Treprostinil Derivative Compounds for Noninvasive Transdermal Delivery
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Solution Overview
Problem
Current treatments for pulmonary hypertension (PH) and pulmonary arterial hypertension (PAH) using treprostinil require invasive administration methods like intravenous or intramuscular routes, causing discomfort and local trauma, and there is a need for improved formulations that enhance systemic availability and bioavailability through oral or transdermal delivery.
Innovation Solution
Development of treprostinil derivatives represented by Formulae I, II, III, and IV, which include compounds and compositions for transdermal delivery, allowing for controlled drug release and tailored chemical structures for specific therapeutic applications, including compositions for transdermal patches.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If treprostinil is administered via intravenous or intramuscular routes, then therapeutic effect is achieved, but patient discomfort and local trauma increase
Solution Approach 1:
The patent employs transdermal delivery systems as an intermediary between the drug and the patient's body, allowing treprostinil to bypass invasive routes while maintaining therapeutic effectiveness. The transdermal patch acts as a mediator that delivers the drug through the skin without requiring intravenous or intramuscular injection.
Solution Approach 2:
The invention replaces the mechanical injection system (needles, syringes) with a non-invasive transdermal delivery system. This substitution eliminates the mechanical trauma associated with injections while preserving the drug's therapeutic action through controlled permeation through the skin.
2Ease of operation
If treprostinil is administered orally, then non-invasive delivery is achieved, but systemic availability is insufficient
Solution Approach 1:
The transdermal delivery system serves as an intermediary that overcomes the limitations of oral administration. It provides a direct pathway for the drug to enter the systemic circulation bypassing first-pass metabolism and absorption issues, thereby achieving both non-invasive delivery and adequate systemic availability.
Solution Approach 2:
The invention changes the delivery parameters by using controlled-release mechanisms in transdermal patches, maintaining steady drug levels and improving systemic availability compared to oral administration. The controlled permeation rate and sustained release profile optimize bioavailability while maintaining non-invasive delivery.
3Ease of operation
If transdermal delivery system is developed for treprostinil, then patient comfort improves, but device complexity increases
Solution Approach 1:
The transdermal delivery system is segmented into functional layers (drug reservoir, rate-controlling membrane, adhesive layer, protective backing) that can be independently optimized. This segmentation allows complex functionality to be achieved through simple, well-defined components, managing overall system complexity while maintaining patient comfort.
Solution Approach 2:
The transdermal patch design incorporates multiple functions into a single device: drug storage, controlled release, skin adhesion, and protection. This multi-functionality reduces the need for multiple separate components, managing device complexity while providing comprehensive patient comfort and therapeutic efficacy.
Data Source
AI summary
Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.