Beta-Guanidinopropionic Acid Salts for Flow and Stability
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Solution Overview
Problem
β-Guanidinopropionic acid (β-GPA) exhibits poor flow properties and compressibility in its solid state, making it difficult to handle and formulate effectively for pharmaceutical applications, particularly for cancer treatment due to its metastasis-suppressing properties.
Innovation Solution
Development of new pharmaceutical salts such as fumarate, succinate, and oxalate salts of β-GPA with improved physical properties, including enhanced flow characteristics and stability, which are characterized by specific Carr's Index and Hausner ratio values, and characterized using X-ray powder diffractometry and Raman spectroscopy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If beta-guanidinopropionic acid is used in its solid state form, then it exhibits poor flow properties and compressibility, but it maintains the desired pharmaceutical activity for cancer treatment
Solution Approach 1:
The patent applies parameter changes by converting beta-GPA into different salt forms (sodium salt, potassium salt, calcium salt, magnesium salt) which fundamentally alter the physical parameters of the compound. These salt forms exhibit improved flow properties and compressibility while retaining the parent compound's pharmaceutical activity for cancer treatment and metastasis suppression.
Solution Approach 2:
The patent creates composite material systems by forming salts of beta-GPA with various cations. Each salt form represents a composite structure that combines the active pharmaceutical ingredient with counterions, resulting in materials that maintain therapeutic efficacy while improving handling characteristics such as flow and compressibility for tablet formulation.
2Reliability
If beta-guanidinopropionic acid is used for cancer treatment, then it suppresses metastasis effectively, but its poor physical properties make formulation difficult
Solution Approach 1:
The patent changes the physical and chemical parameters of beta-GPA by forming various salt derivatives. These parameter changes transform the compound from a difficult-to-formulate substance into materials with improved solubility, flow, and compressibility characteristics, enabling effective pharmaceutical formulation while preserving the metastasis-suppressing therapeutic effect.
Solution Approach 2:
The patent uses counterions (sodium, potassium, calcium, magnesium) as intermediary substances that mediate between the active beta-GPA molecule and the formulation requirements. These intermediary ions form salt structures that facilitate manufacturing processes while the beta-GPA component maintains its biological activity for metastasis suppression.
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 improved salts exhibit excellent flow properties and stability, enabling more effective formulation and administration of β-GPA for cancer treatment, particularly in suppressing metastasis, with the fumarate salt showing excellent flow characteristics and the succinate and oxalate salts demonstrating good stability and retention of crystalline form under various conditions.
Implementation Method 1
characterized using X-ray powder diffractometry and Raman spectroscopy
Implementation Method 2
have at least one peak at diffraction angle 2θ (°) of 20±0.5 as measured by X-ray powder diffractometry
Implementation Method 3
characterized using X-ray powder diffractometry and Raman spectroscopy
Data Source
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AI summary
The present invention relates to new pharmaceutical salts of β-GPA which exhibit improved physical properties. In particular, the invention relates to salts of β-GPA with improved flow properties (e.g., improved Carr's index and/or Hausner ratio) such as fumarate salts, succinate salts, and oxalate salts. The invention also relates to pharmaceutical compositions including a pharmaceutically effective amount of one or more salts of β-GPA, as well as methods of treating cancer including administration of a formulation including a β-GPA salt of the invention to a subject in need thereof.