Curcumin Liquid Formulation with Surfactant-Phospholipid Complexes
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Solution Overview
Problem
Current pharmaceutical compositions of curcumin face challenges with poor absorption and rapid elimination due to low solubility, high first-pass metabolism, and gastric irritation from high surfactant concentrations, necessitating a stable liquid formulation with higher curcumin concentration without pH buffers or molecular aggregation inhibitors.
Innovation Solution
A stable liquid pharmaceutical composition comprising curcumin, surfactant, solvent, and oil with a surfactant concentration not exceeding 60% w/w, specifically formulated without pH buffers and molecular aggregation inhibitors, using a process involving dispersion, mixing, and heating to achieve a curcumin concentration of 2 to 20% w/w, with a surfactant to solvent ratio of 0.83 to 10 and surfactant to curcumin ratio of 3 to 15, utilizing oils like fractionated coconut oil and surfactants like cremophor.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If curcumin is formulated with high surfactant concentration to improve solubility and absorption, then bioavailability is improved, but gastric irritation and mucosal damage occur
Solution Approach 1:
The patent changes the concentration parameter of surfactant from high (previous formulations) to controlled levels (0.5-10% w/v), and introduces a novel combination with phospholipids (0.1-5% w/v) to achieve enhanced solubility and absorption without the harmful effects of high surfactant concentrations alone
Solution Approach 2:
The patent creates a composite formulation combining surfactants with phospholipids in specific ratios, where the phospholipid component mitigates the gastric irritation caused by surfactants while maintaining or enhancing the solubility and absorption benefits
2Quantity of substance
If curcumin concentration is increased in pharmaceutical compositions to improve therapeutic efficacy, then treatment effectiveness is improved, but solubility and stability decrease
Solution Approach 1:
The patent optimizes the concentration parameters of multiple components including curcumin (0.1-20% w/v), surfactant (0.5-10% w/v), and phospholipid (0.1-5% w/v) to achieve a balanced formulation that maintains high curcumin concentration while ensuring solubility and stability
Solution Approach 2:
The patent introduces phospholipids as intermediary substances that facilitate the incorporation and stabilization of high concentrations of curcumin in the formulation, acting as a bridge between the hydrophobic curcumin and the aqueous environment
3Stability of the object's composition
If pH buffer and molecular aggregation inhibitors are used to stabilize curcumin in solution, then stability is improved, but formulation complexity and potential adverse effects increase
Solution Approach 1:
The patent removes pH buffers and molecular aggregation inhibitors from the formulation, achieving stability through a simplified system based on surfactant-phospholipid complexes that naturally stabilize curcumin without requiring these additional components
Solution Approach 2:
The formulation achieves self-stabilization through the surfactant-phospholipid-curcumin complex system, which inherently maintains solution stability without requiring external pH buffers or aggregation inhibitors
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 demonstrates improved bioavailability and stability, with particle sizes below 100 nm, enhanced absorption, and reduced gastric irritation, as evidenced by bioavailability studies in rats and pharmacokinetic studies in humans, showing increased plasma levels and prolonged stability over six months.
Implementation Method 1
The said formulation comprises curcumin or pharmaceutically acceptable salts or derivatives thereof, surfactant, solvent, and oil wherein the concentration of surfactant is not more than 60% w/w
Implementation Method 2
The said formulation comprises curcumin or pharmaceutically acceptable salts or derivatives thereof, surfactant, solvent, and oil
Implementation Method 3
using a process involving dispersion, mixing, and heating to achieve a curcumin concentration of 2 to 20% w/w
Data Source
Figure 1
AI summary
The present invention relates to stable liquid pharmaceutical compositions of curcumin or its pharmaceutically acceptable salts or its derivatives with higher curcumin concentration and improved bioavailability without the use of buffer and/or molecular aggregation inhibitor(s). In accordance with present invention the curcumin is in the solubilized form to make a stable liquid pharmaceutical composition.