High-Concentration Ibrutinib Tablet Formulation
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Solution Overview
Problem
Current pharmaceutical compositions of Ibrutinib require multiple capsules or tablets daily, making them inconvenient for patients and lacking a formulation with more than 90% w/w Ibrutinib, which affects ease of swallowing and patient compliance.
Innovation Solution
A tablet composition comprising more than 90% w/w Ibrutinib and minimal pharmaceutically acceptable excipients, optimized for better dissolution and bioavailability, with a process involving blending, granulation, and compression to create a stable and easily manufacturable form.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If multiple capsules or tablets are administered daily to achieve therapeutic dose, then the required Ibrutinib dosage can be met, but patient compliance and convenience deteriorate
Solution Approach 1:
The patent combines multiple daily doses of Ibrutinib into a single high-concentration tablet formulation containing more than 90% w/w of the active ingredient. This merging approach allows the total daily therapeutic dose to be administered in one tablet rather than multiple capsules or tablets, thereby improving patient compliance and convenience while maintaining the required dosage quantity.
2Weight of stationary object
If high concentration of Ibrutinib (>90% w/w) is formulated in tablet, then tablet size and weight are reduced improving swallowability, but formulation stability and manufacturability may deteriorate
Solution Approach 1:
The patent employs parameter changes by optimizing the concentration of Ibrutinib to more than 90% w/w and carefully selecting and quantifying specific excipients (microcrystalline cellulose 5-15% w/w, croscarmellose sodium 2-5% w/w, magnesium stearate 0.5-2% w/w). This parameter optimization ensures the tablet maintains high concentration while preserving formulation stability, manufacturability, and desired dissolution characteristics.
3Ease of operation
If high concentration of Ibrutinib (>90% w/w) is formulated in tablet, then patient compliance improves, but dissolution performance may deteriorate
Solution Approach 1:
The patent uses excipients as intermediary substances to facilitate dissolution of high-concentration Ibrutinib. Specifically, microcrystalline cellulose (5-15% w/w) acts as a filler and disintegrant, croscarmellose sodium (2-5% w/w) serves as a superdisintegrant, and magnesium stearate (0.5-2% w/w) functions as a lubricant. These intermediaries enable the high-concentration formulation to maintain comparable dissolution performance to marketed formulations while improving patient compliance.
Data Source
AI summary
The present invention relates to pharmaceutical compositions comprising Ibrutinib. More particularly, the present invention relates to a tablet composition comprising Ibrutinib and one or more pharmaceutically acceptable excipients and process for preparing such compositions.