Popcorn Polyacrylates as Tablet Disintegrants
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Solution Overview
Problem
Current disintegrants for pharmaceutical tablets, such as crospovidone and starch derivatives, are either expensive or have inadequate disintegrating effects, and are unsuitable for hydrolysis-sensitive active ingredients due to high pH values or rapid gelation, which affects the disintegration time of tablets.
Innovation Solution
The use of water-insoluble, low-swelling polyacrylates as disintegrants, specifically popcorn polymers derived from acrylic or methacrylic acid, which have a gelation time greater than 30 seconds and are produced through spontaneous radical polymerization in the absence of oxygen, providing a cost-effective and effective disintegration without affecting hydrolysis-sensitive ingredients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If cross-linked polyvinylpyrrolidone (crospovidone) is used as disintegrant, then disintegrant effect is excellent, but cost is high
Solution Approach 1:
The patent replaces expensive crospovidone with a cheaper alternative - cross-linked polyacrylic acid popcorn polymer. This polymer provides comparable disintegrant effect through a different mechanism (lower swelling capacity but sufficient disintegration performance) while significantly reducing formulation cost.
2Speed
If rapidly gelling crosslinked polyacrylates are used as disintegrants, then gelation time is short (30 seconds or less), but disintegration time of tablets is adversely affected
Solution Approach 1:
The patent modifies the gelation time parameter of crosslinked polyacrylates by selecting specific polymers with gelation times greater than 30 seconds. This parameter change ensures that the polymer does not gelate too rapidly, allowing sufficient time for the tablet to disintegrate properly while still providing effective disintegration performance.
3Reliability
If Polacrilin resins (cross-linked polyacrylic acid) are used as disintegrants, then swelling behavior provides disintegrant effect, but pH values are relatively high making them unsuitable for hydrolysis-sensitive active ingredients
Solution Approach 1:
The patent applies local quality by using cross-linked polyacrylic acid popcorn polymer with specific structural characteristics that provide disintegrant effect through controlled swelling and breakdown, while maintaining a lower pH compared to conventional Polacrilin resins. The popcorn polymer structure allows localized water absorption and swelling that drives disintegration without requiring high pH values.
4Quantity of substance
If water-soluble polymers are used as disintegrants, then swelling capacity is high, but they may cause rapid gelation affecting disintegration time
Solution Approach 1:
The patent uses cross-linked polyacrylic acid popcorn polymer which exhibits localized water absorption characteristics. The polymer structure allows water to penetrate and swell specific regions (the popcorn-like structure) without causing rapid overall gelation. This localized swelling provides sufficient disintegrant effect while maintaining appropriate disintegration time.
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
These polyacrylates offer a better disintegrating effect than conventional products, with improved stability for hydrolysis-sensitive active ingredients and enhanced disintegration performance compared to rapidly gelling crosslinked polyacrylates, while maintaining a lower pH, thus providing a more effective and cost-efficient solution for tablet disintegration.
Implementation Method 1
spontaneous radical polymerization in the absence of oxygen
Implementation Method 2
water-insoluble, low-swelling polyacrylates as disintegrants
Data Source
AI summary
The invention relates to the use of pulverulent, cross-linked, water-insoluble, low-swelling polyacrylates as disintegrants for pharmaceutical solid dosage forms.