Delayed Release Testosterone Ester Formulation for Plasma Cmax Reduction
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Solution Overview
Problem
Existing testosterone undecanoate formulations exhibit high peak plasma concentrations (Cmax) and significant fluctuations, which can lead to adverse effects and reduced therapeutic efficacy.
Innovation Solution
A delayed release oral dosage form comprising testosterone alkyl ester and a pharmaceutically acceptable carrier, designed to provide a lower Cmax and more stable plasma concentrations, thereby reducing peak levels and fluctuations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If immediate release oral dosage form is used, then rapid absorption and high plasma Cmax are achieved, but peak plasma concentrations become excessively high causing adverse effects
Solution Approach 1:
The immediate release dosage form is segmented into multiple delayed release dosage forms, each containing a portion of the total dose. This segmentation distributes the absorption event over time, preventing any single dose from producing excessively high peak concentrations while maintaining overall therapeutic efficacy.
Solution Approach 2:
The formulation employs preliminary action by using delayed release technology to postpone the absorption of testosterone alkyl ester until a later time point. This preliminary delay in absorption allows the system to avoid peak concentration problems while still delivering the therapeutic dose at an appropriate time.
2Speed
If immediate release oral dosage form is used, then rapid absorption is achieved, but plasma concentration fluctuations increase reducing therapeutic efficacy
Solution Approach 1:
By dividing the total dose into multiple delayed release units, the plasma concentration profile is segmented into multiple smaller absorption events rather than one large event. This reduces the magnitude of concentration fluctuations and improves overall stability while maintaining adequate absorption.
Solution Approach 2:
The delayed release mechanism performs preliminary action by controlling when absorption occurs, preventing premature or excessive absorption that would cause large fluctuations. The systematic delay ensures more gradual and stable plasma concentration changes.
3Object-affected harmful factors
If delayed release oral dosage form is used, then peak plasma Cmax is reduced improving safety, but absorption time is extended
Solution Approach 1:
The total absorption time is segmented across multiple delayed release doses rather than one prolonged absorption event. This allows the system to extend the overall time window for absorption while keeping each individual absorption event relatively brief, thus improving safety without excessive time loss.
Solution Approach 2:
The delayed release formulation uses preliminary action to control the timing of absorption, deliberately extending the start time to reduce peak concentrations. This time extension is managed through the segmented dose approach to prevent excessive overall absorption time.
Data Source
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. Further provided are methods of preparing steroidal testosterone ester containing compositions and products.