Avacopan MCT Oral Formulation for Poor Water Solubility
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Solution Overview
Problem
There is a need for a suitable formulation of avacopan that can be administered to patients, particularly those with difficulty swallowing and pediatric patients, due to its poor solubility in aqueous environments and challenges in oral delivery for poorly water-soluble drugs.
Innovation Solution
Formulations of avacopan in non-aqueous liquid medium-chain triglycerides, such as Miglyol® 812 N, Miglyol® 810 N, Witarix® 60/40 MCT, Labrafac™ Lipophile WL 1349, Captex® Medium-Chain Triglycerides, and Crodamol GTCC-PN, are developed for oral administration, enhancing solubility and suitability for pediatric patients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If avacopan is administered in traditional aqueous formulations, then it can be delivered orally, but its poor water solubility limits absorption and therapeutic efficacy
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by using non-aqueous liquid vehicles (medium-chain triglycerides, glycols, esters) instead of water-based systems. This parameter change enables avacopan to achieve adequate solubility and absorption while maintaining therapeutic efficacy, directly resolving the contradiction between aqueous solubility and therapeutic reliability
Solution Approach 2:
The patent creates composite formulations by combining avacopan with specific excipients including medium-chain triglycerides (Miglyol 812 N, 810 N), glycols (propylene glycol, polyethylene glycol), and esters. These composite material systems provide both solubility enhancement and controlled release, resolving the contradiction between solubility quantity and therapeutic efficacy
2Ease of operation
If avacopan is formulated for oral administration in liquid form, then it becomes suitable for pediatric patients and those with swallowing difficulties, but formulation complexity increases due to solubility challenges
Solution Approach 1:
The patent introduces intermediary substances (solubilizing excipients such as medium-chain triglycerides, glycols, and esters) that mediate between the poorly water-soluble avacopan and the aqueous biological environment. These intermediaries enable liquid oral formulation without requiring complex delivery devices or administration systems, thus improving ease of operation while managing formulation complexity through well-established pharmaceutical excipients
Solution Approach 2:
The patent employs conventional, readily available pharmaceutical excipients and formulation approaches that are cost-effective and well-understood in the industry. By using standard liquid oral formulation techniques with common solubilizing agents, the patent avoids complex, expensive, or novel delivery systems, making the formulation simple enough for routine pediatric administration
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 provide a stable and effective oral administration option for avacopan, suitable for patients with swallowing difficulties and pediatric patients, ensuring therapeutic efficacy and safety.
Implementation Method 1
Formulations of avacopan in non-aqueous liquid medium-chain triglycerides, such as Miglyol® 812 N, Miglyol® 810 N, Witarix® 60/40 MCT, Labrafac™ Lipophile WL 1349, Captex® Medium-Chain Triglycerides, and Crodamol GTCC-PN, are developed for oral administration, enhancing solubility
Data Source
AI summary
The disclosure provides formulations comprising avocapan and one or more medium-chain triglycerides.