Oil-in-Water JAK Inhibitor Formulation for Stable Skin Permeation
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Solution Overview
Problem
There is a need for stable, easily applied topical formulations of JAK inhibitors with good skin permeation characteristics for the treatment of skin disorders.
Innovation Solution
A pharmaceutical formulation comprising an oil-in-water emulsion with a therapeutically effective amount of (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile or its pharmaceutically acceptable salt, which includes components like water, oil, emulsifier, and occlusive agents, designed for improved skin permeation and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing topical formulations are used, then they can be applied to skin, but they lack stability and efficient skin penetration
Solution Approach 1:
The patent changes the formulation parameters by using an oil-in-water emulsion system with specific oil phases (mineral oil, medium chain triglycerides), emulsifiers (polysorbate 80, glyceryl monostearate), and stabilizers (xanthan gum, carbomer). These parameter changes result in improved formulation stability while maintaining effective skin penetration of the JAK inhibitor
Solution Approach 2:
The patent creates a composite topical formulation combining hydrophobic oil phases with hydrophilic aqueous phases, stabilized by emulsifiers and thickeners. This composite structure allows the formulation to maintain stability while enabling controlled delivery and penetration of the hydrophobic JAK inhibitor through the skin
2Stability of the object's composition
If topical formulation stability is improved, then storage and shelf life are enhanced, but skin permeation characteristics may be compromised
Solution Approach 1:
The patent segments the formulation into distinct oil and water phases that are stabilized as an emulsion. The oil phase contains the JAK inhibitor and hydrophobic components, while the aqueous phase contains hydrophilic stabilizers. This segmentation allows each phase to maintain its stability characteristics while the overall formulation enables skin penetration
Solution Approach 2:
The patent uses emulsifiers (polysorbate 80, glyceryl monostearate) as intermediary substances that bridge the hydrophobic oil phase and hydrophilic aqueous phase. These intermediaries stabilize the emulsion structure while also facilitating the penetration of the JAK inhibitor through the skin by creating a controlled delivery system
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 formulation demonstrates better appearance, spreadability, and stability, with enhanced skin permeation compared to anhydrous formulations, maintaining consistent permeation profiles and ease of manufacture.
Implementation Method 1
The oil-in-water formulation demonstrates improved stability and skin permeation, with increased cumulative amounts across human cadaver and mouse skin
Data Source
AI summary
This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.