Uncoated Tablet with Coating Layer for Disintegration and Photostability
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Solution Overview
Problem
Existing tablets comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (Compound (I)) or its salt lack excellent disintegration ability, storage stability, and photostability.
Innovation Solution
A tablet formulation comprising Compound (I) or its salt, lactose, corn starch, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, and magnesium stearate, with a coating layer containing a colorant like iron oxide, to enhance disintegration, storage, and photostability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a tablet formulation is designed to improve disintegration ability, then disintegration performance is improved, but storage stability and photostability may deteriorate
Solution Approach 1:
The patent divides the tablet into distinct functional layers: a core layer containing the active ingredient and disintegrant for disintegration ability, and a coating layer containing colorant and stabilizing agents for storage and photostability. This segmentation allows each layer to optimize its specific function without compromising the other properties.
Solution Approach 2:
The tablet uses a composite formulation combining multiple materials with complementary properties: low-substituted hydroxypropyl cellulose provides both disintegration capability and stability, while the coating layer incorporates colorants and stabilizing agents that enhance photostability without affecting the core's disintegration performance.
2Stability of the object's composition
If excipients and coatings are added to improve storage and photostability, then stability is improved, but disintegration ability may worsen
Solution Approach 1:
The patent applies different properties to different parts of the tablet: the core layer has high disintegration ability with minimal stabilizing agents, while the coating layer has high stability and photostability. The coating is applied locally on the surface, allowing the core to disintegrate effectively while the coating provides protective functions.
Solution Approach 2:
The patent carefully controls the substitution degree of hydroxypropyl groups in the cellulose derivative (low-substituted, 1.5-3.0 moles per anhydroglucose unit) to balance disintegration and stability. The coating layer parameters are also optimized to provide protection without creating a barrier that would prevent disintegration.
3Stability of the object's composition
If a coating layer with colorant is applied to enhance photostability, then photostability is improved, but device complexity increases
Solution Approach 1:
The coating layer serves multiple functions simultaneously: it provides photostability through colorant inclusion, offers a barrier against moisture and oxygen for enhanced storage stability, and maintains a smooth surface for controlled disintegration. This multi-functionality reduces the need for separate components for each function.
Data Source
Figure 1
AI summary
This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability. The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet.