Solubilized Estradiol–Progesterone Formulations for Uniform Absorption

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Solution Overview

Problem

Current hormone replacement therapies lack FDA-approved formulations of bio-identical estradiol and progesterone combinations, leading to inconsistent absorption and significant patient variability, necessitating higher dosages to compensate for incomplete absorption, which can result in undesirable side effects.

Innovation Solution

Development of pharmaceutical formulations combining solubilized estradiol and micronized or partially solubilized progesterone in single or separate unit doses, packaged in a 28-day regimen to enhance absorption consistency and reduce variability, using oils and surfactants to improve bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional hormone replacement formulations are used, then hormone replacement is achieved, but absorption is inconsistent and patient variability is significant

Engineering Contradiction:

Improveabsorption consistencyVSAvoidpatient variability

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the physical and chemical properties of the hormone formulations. Specifically, it uses solubilized estradiol and micronized progesterone with controlled particle sizes, adjusts pH levels, and optimizes excipient ratios to achieve consistent absorption across different patients, thereby reducing patient variability in response to the therapy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by combining solubilized estradiol with micronized progesterone in a unified formulation system. This composite approach allows for synergistic effects and consistent absorption patterns, as the combined formulation is designed to release and absorb hormones in a controlled manner that reduces individual patient variability

Inventive Principle:

Principle #40Composite materials

2Reliability

If higher dosages are used to compensate for incomplete absorption, then absorption adequacy is improved, but undesirable side effects increase

Engineering Contradiction:

Improveabsorption adequacyVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the absorption parameters of the formulation by using solubilized estradiol and micronized progesterone, which improve bioavailability and absorption efficiency. This allows for lower effective dosages that achieve adequate hormone replacement without the need to compensate with higher doses, thereby reducing side effects

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces intermediary substances (excipients, solubilizing agents, and micronization particles) that act as mediators to enhance the absorption of estradiol and progesterone. These intermediaries facilitate more efficient uptake by the body, allowing adequate hormone replacement at lower dosages and minimizing harmful side effects

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If bio-identical estradiol and progesterone combinations are formulated, then absorption consistency is improved, but FDA approval status remains limited

Engineering Contradiction:

Improveabsorption consistencyVSAvoidregulatory approval

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies preliminary action by conducting extensive preclinical and clinical studies before seeking FDA approval. The formulation undergoes thorough testing for absorption consistency, safety, and efficacy, with preliminary data demonstrating improved absorption and reduced variability, thereby strengthening the case for regulatory approval

Inventive Principle:

Principle #10Preliminary action

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 formulations provide more uniform dissolution and reduced intra- and inter-patient variability, allowing for lower effective dosages with minimized side effects and improved compliance through targeted delivery.

Implementation Method 1

pharmaceutical formulations of solubilized estradiol and micronized and/or partially or completely solubilized progesterone

Methodology Applied

Scientific EffectSolubilization: Solvation

Implementation Method 2

micronized and/or partially or completely solubilized progesterone

Methodology Applied

Scientific EffectMicronization:

Data Source

PatentUS20250325561A1Natural Combination Hormone Replacement Formulations and Therapies

Publication Date: 2025.10.23 THERAPEUTICSMD INC

AI summary

Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.