Sustained-Release Tablet Composition Balancing Hardness and Drug Release
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Solution Overview
Problem
Existing sustained-release solid dosage forms, such as tablets, face challenges in achieving the required hardness and friability while maintaining a desired sustained-release property, particularly when containing readily water-soluble pharmaceutical ingredients, as they often fail to meet international pharmacopeia standards for polyvinyl alcohol saponification and polymerization degrees.
Innovation Solution
A composition comprising a polyvinyl alcohol-based resin with a specific saponification degree of 78 to 96 mol% and polymerization degree of 800 or more, combined with tannic acid as a polyhydric phenol compound, is used to enhance tablet hardness and moldability, forming a hydrogel that prolongs the release of pharmaceutical ingredients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Strength
If a polyvinyl alcohol-based resin with high saponification degree (88 mol%) is used as binder, then adhesiveness of ingredients is enhanced, but tablet hardness becomes insufficient and sustained-release property cannot be achieved
Solution Approach 1:
The invention changes the polymerization degree parameter of the polyvinyl alcohol-based resin from conventional values to specifically 800 or more, while controlling saponification degree at 78-96 mol%. This parameter change transforms the resin's properties to simultaneously provide sufficient adhesiveness for tablet formation and sustained-release capability, resolving the contradiction between binding strength and release duration
Solution Approach 2:
The invention creates a composite material system by combining polyvinyl alcohol-based resin with specific excipients (crystalline cellulose, microcrystalline cellulose, and/or pregelatinized starch) in controlled ratios. This composite approach allows the resin to provide sustained-release while excipients contribute to tablet hardness and disintegration, achieving both binding and sustained-release requirements simultaneously
2Duration of action of stationary object
If polyvinyl alcohol-based resin with high polymerization degree is used to achieve sustained-release, then release time is extended, but tablet compressibility and hardness become insufficient
Solution Approach 1:
The invention formulates a composite material comprising polyvinyl alcohol-based resin (polymerization degree ≥800) combined with specific excipients in controlled ratios. The resin provides sustained-release through its high polymerization degree, while excipients like crystalline cellulose and microcrystalline cellulose contribute to tablet compressibility and hardness, resolving the contradiction between release time and mechanical strength
Solution Approach 2:
The invention applies different functional properties to different components locally: the polyvinyl alcohol-based resin with high polymerization degree is specifically positioned to provide sustained-release at the molecular level, while excipients are positioned to provide mechanical strength and compressibility at the macro level, allowing each component to optimize its local function without compromising overall tablet performance
3Ease of manufacture
If conventional polyvinyl alcohol-based resin is used for tablet binding, then tablet formation is facilitated, but sustained-release property cannot be achieved particularly for water-soluble ingredients
Solution Approach 1:
The invention changes the critical parameter of polymerization degree to 800 or more, which fundamentally alters the resin's behavior: it maintains adequate adhesiveness for tablet formation during manufacturing, but creates a matrix structure that controls drug release over extended periods. This parameter change enables the same material to fulfill both manufacturing ease and sustained-release requirements
Solution Approach 2:
The polyvinyl alcohol-based resin with polymerization degree ≥800 serves multiple functions simultaneously: it acts as a binder during tablet formation, provides structural matrix for drug incorporation, and controls sustained-release of the pharmaceutical ingredient. This multi-functionality eliminates the need for separate binder and sustained-release agents, achieving both ease of manufacture and sustained-release property
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 composition achieves a sustained-release tablet with high hardness and compressibility, effectively controlling the release of pharmaceutical ingredients, including readily water-soluble ones, by forming a three-dimensional network structure through hydrogen bonding.
Implementation Method 1
forming a three-dimensional network structure through hydrogen bonding
Implementation Method 2
can form a three-dimensional network structure in a tablet. A gel having a three-dimensional network structure can suppress the release of pharmaceutical ingredients contained in the tablet
Data Source
AI summary
The present invention discloses a composition for sustained-release solid dosage form comprising (A) a polyvinyl alcohol-based resin having an average saponification degree of 78 to 96 mol% and an average polymerization degree of 800 or more and (B) a polyhydric phenol compound, preferably tannic acid. A sustained-release tablet having an intended hardness can be produced by a method comprising mixing a granulate prepared from a composition containing (A) a polyvinyl alcohol-based resin powder and a pharmaceutical ingredient with a tannic acid powder, and compressing the mixture into a tablet.