Stable Oral Formulation of 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic Acid
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Solution Overview
Problem
Current oral formulations containing 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazol-4-carboxylic acid as a xanthine oxidase inhibitor face stability and assay homogeneity issues due to interactions with excipients, necessitating the inclusion of stabilizers, which complicates drug development and increases costs.
Innovation Solution
An oral formulation comprising 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazol-4-carboxylic acid or its pharmaceutically acceptable salt without a separate stabilizer, using a combination of diluent, disintegrant, binder, glidant, and lubricant excipients, ensuring stability and assay homogeneity across various storage conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If stabilizers are added to the oral formulation to maintain API stability, then the stability of the formulation is improved, but the device complexity and manufacturing complexity increase
Solution Approach 1:
The patent removes the stabilizer component from the formulation entirely. Through careful selection of excipients (microcrystalline cellulose, crospovidone, magnesium stearate, colloidal silicon dioxide) that are inherently compatible with the API, the formulation achieves stability without requiring additional stabilizing agents, thereby simplifying the formulation composition
Solution Approach 2:
The patent changes the formulation parameters by selecting specific excipients with appropriate properties (particle size, surface area, chemical compatibility) that naturally prevent API degradation. This parameter optimization allows the formulation to maintain stability through excipient-API compatibility rather than through stabilizer addition
2Stability of the object's composition
If multiple excipients are tested and combined to ensure API compatibility, then the formulation stability is improved, but the development time and productivity are reduced
Solution Approach 1:
The patent applies preliminary compatibility assessment between the API and selected excipients during the formulation design stage. By pre-selecting excipients known to be compatible with xanthine oxidase inhibitors and conducting targeted stability testing, the development process avoids extensive trial-and-error experimentation, thereby improving development efficiency while ensuring formulation stability
3Manufacturing precision
If stabilizers are included in the formulation, then the assay homogeneity is maintained, but the manufacturing cost increases
Solution Approach 1:
The patent eliminates the stabilizer component from the formulation, thereby removing the associated manufacturing cost. The assay homogeneity is maintained through proper excipient selection and formulation design that ensures uniform distribution and stability of the API without requiring additional stabilizing agents
Data Source
AI summary
The present invention relates to a stable oral formulation comprising 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazol-4-carboxylic acid or a pharmaceutically acceptable salt thereof as an API.The stable oral formulation according to the present invention has the characteristics of maintaining stability even if it does not comprise a stabilizer as an excipient, and does not comprise a stabilizer but has increased API content, and thus the convenience of administration can be increased.