Abiraterone Acetate Self-Microemulsion System for Oral Bioavailability
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Solution Overview
Problem
Abiraterone acetate has low solubility and permeability, leading to low bioavailability and stability issues, particularly when administered orally, and is heavily influenced by food intake, requiring specific timing for optimal absorption.
Innovation Solution
A self-microemulsion system comprising glycerol monolinoleate, medium chain triglyceride, PEG-40 hydrogenated castor oil, and 2-(2-ethoxyethoxy)ethanol is developed to enhance solubility and stability, allowing for improved absorption and bioavailability, and can be taken with or without food.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If abiraterone acetate is administered orally as a conventional tablet, then the dosage can be easily controlled, but the oral bioavailability is very low due to low solubility and poor permeability
Solution Approach 1:
The patent uses a self-microemulsion system comprising multiple components (glycerol monolinoleate, medium chain triglyceride, PEG-40 hydrogenated castor oil, and 2-(2-ethoxyethoxy)ethanol) to form a composite preparation that enhances both solubility and permeability of abiraterone acetate, thereby improving oral bioavailability while maintaining reasonable preparation complexity
Solution Approach 2:
The patent changes the physical and chemical parameters of the drug delivery system by converting abiraterone acetate from a conventional crystalline tablet into a self-microemulsion system with specific oil phase and emulsion phase ratios, which fundamentally alters the dissolution and absorption characteristics to improve bioavailability
2Reliability
If abiraterone acetate is taken on an empty stomach to control plasma concentration, then the absorption is more predictable, but the patient compliance is reduced due to strict timing requirements
Solution Approach 1:
The self-microemulsion system changes the physicochemical parameters of the drug formulation to reduce food-effect sensitivity, allowing the drug to be taken with or without food while maintaining relatively stable plasma concentration, thereby improving dosing convenience without sacrificing reliability
3Reliability
If the dosage of abiraterone acetate is increased to compensate for low bioavailability, then the effective drug amount can be sufficient, but the side effects are increased
Solution Approach 1:
The patent changes the delivery system parameters from conventional tablet to self-microemulsion, which improves the efficiency of drug absorption and utilization. This allows achieving the same effective drug amount at lower doses, thereby reducing side effects while maintaining 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 self-microemulsion system significantly increases oral bioavailability and stability of abiraterone acetate, reducing the impact of food on absorption and allowing for flexible dosing times, while maintaining long-term storage stability.
Implementation Method 1
a self-microemulsion system for loading abiraterone acetate... comprises an oil phase and an emulsion phase... the oil phase comprises glycerol monolinoleate and medium chain triglyceride; the emulsion phase comprises PEG-40 hydrogenated castor oil and 2-(2-ethoxyethoxy)ethanol
Data Source
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AI summary
Disclosed is a self-microemulsion system for loading abiraterone acetate, and a composition and an application thereof. The self-microemulsion system for loading abiraterone acetate has excellent solubility and stability for abiraterone acetate, and the composition formed by dissolving abiraterone acetate in this system can significantly reduce the effect of food on the absorption of abiraterone acetate, and reduce the differences between preprandial administration and postprandial administration, thus making it possible to take the medicament on both an empty and a full stomach and reducing the limitation for the time of taking medicament.