Soluble Aspirin Composition with Effervescent Dissolution
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Solution Overview
Problem
Existing soluble aspirin products face issues with stability, residue formation, and slow dissolution rates, especially in cold water, limiting their effectiveness and ease of use.
Innovation Solution
A soluble aspirin composition comprising granules of aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin, and surfactant, mixed with crystalline particles of acid and heat-treated bicarbonate salt, which react to produce an effervescing action and rapid disintegration, ensuring complete dissolution in water without residue.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If soluble salts (sodium, potassium, calcium, magnesium) are used to create soluble aspirin products, then aqueous solubility is improved, but stability deteriorates due to water of crystallization causing degradation into salicylic and acetic acids
Solution Approach 1:
The patent removes water of crystallization from the salt structure by using anhydrous conditions and processing methods that prevent hydration. This extraction of the harmful water component allows the use of soluble salts without the degradation problem that normally accompanies their use.
Solution Approach 2:
The patent performs preliminary dehydration of the bicarbonate salt before combining it with aspirin. By pre-treating the salt to remove water of crystallization and maintaining anhydrous conditions during formulation, the stability issue is addressed before the final product is assembled.
2Object-affected harmful factors
If buffering coatings are applied to neutralize gastric acidity, then gastric irritation is reduced, but the coatings are ineffective in preventing aspirin particles from adhering to gastrointestinal mucosa
Solution Approach 1:
The patent removes the need for buffering coatings entirely by using a chemically different approach - an effervescent system that converts aspirin to a soluble salt form in situ. This extraction of the coating requirement eliminates the inadequacy of current protective methods.
Solution Approach 2:
The patent changes the chemical state of aspirin from acidic solid particles to a soluble salt form through effervescent reaction. By changing the pH and chemical form parameters, the medication becomes non-irritating without requiring physical coatings.
3Object-affected harmful factors
If enteric coatings are used to protect aspirin, then gastric acidity is avoided, but the same mucosal adhesion problems occur in the intestinal locus
Solution Approach 1:
The patent changes the chemical form of aspirin to a soluble salt through effervescent reaction, which occurs in both gastric and intestinal environments. This parameter change eliminates the need for location-specific coatings and prevents mucosal adhesion throughout the gastrointestinal tract.
4Ease of operation
If soluble aspirin products are designed for rapid dissolution, then ease of use is improved, but residue formation increases and dissolution completeness decreases
Solution Approach 1:
The patent utilizes phase transition in the form of effervescent reaction, where solid aspirin and bicarbonate react to produce carbon dioxide gas and soluble salt. This phase change mechanism ensures complete dissolution by converting all solid components into soluble or gaseous forms, eliminating residue while maintaining rapid dissolution.
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 rapid and complete dissolution in less than 60 seconds in aqueous media, providing effective aspirin treatment with improved taste and ease of use, and is stable against moisture degradation.
Implementation Method 1
undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt to effect effervescing action
Implementation Method 2
granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant
Implementation Method 3
heat-treated bicarbonate salt
Data Source
AI summary
A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation so that the composition rapidly dissolves in the water without occurrence of undissolved residue. The composition is solublizable within 30 seconds in cool to cold water to provide an effervescent analgesic solution that can be readily orally administered to an individual in need of analgesia.