Transdermal NES-Testosterone Gel for Reversible Male Contraception
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Solution Overview
Problem
Current male contraceptive methods are limited, inconvenient, and often result in high testosterone levels or side effects, making them unsafe and irreversible.
Innovation Solution
A transdermal composition combining 16-methylene-17α-acetoxy-19-norpregn-4-ene-3,20-dione (NES) and testosterone (T) in a hydroalcoholic gel form, applied once daily, to suppress sperm production while maintaining normal testosterone levels and minimizing side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high dose testosterone is used for male contraception, then sperm production is suppressed, but testosterone levels become abnormally high and side effects increase
Solution Approach 1:
The patent combines testosterone with a progestin (16-methylene-17α-acetoxy-19-norpregn-4-ene-3,20-dione) in a fixed-ratio transdermal gel formulation. This merging of two hormonal agents allows for synergistic suppression of spermatogenesis while using lower doses of each component, thereby maintaining contraceptive efficacy while reducing androgenic side effects associated with high-dose testosterone monotherapy.
Solution Approach 2:
The patent changes the dosing parameters by using a fixed-ratio combination where testosterone is delivered at 0.5% w/w concentration in the transdermal gel, providing controlled systemic absorption. This parameter adjustment ensures testosterone levels remain within the normal physiological range (300-1000 ng/dL) while achieving sufficient suppression of gonadotropins and sperm production, avoiding the harmful effects of supraphysiological testosterone levels.
2Reliability
If testosterone alone is used for male contraception, then sperm production is suppressed, but the method is irreversible and causes harmful side effects
Solution Approach 1:
The combination of testosterone and progestin in the transdermal gel creates a reversible contraceptive mechanism. The progestin component enhances suppression of the hypothalamic-pituitary-gonadal axis while allowing for easier reversibility upon discontinuation compared to high-dose testosterone alone, addressing the irreversibility concern while maintaining contraceptive reliability.
3Ease of operation
If transdermal gel is used for male contraception, then convenience is improved, but testosterone levels may become uncontrolled
Solution Approach 1:
The patent specifies precise formulation parameters for the transdermal gel, including 0.5% w/w testosterone concentration and 0.025% w/w progestin concentration. These controlled parameters ensure consistent drug release and absorption, maintaining testosterone levels within the normal physiological range (300-1000 ng/dL) while providing the convenience of daily self-application.
Solution Approach 2:
The patent incorporates monitoring requirements where serum testosterone levels are assessed periodically to ensure they remain within the target range. This feedback mechanism allows for dose adjustments if necessary, ensuring controlled testosterone levels while maintaining the convenience of transdermal delivery.
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
Effectively suppresses gonadotropins and sperm concentration with minimal side effects, offering a safe and reversible male contraceptive option.
Implementation Method 1
a transdermal composition in a unit dose form for contraceptive treatment of males
Data Source
AI summary
The present disclosure relates to a specific combination of a progestin and testosterone in a transdermal composition and usage thereof in a method for ensuring male contraception with more efficacy and less side effects.