Taste-Masking Coated Particles for Immediate Drug Release
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Solution Overview
Problem
Current taste-masking coatings for oral formulations fail to ensure immediate and complete release of active substances across various pH levels in the intestinal tract, leading to delayed release due to insolubility at stomach pH and permeability at higher pH levels.
Innovation Solution
Coated particles with a core containing an active substance and an acidic compound, coated with a polymer that is soluble at pH 5 or less and permeable at pH above 5, allowing for quick dissolution and release of the active substance regardless of stomach pH.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If a polymer coating soluble at stomach pH (1-3) is used for taste-masking, then the active substance is released immediately in the stomach, but the coating becomes permeable at higher pH levels (above 5) causing delayed release in the intestinal tract
Solution Approach 1:
The patent changes the pH sensitivity parameter of the polymer coating by selecting polymers with specific pKa values (above 5) and adjusting the coating composition to maintain solubility at stomach pH while ensuring complete dissolution across the entire pH range from buccal cavity to intestinal tract
Solution Approach 2:
The patent uses composite coating systems combining multiple polymers with complementary solubility profiles, including water-soluble polymers and pH-sensitive polymers, to achieve both immediate release at stomach pH and reliable dissolution at higher pH levels in the intestinal tract
2Ease of operation
If the stomach residence time is short or stomach pH is increased by antacids, then the polymer coating remains insoluble and only permeable, causing delayed active substance release
Solution Approach 1:
The patent selects polymers with specific solubility parameters that ensure dissolution at pH 5 and above, transforming the coating from pH-insoluble to pH-soluble behavior, thereby making release independent of stomach residence time and antacid effects
Solution Approach 2:
The coating is designed to preliminarily dissolve in the buccal cavity or stomach regardless of pH conditions, ensuring the active substance is released before reaching the intestinal tract, preventing any delay caused by short stomach residence time
3Object-affected harmful factors
If enteric polymer membrane with acidic compound is used to prevent dissolution in buccal cavity, then taste-masking is improved, but immediate release in stomach is prevented because polymers are insoluble at stomach pH
Solution Approach 1:
The patent inverts the pH solubility profile by selecting polymers that are soluble at low pH (stomach) and become less soluble at high pH (intestinal tract), opposite to conventional enteric polymers, enabling both taste-masking and immediate gastric release
Solution Approach 2:
The patent uses the acidic compound not as a barrier but as a catalyst that enhances polymer dissolution in the stomach, creating a synergistic effect where the acidic environment accelerates coating dissolution rather than preventing it
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
Ensures immediate and complete release of active substances, maintaining taste-masking properties and suitable for use in orodispersible tablets with pleasant palatability, independent of pH levels in the intestinal tract.
Implementation Method 1
Said polymers present a solubility profile according to which they are insoluble at the saliva pH, i.e. pH=6-8 in order to prevent the active substance from contacting the tongue when the formulation is in the buccal cavity, but they are soluble at the stomach pH, i.e. pH=1-3
Implementation Method 2
At said pH, the acidic compound which is present in the core locally creates a very acidic micro-environment, which allows the quick dissolution of the polymer film and consequently the release of the active substance from the core
Data Source
AI summary
The present invention relates to a coated particle of active substance comprising a core, said core comprising the active substance and an acidic compound, said core being coated with a taste masking coating based on a polymer which is soluble at pH of 5 or less, and which is permeable at pH above 5.