Micronized Progesterone Formulation Using Type II Safflower Oil

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Solution Overview

Problem

Current pharmaceutical formulations of micronized progesterone suffer from allergenic reactions due to the use of peanut oil and soy lecithin, which are poorly tolerated by some individuals, leading to hypersensitivity reactions and reduced bioavailability of progesterone.

Innovation Solution

A pharmaceutical composition comprising micronized progesterone suspended in type II safflower oil, which is allergen-free and rich in unsaturated fatty acids, providing improved bioavailability and stability without the use of soy lecithin, and can be administered orally or vaginally.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If peanut oil is used as the oily base in micronized progesterone formulation, then the progesterone can be effectively delivered, but significant allergenic reactions and hypersensitivity occur

Engineering Contradiction:
Improveprogesterone delivery effectivenessVSAvoidallergenic reactions
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical composition parameter of the oily base from peanut oil to type II safflower oil. This substitution maintains the essential function of solubilizing and delivering micronized progesterone while eliminating the allergenic properties associated with peanut oil, thus resolving the contradiction between effective delivery and allergenicity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent replaces a commonly used but problematic oil (peanut oil) with an alternative oil (type II safflower oil) that achieves the same functional purpose without the harmful side effects. This substitution allows the formulation to be discarded of its allergenic component while retaining therapeutic effectiveness

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

2Stability of the object's composition

If soy lecithin is added to the formulation, then the dispersion quality of micronized progesterone is improved, but significant allergenic reactions and hypersensitivity occur

Engineering Contradiction:
Improvedispersion quality of micronized progesteroneVSAvoidhypersensitivity reactions
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and removes soy lecithin from the formulation entirely. By eliminating this allergenic component, the formulation maintains its ability to disperse micronized progesterone effectively (through the oily base alone) while removing the source of hypersensitivity reactions, thus resolving the contradiction between dispersion quality and allergenicity

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent converts the potential harm of requiring additional excipients (like soy lecithin) for dispersion into a benefit by demonstrating that the type II safflower oil base alone is sufficient to provide excellent dispersion quality of micronized progesterone, thereby eliminating the need for allergenic additives

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Ease of operation

If oral administration route is used, then the treatment is convenient, but progesterone is poorly absorbed and plasma half-life is short

Engineering Contradiction:
Improveadministration convenienceVSAvoidabsorption efficiency and plasma half-life
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent changes the physical state and formulation parameters of progesterone by using micronized particles suspended in type II safflower oil. This formulation modification enhances the solubility and absorption characteristics of progesterone, allowing oral administration to achieve adequate plasma concentrations and extended half-life, thus resolving the contradiction between administration convenience and absorption efficiency

Inventive Principle:
Principle #35Parameter changes

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 use of type II safflower oil in the formulation enhances the stability and bioavailability of progesterone, reducing the risk of allergic reactions and maintaining physiological progesterone levels for extended periods, thus effectively treating conditions related to progesterone insufficiency.

Implementation Method 1

A pharmaceutical composition comprising micronized progesterone suspended in type II safflower oil

Methodology Applied
Scientific EffectSuspension: Suspension

Data Source

PatentEP2269592B1Pharmaceutical composition of micronised progesterone and its use
Publication Date: 2013.08.07 EFFIK SA
  • EP2269592B1 patent drawingFigure 1

AI summary

The present invention relates to a pharmaceutical composition containing micronized progesterone and at least one high-oleic safflower oil, referred to as type II safflower oil. It also relates to medicinal products comprising said pharmaceutical composition. The invention further relates to the medical uses of this pharmaceutical composition.