Levonorgestrel Transdermal Patch Stabilization
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Solution Overview
Problem
Existing transdermal delivery systems for levonorgestrel face challenges in stability due to components like polyacrylate pressure sensitive adhesive and PVP humectant, which contribute to degradation, necessitating the development of a composition that stabilizes levonorgestrel without concomitant estrogen delivery.
Innovation Solution
A polymeric matrix composition incorporating a skin permeation enhancer and an antioxidant like BHT, which forms a biologically acceptable adhesive polymer matrix, stabilizes levonorgestrel, preventing degradation and increasing shelf life, and is formulated without estrogen, using a polymer pressure-sensitive adhesive as a carrier with suitable polymers and humectants like PVP/VA.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polyacrylate pressure sensitive adhesive and PVP humectant are used in the transdermal delivery system, then adhesion and humectant properties are improved, but levonorgestrel stability deteriorates due to degradation
Solution Approach 1:
The patent introduces an ester wax intermediary substance that mediates between the adhesive/humectant components and levonorgestrel. This ester wax forms a protective interface that prevents direct interaction between levonorgestrel and degrading components (polyacrylate PSA and PVP), thereby maintaining stability while preserving adhesion and humectant functions.
Solution Approach 2:
The patent creates a composite adhesive matrix composition combining polyacrylate pressure sensitive adhesive, PVP humectant, ester wax, and levonorgestrel. This composite structure leverages the beneficial properties of each component while mitigating their adverse effects through proper formulation and interaction within the matrix system.
2Productivity
If conventional transdermal delivery composition is used, then transdermal delivery capability is achieved, but shelf life is reduced due to levonorgestrel degradation
Solution Approach 1:
The patent applies preliminary protective action by incorporating ester wax and antioxidants into the composition before use. These substances preemptively prevent oxidation and degradation of levonorgestrel during storage, extending shelf life while maintaining the transdermal delivery capability when applied.
Solution Approach 2:
The patent converts potentially harmful oxidative degradation into a beneficial stabilized state by incorporating antioxidants and ester wax. These substances transform the degradation-prone environment into a protective matrix that actually enhances levonorgestrel stability while preserving delivery function.
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 effectively stabilizes levonorgestrel, maintaining its potency and extending shelf life by incorporating antioxidants, while ensuring effective transdermal delivery without estrogen, as demonstrated by improved stability and permeation results.
Implementation Method 1
the anti-oxidant in the composition includes BHT... improving the stability of levonorgestrel in a levonorgestrel transdermal delivery composition
Implementation Method 2
a skin permeation enhancer... The skin permeation enhancer can present in a concentration based on weight of the composition of 1% to 50%
Data Source
AI summary
A composition for transdermal delivery of a progestin for progestin hormone therapy is disclosed. Also disclosed is a transdermal delivery device comprising the composition. For progestin-only hormone therapy, the composition contains an anti-oxidant and does not contain an estrogen. For therapy involving a progestin and an estrogen, the composition contains the progestin, the estrogen and an additional anti-oxidant. Methods of improving the stability of progestin-containing compositions comprising oxidative agents are also disclosed. The methods comprise including one or more anti-oxidants in the compositions.