Amorphous Biopharmaceutical Powder for Transmucosal Delivery
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Solution Overview
Problem
Current transmucosal drug delivery systems, particularly for intranasal administration, face challenges such as limited drug load, rapid clearance, and chemical instability of biologic active ingredients, leading to inefficiencies in absorption and stability, which affects the efficacy and safety of treatments.
Innovation Solution
Development of a solid, amorphous, mono-particulate powder composition combining a biopharmaceutical drug compound with a disaccharide and polymeric carrier material, optimized through spray-drying, to enhance physical and chemical stability and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If peroral drug administration is used, then patient compliance is improved, but drug bioavailability deteriorates due to hepatic first-pass metabolism and enzymatic degradation
Solution Approach 1:
The patent introduces an oral mucosal adhesive composition as an intermediary system that allows drugs to be administered perorally while adhering to the oral mucosa. This enables the drug to be absorbed through the mucosal membrane directly into systemic circulation, bypassing hepatic first-pass metabolism and gastrointestinal enzymatic degradation, thus maintaining high bioavailability while preserving patient compliance
Solution Approach 2:
The invention changes the physical and chemical parameters of the drug delivery system by using adhesive materials that allow the drug to remain in contact with the oral mucosa for extended periods. This parameter change (from rapid passage through GI tract to sustained mucosal contact) enables efficient absorption while avoiding metabolic degradation pathways
2Ease of operation
If peroral drug delivery is used, then administration convenience is improved, but absorption time deteriorates due to the digestive process
Solution Approach 1:
The oral mucosal adhesive composition serves as an intermediary that enables direct absorption through the mucosal membrane, bypassing the slow digestive absorption process. The adhesive nature ensures prolonged contact time with the absorption surface, achieving rapid and efficient drug uptake while maintaining peroral administration convenience
3Reliability
If high doses of active ingredients are used to compensate for low bioavailability, then therapeutic effect is improved, but side effects and safety issues worsen
Solution Approach 1:
The adhesive oral mucosal composition acts as an intermediary delivery system that dramatically improves bioavailability by enabling direct mucosal absorption. This allows therapeutic doses to be reduced by factors of 10-100 times while maintaining equivalent therapeutic effects, thereby minimizing side effects and safety concerns associated with high-dose peroral administration
4Reliability
If transmucosal administration is used, then drug bioavailability is improved, but the amount of active ingredient that can be administered deteriorates due to limited mucosal surface area and fluid volume
Solution Approach 1:
The invention changes key parameters of the transmucosal delivery system by using adhesive materials that extend the residence time of the drug on the mucosal surface. This parameter change compensates for the limited surface area and fluid volume, enabling significantly higher amounts of active ingredient to be administered and absorbed through the mucosa
5Object-affected harmful factors
If rapid clearance mechanisms in oral and nasal cavities are present, then mucosal surface is maintained clean, but absorption time deteriorates
Solution Approach 1:
The adhesive composition serves as an intermediary that overcomes the rapid clearance mechanisms by strongly adhering to the mucosal surface. This adhesive property counteracts the clearance forces, maintaining prolonged contact between the drug and absorption site, thereby enabling sufficient absorption time despite the inherently rapid clearance environment
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 composition provides improved stability, bioavailability, and rapid absorption of biologic active ingredients, enabling effective and safe transmucosal delivery with enhanced pharmacological effects and prolonged shelf-life.
Implementation Method 1
optimized through spray-drying
Implementation Method 2
solid, amorphous, mono-particulate powder composition
Data Source
AI summary
According to the invention, there is provided a which composition is in the form of an amorphous, mono-particulate powder comprising a mixture of: (a) a pharmacologically-effective dosage amount of at least one biopharmaceutical drug compound; and (b) a pharmaceutically-acceptable carrier material, which carrier material comprises a combination of a disaccharide and a polymeric material. Preferred pharmaceutically-acceptable carriers in this regard include lactose or trehalose and dextrins (e.g. maltodextrins). Compositions may further comprise one or more alkyl saccharides. Preferred alkyl saccharides include sucrose esters, such as sucrose monolaurate. Powder compositions may be produced by spray-drying the various components together in combination.