Progesterone Receptor Modulator Vaginal Ring Sustained Release
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Solution Overview
Problem
There is a need for long-acting, sustained-release contraceptive methods that are easy to use and require minimal medical guidance, particularly in resource-limited settings, as existing methods often necessitate frequent administration and have side effects associated with estrogen use.
Innovation Solution
A vaginal ring or transdermal composition containing the progesterone receptor modulator CDB-2914, which provides a sustained release of the drug through a silicone elastomer matrix, allowing for effective contraception and therapeutic benefits without daily attention and minimizing hepatic first-pass effect, side effects, and menstrual bleeding.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If oral contraceptives are used, then contraception is achieved, but frequent administration is required and medical guidance is needed
Solution Approach 1:
The contraceptive system is segmented into a reservoir containing the progesterone receptor modulator and a release mechanism in the form of a vaginal ring. This segmentation allows the drug to be stored in a controlled manner and released gradually over an extended period, eliminating the need for frequent administration while maintaining contraceptive efficacy.
Solution Approach 2:
The vaginal ring is pre-loaded with a sufficient quantity of progesterone receptor modulator before insertion. This preliminary action ensures that the contraceptive agent is already prepared and will be released automatically over time without requiring repeated user intervention or medical guidance for re-administration.
2Ease of operation
If sustained-release formulations are used, then administration frequency is reduced, but device complexity increases
Solution Approach 1:
A vaginal ring acts as an intermediary device between the user and the contraceptive effect. The ring contains and controls the release of the progesterone receptor modulator, simplifying the user's role to mere insertion and removal while the intermediary handles the complex task of sustained drug delivery through its matrix structure and diffusion mechanism.
Solution Approach 2:
The vaginal ring utilizes a flexible elastomeric matrix that can be inserted into the vaginal cavity. This thin, flexible structure provides a large surface area for drug diffusion while maintaining structural integrity, achieving sustained release without requiring complex mechanical or electronic components.
3Reliability
If progesterone receptor modulators are administered, then contraceptive effect is achieved, but side effects occur
Solution Approach 1:
The invention changes the administration parameters by using a sustained-release formulation that delivers the progesterone receptor modulator at controlled, lower rates over an extended period. This parameter change reduces peak plasma concentrations and associated side effects while maintaining effective contraceptive levels through consistent delivery, thereby improving the reliability-to-side-effect ratio.
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 sustained-release composition offers continuous, user-controlled contraception with reduced side effects and menstrual bleeding, direct absorption avoiding hepatic first-pass effect, and effectiveness in various therapeutic indications, including endometriosis and breast cancer treatment.
Implementation Method 1
the ring is configured such that the PRM e.g., CDB-2914, diffuses through at least one layer of a polymeric material comprising a silicone elastomer to reach the external environment (e.g., the vaginal mucosa)
Data Source
AI summary
Disclosed are sustained release compositions for vaginal or transdermal administration that contain a progesterone receptor modulator such as CDB-2914 (also referred to as VA-2914), and methods of using them for long term contraception or therapeutic purposes. Also disclosed are methods for making the compositions.