Fluasterone Formulations with Polysorbates
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Solution Overview
Problem
Fluasterone, a compound with anti-cancer and anti-inflammatory properties, faces challenges due to its poor water solubility, leading to high oral doses required for efficacy and difficulties in topical administration, along with androgenic side effects associated with steroid treatments.
Innovation Solution
Formulations combining fluasterone with organic alcohols and polysorbates, such as Tween 80, enhance solubility and bioavailability, allowing for topical and parenteral administration with reduced androgenicity, and co-administration with glucocorticoids to mitigate side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If fluasterone is administered orally to achieve therapeutic efficacy, then anti-cancer and anti-inflammatory effects are obtained, but high doses are required due to poor water solubility and low bioavailability
Solution Approach 1:
The patent changes the physical state and solubility parameters of fluasterone by formulating it as a micronized or nanosized particle suspension in aqueous or non-aqueous vehicles. This parameter change improves bioavailability and reduces the oral dose required to achieve therapeutic efficacy.
Solution Approach 2:
The patent introduces intermediary substances such as surfactants, emulsifiers, and solubilizing agents (e.g., polysorbates, ethanol, propylene glycol) that act as mediators to enhance the solubility and absorption of fluasterone, thereby reducing the dose required for effective treatment.
2Object-affected harmful factors
If topical formulations of fluasterone are prepared to reduce androgenic side effects, then local application is achieved, but poor water solubility prevents effective formulation
Solution Approach 1:
The patent creates composite formulation systems combining fluasterone with multiple excipients including surfactants, emulsifiers, and co-solvents to achieve both good solubility and reduced androgenic side effects through localized topical application.
Solution Approach 2:
The patent employs intermediary substances such as polysorbates and organic alcohol co-solvents that mediate between the hydrophobic fluasterone and the aqueous topical formulation system, enabling effective solubilization and reducing androgenic side effects through controlled local delivery.
3Reliability
If glucocorticoids are used to treat inflammatory conditions, then anti-inflammatory effects are achieved, but androgenic side effects and skin atrophy occur
Solution Approach 1:
The patent merges fluasterone with glucocorticoids in combined topical formulations, where fluasterone provides anti-inflammatory effects with reduced androgenic side effects, while the glucocorticoid component addresses the inflammatory condition, creating a synergistic therapeutic effect.
Solution Approach 2:
The patent converts the potential harm of androgenic side effects into a benefit by using fluasterone, which has anti-androgenic properties, to counteract the androgenic side effects of glucocorticoid therapy while maintaining the desired anti-inflammatory effects.
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 improve bioavailability and reduce androgenic side effects, enabling effective topical treatment of various conditions including cancer, diabetes, and arthritis with lower doses and enhanced absorption.
Implementation Method 1
Formulations combining fluasterone with organic alcohols and polysorbates, such as Tween 80, enhance solubility and bioavailability
Data Source
AI summary
The present invention relates to formulations of poorly water soluble pharmaceutical agents of Formula I and II. The present invention also relates to compositions containing compounds of Formula I or II, and glucocorticoids, and methods for reducing side effects from glucocorticoid treatment by co-administration of compounds of Formula I and II. The compositions herein are useful for the treatment of diabetes and obesity related diseases including metabolic syndrome.