Afatinib Dimaleate Form Alpha Stability
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Solution Overview
Problem
There is a need for additional solid state forms of Afatinib di-maleate to improve processing properties, stability, and bioavailability, as existing forms may have limitations in handling, dissolution profiles, and shelf-life.
Innovation Solution
The development of Afatinib di-maleate Form Alpha, characterized by specific X-ray powder diffraction patterns and thermal properties, which can be used to prepare pharmaceutical compositions and other Afatinib salts, enhancing thermodynamic stability and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing solid state forms of Afatinib di-maleate are used, then the basic therapeutic function is achieved, but processing properties and stability are limited
Solution Approach 1:
The patent applies parameter changes by discovering and characterizing multiple polymorphic forms (Forms A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, Q, R, S, T, U, V, W, X, Y, Z) of Afatinib di-maleate, each with distinct crystal structures, X-ray diffraction patterns, and physical properties. This allows selection of the optimal polymorphic form based on desired processing properties and stability requirements for specific pharmaceutical applications
2Reliability
If existing solid state forms of Afatinib di-maleate are used, then the formulation is achieved, but dissolution profile and bioavailability are limited
Solution Approach 1:
The patent utilizes parameter changes by providing a comprehensive set of polymorphic forms with varying dissolution characteristics. Each polymorphic form exhibits different solubility and dissolution rates, enabling formulation scientists to select the optimal form to achieve target bioavailability and dissolution profiles for specific dosage forms and therapeutic indications
3Duration of action of stationary object
If existing solid state forms of Afatinib di-maleate are used, then the basic formulation is achieved, but shelf-life is limited
Solution Approach 1:
The patent applies parameter changes by characterizing multiple polymorphic forms with distinct thermal behaviors, melting points, and stability profiles. This enables selection of polymorphic forms with optimized shelf-life characteristics and handling properties, such as improved flowability, compressibility, and resistance to polymorphic transformation during storage and processing
Data Source
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AI summary
The present disclosure encompasses crystalline forms of Afatininb di-maleate and methods of their use.