Anhydrous Dasatinib Photostability via Titanium Oxide
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Solution Overview
Problem
Anhydrous dasatinib-containing preparations are unstable to light, leading to light-induced discoloration and the generation of related substances during storage, which affects their photostability.
Innovation Solution
Incorporating titanium oxide, yellow or red ferric oxide as colorants, and antioxidants such as tocopherol or dibutylhydroxytoluene into the anhydrous dasatinib-containing preparations, either within the tablet formulation or as a film-coating, to enhance photostability by inhibiting light-induced discoloration and the formation of related substances.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If anhydrous dasatinib is used as the drug substance, then the photostability is poor and light-induced discoloration occurs, but using dasatinib hydrate may have other stability issues
Solution Approach 1:
The patent introduces titanium oxide as an intermediary substance that absorbs or blocks light before it can interact with the anhydrous dasatinib. The titanium oxide acts as a protective mediator between the light source and the drug substance, preventing the harmful photochemical reactions that cause discoloration and degradation while allowing the anhydrous form to maintain its stability advantages.
Solution Approach 2:
The patent creates a protected environment by incorporating titanium oxide and antioxidants into the formulation, effectively creating a light-shielding and chemically protective matrix around the anhydrous dasatinib. This inert environment prevents light from directly interacting with the drug substance, thereby maintaining photostability.
2Reliability
If antioxidants are added to improve photostability, then the stability during storage improves, but the formulation complexity increases
Solution Approach 1:
The patent optimizes the concentration and type of antioxidants used, adjusting these parameters to achieve the desired photostability improvement while minimizing formulation complexity. By carefully selecting specific antioxidants and their optimal concentrations, the patent balances stability enhancement with formulation simplicity.
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 addition of these additives significantly improves the photostability of anhydrous dasatinib-containing preparations by reducing color change and the generation of related substances when exposed to light, thereby maintaining the stability and efficacy of the drug during storage.
Implementation Method 1
the preparation containing anhydrous dasatinib as a drug substance was unstable to light
Implementation Method 2
the weight ratio of the colorant per the anhydrous dasatinib may be more than 0 and 1 or less
Implementation Method 3
the antioxidant may be an antioxidant with a benzene ring. The antioxidant with a benzene ring may be a tocopherol or a dibutylhydroxytoluene
Data Source
AI summary
An anhydrous dasatinib-containing preparation comprising an anhydrous dasatinib and a titanium oxide or colorant or antioxidant is provided. In one embodiment, the anhydrous dasatinib-containing preparation improves photostability upon storage. The weight ratio of the titanium oxide per the anhydrous dasatinib may be more than 0 and 2 or less, or the weight ratio of the colorant per the anhydrous dasatinib may be more than 0 and 1 or less, or the weight ratio of the antioxidant per the anhydrous dasatinib may be more than 0 and 0.5 or less.