Oral Naproxen Formulation with Soluble Carbonates
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Solution Overview
Problem
Current oral formulations of therapeutic compounds, particularly acids, bases, and amphoteric drugs, face challenges in achieving rapid and enhanced dissolution and absorption due to limitations in pH modulation and solubility, leading to suboptimal bioavailability and absorption rates.
Innovation Solution
Incorporating an appropriate amount of soluble carbonates, such as sodium bicarbonate, into therapeutic formulations to neutralize hydrochloric acid and facilitate rapid dissolution, with optimized levels ensuring enhanced absorption without significantly increasing pH, thereby improving the bioavailability of therapeutic compounds.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional oral formulations are used, then the formulation maintains stable pH and composition, but dissolution rate and absorption rate are slow
Solution Approach 1:
The patent applies parameter changes by incorporating pH-modulating agents (acids or bases) that temporarily alter the pH environment in the gastrointestinal tract to enhance dissolution rate. The pH is changed from neutral to acidic or alkaline conditions to improve drug solubility and dissolution kinetics, then returns to normal physiological pH after the dissolution process completes.
Solution Approach 2:
The formulation performs preliminary action by pre-incorporating pH-modulating agents and effervescent couples into the tablet structure before administration. These agents are positioned to immediately affect the local pH environment upon contact with gastric fluids, creating optimal dissolution conditions before the drug needs to be absorbed.
2Speed
If effervescent couples in large amounts are used, then dissolution rate increases, but formulation complexity and manufacturing difficulty increase
Solution Approach 1:
The patent applies partial action by using effervescent couples and pH-modulating agents in optimized, sub-stoichiometric amounts that provide sufficient pH modification for enhanced dissolution without requiring large excesses. This reduces the total amount of reactive components needed while achieving the desired dissolution effect.
Solution Approach 2:
The pH-modulating agents serve multiple functions: they modify pH to enhance dissolution, provide effervescent action for disintegration, and potentially enhance drug solubility through salt formation. This multi-functionality reduces the need for separate excipients and simplifies the overall formulation.
3Speed
If pH is significantly increased to enhance dissolution, then absorption rate improves, but gastric toxicity increases
Solution Approach 1:
The patent applies local quality by creating localized pH modification only at the site of drug dissolution in the gastrointestinal tract. The pH-modulating agents are incorporated into the tablet matrix and release pH changes specifically where the drug needs to dissolve, rather than systematically altering pH throughout the entire gastrointestinal system, thereby minimizing gastric toxicity.
Solution Approach 2:
The formulation converts the potentially harmful effect of pH modification into a beneficial effect by using controlled, temporary pH changes that enhance dissolution and absorption. The pH is modified only to the extent needed for dissolution enhancement, then returns to normal physiological levels, converting what could be a toxic effect into a therapeutic benefit.
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 use of soluble carbonates in oral formulations results in rapid and reproducible absorption of therapeutic compounds, achieving at least 20% dissolution within 180 seconds and up to 90% within 300 seconds, enhancing the bioavailability and absorption rates of drugs with limited solubility.
Implementation Method 1
Incorporating an appropriate amount of soluble carbonates, such as sodium bicarbonate, into therapeutic formulations to neutralize hydrochloric acid
Implementation Method 2
The use of sodium bicarbonate and other alkali metal carbonates, as the base component of an effervescent couple in dosage forms intended for dissolution or dispersion in water prior to administration
Data Source
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AI summary
The present application provides an oral delivery system for Naproxen or a pharmaceutically acceptable salt thereof. The present application particularly provides a swallow formulation comprising Naproxen or a pharmaceutically acceptable salt thereof which facilitates the rapid delivery of the therapeutic compound to the circulatory system.