PVA-Coated Ribociclib Tablets for High Drug Load Stability
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Solution Overview
Problem
Existing formulations of ribociclib succinate tablets face challenges in achieving high drug load and maintaining stability while ensuring an immediate release profile without defects such as cracking.
Innovation Solution
A coated pharmaceutical oral tablet formulation of ribociclib succinate with a high drug load of at least 40% and an aqueous moisture barrier coating comprising polyvinyl alcohol (PVA) based Opadry ®< amb II, which improves tablet appearance and prevents cracking.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If high drug load is achieved in ribociclib succinate tablets, then the therapeutic efficacy is improved, but tablet stability and integrity deteriorate due to cracking and defects
Solution Approach 1:
The patent modifies the coating composition by incorporating polyvinyl alcohol (PVA) as a key polymer component and adjusting the coating formulation to create a flexible moisture barrier coating. This parameter change in the coating system allows the tablet to maintain structural integrity and prevent cracking while accommodating high drug loads of ribociclib succinate (at least 40% w/w), thereby resolving the contradiction between high drug load and tablet stability.
2Reliability
If aqueous coating is used to prevent cracking, then tablet integrity is improved, but moisture barrier effectiveness may be compromised
Solution Approach 1:
The patent employs a composite coating formulation that combines polyvinyl alcohol (PVA) with other polymers and functional ingredients to create a multi-functional coating system. This composite material simultaneously provides flexibility to prevent cracking and maintains effective moisture barrier properties, thus resolving the contradiction between tablet integrity and moisture protection in aqueous-coated tablets.
3Productivity
If immediate release profile is achieved, then bioavailability is improved, but coating requirements become more stringent to prevent premature release
Solution Approach 1:
The patent optimizes the coating parameters including polymer composition (PVA-based), coating thickness, and formulation ingredients to create a coating system that permits immediate release of the active ingredient while maintaining adequate barrier function. This parameter optimization achieves rapid drug release (at least 75% within 45 minutes) without requiring overly complex multi-layer coating structures, thus resolving the contradiction between immediate release and coating 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 formulation achieves an immediate release profile with at least 75% of the active drug released within 45 minutes and maintains high stability, with improved tablet integrity and reduced defects.
Implementation Method 1
the coating is an aqueous moisture barrier coating, wherein the coating comprises polyvinyl alcohol (PVA)
Data Source
Figure 1A
Figure 1B
Figure 2(A)~2(B)
AI summary
The present disclosure is directed to oral tablet of ribociclib including its salt(s). One embodiment of the present disclosure is directed to tablet of ribociclib with high drug load with an immediate release profile. One embodiment of the present disclosure is directed to coated tablet of ribociclib. Another embodiment of the present disclosure is directed to coated tablet of ribociclib where the coating is an advanced moisture barrier coating (e.g., Opadry® amb II coating where the coating is PVA based).