Rasagiline L-Tartrate Stabilization via Eutectic Mixtures
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Solution Overview
Problem
Current pharmaceutical compositions of rasagiline, particularly rasagiline mesylate, face stability issues and challenges in achieving uniform distribution of the active ingredient, limiting their effectiveness and stability, and there is a need for alternative salt forms that can extend the spectrum of use without relying heavily on mannitol as a stabilizer.
Innovation Solution
The development of stable and content uniform solid pharmaceutical compositions using rasagiline L-tartrate with L-tartaric acid as a stabilizer, which involves combining rasagiline L-tartrate with 1-5 weight parts of L-tartaric acid and at least one inert pharmaceutically acceptable excipient, allowing for the creation of stable compositions that can be used in oral administration forms such as tablets, without the need for large amounts of mannitol or specific particle size control of rasagiline.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If rasagiline mesylate is used in pharmaceutical formulations, then the active ingredient can be delivered effectively, but stability problems occur and large amounts of mannitol are required as stabilizer
Solution Approach 1:
The patent changes the salt form parameter of rasagiline from mesylate to L-tartrate, which fundamentally alters the chemical properties of the active ingredient. This parameter change enables the formation of a stable eutectic mixture with L-tartaric acid, reducing the need for mannitol stabilizer while maintaining or improving stability
Solution Approach 2:
The patent creates a composite system consisting of rasagiline L-tartrate and L-tartaric acid in specific weight ratios (1:1 to 1:5). This composite mixture forms a stable eutectic composition that inherently provides stabilization without requiring large amounts of external stabilizers like mannitol
2Reliability
If rasagiline is distributed in pharmaceutical product, then the active ingredient reaches the therapeutic site, but homogeneous distribution cannot be fully guaranteed due to low loading
Solution Approach 1:
The patent changes the physical state parameter by creating a eutectic mixture between rasagiline L-tartrate and L-tartaric acid. This eutectic system improves the flow and distribution characteristics of the low-loading active ingredient, enabling more homogeneous distribution throughout the pharmaceutical product
Solution Approach 2:
L-tartaric acid serves as an intermediary substance that facilitates the uniform distribution of rasagiline L-tartrate. The eutectic mixture acts as a carrier system that ensures consistent dispersion of the active ingredient at low loading levels throughout the pharmaceutical formulation
3Adaptability or versatility
If alternative salt forms of rasagiline are used, then the spectrum of use can be extended, but stability problems may arise
Solution Approach 1:
The patent systematically evaluates different salt forms (parameter change) of rasagiline and identifies L-tartrate as the optimal choice. This specific parameter change extends the spectrum of use while simultaneously achieving superior stability through the eutectic mixture with L-tartaric acid
Solution Approach 2:
While not directly related to color, this principle analogously applies to identifying distinct physical and chemical characteristics of different salt forms. The patent uses analytical methods to detect and characterize the properties of various rasagiline salts, enabling selection of the most suitable form that balances versatility and stability
Data Source
AI summary
The invention deals with processes of making stable and content uniform solid pharmaceutical compositions comprising a salt of rasagiline with L-tartraric or fumaric acid as the active ingredient. As a result of such process, a stable and content uniform pharmaceutical composition comprising rasagiline L-tartrate or fumarate and L-tartaric acid is provided.