Oral Hydroxyprogesterone Caproate Regimens for Preterm Birth Prevention

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Solution Overview

Problem

Current injectable forms of hydroxyprogesterone caproate (HPC) compositions have shown questionable efficacy in preventing preterm birth and do not meet the needs for an effective oral treatment form, which is preferred by patients and healthcare providers.

Innovation Solution

A novel oral HPC composition and administration method, allowing for dosing regimens starting as early as 14 weeks of gestation, with dosages ranging from 1,200 mg to 1,600 mg administered once, twice, or three times a day, to achieve therapeutically effective levels of HPC for up to 25 weeks, targeting improved neonatal outcomes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If injectable HPC compositions are used for prevention of preterm birth, then the treatment can be administered, but the efficacy is questionable and does not meet effectiveness requirements

Engineering Contradiction:
Improveefficacy in preventing preterm birthVSAvoidpatient preference for oral administration
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the physical form of HPC from injectable to oral dosage forms (tablets, capsules, softgels) and modifies the chemical structure by creating prodrug esters (HPC-S, HPC-L, HPC-V) with improved bioavailability. These parameter changes enable oral administration while achieving therapeutic effectiveness for preventing preterm birth

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses lipid-based carriers and surfactants as intermediaries to enhance the solubility and absorption of HPC in the gastrointestinal tract. These intermediaries facilitate the delivery of HPC through oral route, bridging the gap between oral administration preference and effective drug delivery

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If oral HPC compositions are developed, then patient preference and ease of administration are improved, but achieving therapeutically effective levels consistently is challenging

Engineering Contradiction:
Improveease of administrationVSAvoidconsistency in achieving therapeutically effective levels
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent develops multiple oral dosage forms (tablets, capsules, softgels) with different release mechanisms and modifies HPC into prodrug esters with enhanced bioavailability. These changes ensure consistent absorption and achievement of therapeutic levels through oral administration

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs lipid-based carriers, cyclodextrins, and surfactants as intermediaries to improve the solubility and stability of HPC in the gastrointestinal environment. These intermediaries ensure reliable and consistent absorption of HPC, achieving therapeutically effective levels through oral route

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If HPC is administered to achieve high levels of progestin, then prevention of preterm birth is improved, but the treatment duration and dosing frequency increase

Engineering Contradiction:
Improveprevention of preterm birthVSAvoidtreatment duration and dosing frequency
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent divides the treatment into structured dosing regimens with specific frequency (once daily, twice daily, or three times daily) and duration (from 14 weeks to 37 weeks of gestation). This segmentation of dosing schedule ensures sustained therapeutic levels while providing flexibility in treatment planning

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent establishes periodic dosing schedules at regular intervals (daily, twice daily, or three times daily) to maintain consistent therapeutic levels of HPC throughout the treatment period, ensuring continuous protection against preterm birth

Inventive Principle:
Principle #19Periodic action

Data Source

PatentUS12502396B2Hydroxyprogesterone caproate compositions and methods of use in preventing preterm birth
Publication Date: 2025.12.23 LIPOCINE INC

AI summary

An HPC composition and method of treatment for the prevention of PTB and improved neonatal outcomes. The invention provides for a dosing regimen beginning as early as 14 weeks of fetal gestation and dosing regimens of a duration of as much as 25 weeks. The invention provides a high level of exogeneous progestin to endogenous progesterone when it is most needed. The instant invention consistently achieves active levels of HPC which achieve effectiveness. Exemplary dosing regimens comprise an oral administration of HPC in the range of 1,200 mg to 1600 mg, wherein the HPC is administered via a once a day, twice a day, or three times a day administration.