Oral Testosterone Undecanoate Composition for Stable Plasma Levels

Solution Overview

Problem

Existing oral testosterone formulations experience high peak plasma concentrations and significant fluctuations, leading to potential side effects and inefficiencies in maintaining stable androgen levels.

Innovation Solution

A pharmaceutical composition comprising testosterone C2-C13 alkyl esters, specifically testosterone undecanoate, formulated with a hydrophilic carrier like polyoxylated castor oil and a lipophilic carrier such as monoglycerides, along with a solidifying agent like high molecular weight polyethylene glycol, to provide a delayed release mechanism, reducing peak plasma concentrations and stabilizing androgen levels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate release oral dosage form is used, then rapid absorption and high plasma concentration is achieved, but peak plasma concentration becomes too high and fluctuation increases

Engineering Contradiction:

Improveabsorption speedVSAvoidplasma concentration stability

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The dosage form is segmented into multiple functional components: immediate release portion (30-70% of testosterone alkyl ester) for rapid absorption, and delayed release portion (20-70% of testosterone alkyl ester) for sustained release. This segmentation allows the formulation to achieve both rapid onset and sustained plasma concentrations, reducing fluctuation while maintaining effective levels.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The formulation dynamically releases testosterone alkyl ester over time through the combination of immediate and delayed release mechanisms. The dynamic release profile adapts to maintain therapeutic levels by providing initial rapid absorption followed by sustained release, thereby stabilizing plasma concentration and reducing peak fluctuations.

Inventive Principle:

Principle #15Dynamics

2Stability of the object's composition

If delayed release oral dosage form is used, then plasma concentration stability is improved, but absorption speed is reduced

Engineering Contradiction:

Improveplasma concentration stabilityVSAvoidabsorption speed

Core Design Contradiction:

Stability of the object's compositionVSSpeed

Solution Approach 1:

The dosage form is segmented into multiple functional components: immediate release portion (30-70% of testosterone alkyl ester) for rapid absorption, and delayed release portion (20-70% of testosterone alkyl ester) for sustained release. This segmentation allows the formulation to achieve both rapid onset and sustained plasma concentrations, reducing fluctuation while maintaining effective levels.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The immediate release portion provides preliminary action by rapidly absorbing testosterone alkyl ester into the system first, establishing initial therapeutic levels. This preliminary rapid absorption is followed by the delayed release portion that maintains stable concentrations, thus achieving both speed and stability through staged release.

Inventive Principle:

Principle #10Preliminary action

3Productivity

If immediate release oral dosage form is used, then rapid therapeutic effect is achieved, but fluctuation index increases

Engineering Contradiction:

Improvetherapeutic effect onsetVSAvoidfluctuation index

Core Design Contradiction:

ProductivityVSStability of the object's composition

Solution Approach 1:

The dosage form is segmented into multiple functional components: immediate release portion (30-70% of testosterone alkyl ester) for rapid absorption, and delayed release portion (20-70% of testosterone alkyl ester) for sustained release. This segmentation allows the formulation to achieve both rapid onset and sustained plasma concentrations, reducing fluctuation while maintaining effective levels.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The formulation ensures continuity of useful action by combining immediate release (providing rapid initial therapeutic effect) with delayed release (providing sustained maintenance). This continuous release mechanism eliminates the peaks and valleys associated with immediate release alone, maintaining steady therapeutic levels and reducing fluctuation index while preserving rapid onset benefits.

Inventive Principle:

Principle #20Continuity of useful action

Data Source

PatentEP3078368B1Steroidal compositions

Publication Date: 2026.05.06 LIPOCINE INC

Figure 1
Figure 2
Figure 3~4

AI summary

Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.