Ribociclib Immediate Release Tablets Using Cellulose Derivative Coatings
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Solution Overview
Problem
Current pharmaceutical compositions of Ribociclib, particularly those coated with polyvinyl alcohol (PVA), do not offer sufficient alternatives for immediate release formulations with comparable or better dissolution properties, content uniformity, stability, and bioavailability compared to commercialized dosage forms.
Innovation Solution
Development of an immediate release tablet composition using Ribociclib coated with a coating composition comprising one or more cellulose derivatives, such as hydroxypropyl methylcellulose and ethyl cellulose, which is free of polyvinyl alcohol, to enhance dissolution and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Ribociclib is coated with polyvinyl alcohol (PVA) based coating composition, then the tablet has protective coating, but the dissolution properties and bioavailability are limited
Solution Approach 1:
The patent changes the chemical composition parameters of the coating material from polyvinyl alcohol to cellulose derivatives (hydroxypropyl cellulose, hydroxyethyl cellulose, methyl cellulose, ethyl cellulose). This parameter change in the coating material's molecular structure and solubility characteristics directly improves dissolution properties and enhances bioavailability while maintaining the protective function of the coating.
Solution Approach 2:
The patent uses composite coating formulations comprising cellulose derivatives combined with other excipients such as titanium dioxide, talc, and various polymers. These composite materials provide both protective functions and improved dissolution characteristics, resolving the contradiction between coating protection and bioavailability.
2Reliability
If immediate release formulation is developed with cellulose derivatives coating, then dissolution and bioavailability are improved, but formulation development complexity increases
Solution Approach 1:
The patent segments the formulation development into distinct components: core tablet composition (Ribociclib with excipients like microcrystalline cellulose, mannitol, starch) and separate coating composition (cellulose derivatives with functional excipients). This segmentation allows independent optimization of each component, simplifying the overall development process despite the improved bioavailability requirements.
Solution Approach 2:
The cellulose derivative coating serves multiple functions simultaneously: it provides protective barrier function, enhances dissolution properties, improves bioavailability, and enables immediate release characteristics. This multi-functionality reduces the need for additional separate formulations or processes, thereby managing development complexity.
3Ease of manufacture
If PVA-based coating is used for Ribociclib tablets, then manufacturing process is established, but alternative formulations with better dissolution properties are lacking
Solution Approach 1:
The patent employs cellulose derivatives which are readily available, cost-effective materials that can be processed using standard pharmaceutical coating equipment. The coating formulation uses common excipients and follows conventional coating processes, making it economically viable and manufacturable while achieving superior dissolution properties compared to PVA-based coatings.
Data Source
AI summary
The present invention relates to pharmaceutical compositions comprising a kinase inhibitor. More particularly, the present invention relates to immediate release pharmaceutical compositions comprising Ribociclib or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients and process for preparing such compositions.