Etonogestrel Injectable Formulation for Contraception
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Solution Overview
Problem
There is a need for a contraceptive method that provides secure, flexible, and accessible contraception over multiple months without the burdensome surgical implantation and removal, suitable for use in developing countries with varying climates, and scalable manufacturing methods.
Innovation Solution
An injectable formulation of etonogestrel using a triblock copolymer and diblock copolymer with DMSO as a solvent, forming a depot that provides sustained release of etonogestrel for up to 120 days, allowing for easy administration and biodegradability, reducing the need for surgical removal and enabling stable storage and transportation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If solid rod implants are used to provide long-duration contraception, then the duration of action is extended, but the ease of operation deteriorates due to surgical implantation and removal requirements
Solution Approach 1:
The patent employs a biodegradable polymer matrix that naturally degrades over time, eliminating the need for surgical removal. The implant is designed to be disposed of naturally by the body through biodegradation, transforming the permanent rod concept into a temporary, self-resolving system that provides contraception for 3-5 months without requiring explantation surgery.
Solution Approach 2:
The patent changes the physical state from solid rod to injectable formulation, and modifies the polymer properties to be biodegradable. This parameter change allows the implant to be administered via injection rather than surgery, and to dissolve naturally in the body, thereby improving ease of operation while maintaining adequate duration of action.
2Duration of action of moving object
If solid rod implants are used for contraception, then the duration of action is extended, but the device complexity increases due to requirement for specially trained doctors or nurses for implant removal
Solution Approach 1:
The biodegradable polymer matrix performs the function of self-removal through natural degradation processes. The implant serves itself by gradually dissolving and being absorbed by the body, eliminating the need for professional intervention for removal. This self-service mechanism reduces device complexity by removing the requirement for specially trained personnel for explantation.
3Duration of action of moving object
If non-biodegradable rod implants are used, then the duration of action is extended, but the loss of substance increases due to need for surgical removal
Solution Approach 1:
The patent employs a biodegradable polymer that is safely discarded by the body through natural degradation and metabolic processes. The implant material is designed to be recovered by the body's natural functions (enzymatic breakdown, cellular uptake), transforming the waste disposal problem into a beneficial biological process that eliminates harmful substance loss.
4Reliability
If contraceptive formulation is designed for stable storage and transportation, then the reliability is improved, but the ease of manufacture deteriorates due to manufacturing complexity
Solution Approach 1:
The patent formulates the contraceptive as an injectable solution with optimized pH, osmolality, and sterility. These parameter changes enable the formulation to be stable during storage and transportation while maintaining compatibility with standard manufacturing processes. The liquid formulation is more amenable to scalable manufacturing compared to solid rod fabrication.
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 formulation offers a flexible and effective contraceptive solution with controlled release of etonogestrel, facilitating easier administration, eliminating the need for surgical implant removal, and ensuring stability and scalability for global access.
Implementation Method 1
The formulation provides sustained release of etonogestrel through a triblock copolymer and diblock copolymer matrix, utilizing diffusion of the drug through the polymer network
Implementation Method 2
The copolymer matrix is designed to be biodegradable, allowing natural breakdown and dissolution in the body to release etonogestrel over the contraceptive period
Implementation Method 3
The formulation uses a water-miscible, pharmaceutically acceptable organic solvent comprising DMSO to dissolve the triblock copolymer, diblock copolymer, and etonogestrel, creating a homogeneous solution
Data Source
AI summary
The present invention generally relates to an injectable formulation for sustained release of etonogestrel, a pharmaceutical dosage and an application device comprising such formulation, methods for preparing thereof, and use thereof for contraception.