Docetaxel Amorphous Solid Dispersion for Oral Bioavailability
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Solution Overview
Problem
Docetaxel, a poorly soluble drug, has low bioavailability due to limited absorption in the body, hindering its pharmacological effect when administered orally.
Innovation Solution
A pharmaceutical composition comprising docetaxel or its pharmaceutically acceptable salt combined with polyvinyl pyrrolidone-based, cellulose-based, poloxamer-based, polyethylene glycol-based, alginic acid-based, and polygamma glutamic acid compounds, along with sodium dodecyl sulfate, is prepared to enhance solubility and stability in the body.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If docetaxel is administered orally, then the drug can be taken without injection, but the bioavailability is low due to poor solubility and absorption
Solution Approach 1:
The patent changes the physical state of docetaxel from crystalline to amorphous form, which fundamentally alters its solubility and absorption characteristics. This parameter change enables the drug to achieve sufficient bioavailability for oral administration while maintaining the ease of oral dosing.
Solution Approach 2:
The patent creates a composite formulation by combining amorphous docetaxel with specific excipients and carriers to form a stable amorphous solid dispersion. This composite structure enhances solubility and absorption while maintaining oral administrability.
2Reliability
If docetaxel is formulated to improve solubility, then bioavailability increases, but the drug may crystallize in the body reducing stability
Solution Approach 1:
The patent performs preliminary action by pre-formulating docetaxel as a stable amorphous solid dispersion with appropriate excipients before administration. This preliminary stabilization prevents crystallization from occurring in the body, maintaining both solubility and stability simultaneously.
Solution Approach 2:
The patent introduces intermediary substances (excipients and carriers) that act as stabilizing agents within the amorphous formulation. These intermediaries prevent crystallization by maintaining the amorphous state and enhancing solubility, thus resolving the contradiction between bioavailability and stability.
3Productivity
If polymeric materials are used to improve solubility, then dissolution enhances, but the pharmacological effect is not sufficiently achieved
Solution Approach 1:
The patent optimizes the physical state parameter of the drug formulation by creating a stable amorphous form with controlled crystal structure. This parameter change enables sufficient dissolution while ensuring the pharmacological effect is achieved through proper formulation composition and stability.
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 significantly improves docetaxel's bioavailability by delaying crystallization and minimizing the effects of body fluids, achieving a desired pharmacological effect.
Implementation Method 1
preparing a first dissolved product by dissolving one or more compounds selected from among a polyvinyl pyrrolidone-based compound, a cellulose-based compound, a poloxamer-based compound, a polyethylene glycol-based compound, an alginic acid-based compound, polygamma glutamic acid and sodium dodecyl sulfate
Implementation Method 2
capable of stably delivering a drug to the intestine by slowing the crystallization of the drug in the body
Implementation Method 3
a method of granulating a crystalline drug into an amorphous drug using a poorly soluble drug, an ionic or non-ionic polymer, a surfactant, or the like
Data Source
AI summary
The present invention relates to a pharmaceutical composition containing docetaxel or a pharmaceutically acceptable salt thereof and a method for preparing the same, which can improve the low body absorption rate of docetaxel.