved therapeutic 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 crystalline forms of ((S)-2-amino-3-(3,4-dihydroxyphenyl) propanoyl)-L-tyrosine provide a stable and effective therapeutic option for conditions like Parkinson's disease, offering improved solubility and bioavailability, and can be formulated into various dosage forms for administration.
Implementation Method 1
characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 2θ at about 20.1
Implementation Method 2
characterized by a powder X-ray diffraction pattern having characteristic peaks in degrees 2θ at about 12.6, 16.3, and 20.1
Data Source
AI summary
The disclosure is in part directed to crystalline forms of ((S)-2-amino-3-(3,4-dihydroxyphenyl)propanoyl)-A-tyrosine and pharmaceutical compositions thereof.