HCA Salt Liquid Capsule Delivery for Bioavailability
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Solution Overview
Problem
Current delivery methods for (−)-hydroxycitric acid (HCA) such as capsules and tablets are ineffective in providing adequate dispersion and bioavailability, leading to poor satiety and weight loss results due to issues like lactone formation, binding with other ingredients, and poor solubility, which are not adequately addressed by existing formulations.
Innovation Solution
A novel delivery system using soft gelatin or liquid-filled hard shell capsules comprising a water-glycerol solution with a high concentration of HCA salt, which is pre-solubilized to ensure stability and complete distribution in the gastrointestinal system, avoiding lactonization and binding agents, and allowing for compact dosage forms.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If HCA salts are coated with fats and placed in large capsules, then the HCA can be delivered orally, but the dispersion and bioavailability in the gut remains inadequate
Solution Approach 1:
The patent changes the physical state of HCA from solid salt to solubilized form in a liquid vehicle containing surfactants and co-solvents. This parameter change enables complete dispersion and rapid dissolution in the gastrointestinal tract, resolving the bioavailability issue while maintaining oral delivery capability
Solution Approach 2:
The patent introduces surfactants and co-solvents as intermediary substances that facilitate the solubilization of HCA salts in the liquid vehicle. These intermediaries enable complete dispersion of HCA in the gut by reducing surface tension and improving solubility, thereby enhancing bioavailability without requiring large capsule sizes
2Device complexity
If HCA is delivered in tablet or ordinary capsule form, then the formulation is simple, but dispersion in the gut is poor
Solution Approach 1:
The patent creates a composite liquid vehicle system combining surfactants, co-solvents, and HCA salts in specific ratios. This composite formulation achieves complete dispersion and rapid dissolution in the gastrointestinal tract, significantly improving dispersion quality while maintaining reasonable formulation simplicity through standardized ingredient combinations
3Ease of operation
If beverage deliveries are used for HCA, then the compound can be consumed easily, but active ingredient amounts are low and lactone formation occurs
Solution Approach 1:
The patent performs preliminary solubilization of HCA salts in the liquid vehicle containing surfactants and co-solvents before administration. This preliminary action ensures complete dissolution and stability of the active ingredient, preventing lactone formation and ensuring adequate dosing strength while maintaining ease of consumption through liquid or soft capsule delivery
Solution Approach 2:
The patent uses surfactants and co-solvents as intermediaries that stabilize HCA in the liquid formulation, preventing lactone formation and ensuring adequate concentration of active ingredient. These intermediaries enable the beverage or soft capsule to deliver sufficient active HCA while remaining easy to consume
4Ease of manufacture
If free acid or lactone forms of HCA are used, then the compound can be formulated, but chelating properties cause zinc loss and safety issues
Solution Approach 1:
The patent changes the chemical form of HCA from free acid or lactone to stable salt forms (potassium, sodium, calcium, magnesium hydroxycitrate) in the liquid vehicle. This parameter change eliminates the harmful chelating properties and zinc loss associated with free acid and lactone forms while maintaining formulation capability and therapeutic efficacy
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 proposed delivery system effectively provides rapid and complete bioavailability of HCA, enhancing satiety and weight loss efficacy by maintaining stability and avoiding the limitations of existing formulations, with HCA salts like potassium-magnesium being effective at dosages of 1-5 grams per day.
Implementation Method 1
a liquid formulation comprising, consisting essentially of, or consisting only of a salt of hydroxycitric acid (HCA), water and glycerol in ratio amounts such that the HCA salt is completely dissolved in the water and glycerol
Implementation Method 2
HCA salts are insoluble or virtually insoluble in glycerin, which makes the formulation of the present invention an unexpected discovery over the prior art
Data Source
AI summary
A capsule oral delivery system is disclosed. The system includes an outer capsule completely enclosing an inner content, or a hard shell comprised of hydroxypropyl methylcellulose (HPMC) enclosing the content. A liquid formulation forming the inner content of the outer capsule is comprised of a hydroxycitric acid (HCA) salt, water, and glycerol, with the HCA being completely dissolved in the water and glycerol which may be the only components present in the capsule, which may be administered to a patient in a method of treatment to cause weight loss when repeatedly administered.