Amorphous Celecoxib Liquid Formulation for Rapid Pain Relief
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Solution Overview
Problem
Celecoxib, a hydrophobic and highly permeable drug, experiences limited bioavailability due to its poor solubility and delayed absorption when administered orally, leading to delayed onset of action, which is inadequate for acute pain conditions requiring immediate relief.
Innovation Solution
Development of stable oral liquid pharmaceutical compositions comprising celecoxib, solubilizers, medium chain glycerides, polar solvents, and pharmaceutically acceptable excipients that prevent precipitation in simulated gastric fluid, enhancing solubilization and absorption for faster pain relief.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If celecoxib is administered orally in conventional formulations, then the drug can be delivered to the gastrointestinal tract, but the poor solubility leads to delayed absorption and limited bioavailability
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using amorphous celecoxib instead of crystalline form, and by formulating it in an oil-based liquid composition with specific solubilizers. This transforms the drug from a poorly soluble crystalline solid to a soluble amorphous state in a liquid medium, dramatically improving both absorption speed and bioavailability
Solution Approach 2:
The patent creates a composite liquid formulation combining celecoxib with multiple components including medium-chain triglycerides, long-chain triglycerides, solubilizers (such as polysorbates), and other excipients. This composite system works synergistically to maintain celecoxib in a soluble state and facilitate rapid absorption in the gastrointestinal tract
2Loss of time
If celecoxib is formulated for rapid absorption, then pain relief onset can be accelerated, but formulation stability and prevention of precipitation become challenging
Solution Approach 1:
The patent performs preliminary action by formulating celecoxib in an oil-based liquid composition before administration, where the drug is pre-dissolved and stabilized in the gastrointestinal-friendly medium. This preliminary preparation ensures that upon oral administration, the drug is already in a state ready for rapid absorption without needing to dissolve further in the GI tract, thus achieving fast onset while maintaining stability
Solution Approach 2:
The patent uses solubilizers such as polysorbates and lipid vehicles as intermediaries between celecoxib and the aqueous gastrointestinal environment. These intermediaries emulsify and stabilize the hydrophobic celecoxib in the oil-based formulation, preventing precipitation upon contact with gastric fluids while enabling rapid release and absorption
3Reliability
If conventional celecoxib formulations are used, then the dosage can be standardized, but the high variability in absorption leads to inconsistent therapeutic效果
Solution Approach 1:
The patent changes the formulation parameters from conventional solid dosage forms to an oil-based liquid formulation with amorphous celecoxib. This parameter change eliminates the dissolution variability inherent in solid formulations, providing consistent and predictable absorption profiles, thereby improving both reliability and therapeutic effectiveness
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 compositions provide rapid absorption and increased bioavailability of celecoxib, achieving significant pain relief within 2 hours in a higher percentage of subjects compared to conventional formulations, with improved pharmacokinetic parameters and reduced dosing requirements.
Implementation Method 1
comprising a therapeutically effective amount of celecoxib, at least one solubiliser, at least one medium chain glyceride, at least one polar solvent
Implementation Method 2
stable oral liquid pharmaceutical compositions... does not show any precipitation in Fasted-State Simulated Gastric Fluid
Implementation Method 3
can be readily dissolved/dispersed for rapid absorption in the gastrointestinal tract
Implementation Method 4
Celecoxib is a hydrophobic and highly permeable drug
Data Source
AI summary
The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.