Aqueous Inhalation Composition for Polypeptide Delivery
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Solution Overview
Problem
Current polypeptide and protein drugs have low bioavailability due to degradation in the stomach, poor intestinal absorption, and the first-pass effect in the liver, leading to inadequate therapeutic effects and increased toxicity when administered orally, while pulmonary delivery methods face challenges with absorption enhancers causing lung toxicity.
Innovation Solution
An aqueous inhalation pharmaceutical composition comprising a therapeutically effective amount of a polypeptide or protein, an aqueous vehicle, and an absorption enhancer such as L-α-Lysophosphatidylcholine (LPTC) or water-soluble surfactants like Tween-80, which enhances lung absorption without causing lung toxicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If absorption enhancers are used to improve drug absorption in the lung, then the bioavailability of polypeptide and protein drugs is improved, but lung toxicity increases
Solution Approach 1:
The patent changes the chemical parameters of the absorption enhancer by using L-α-lysophosphatidylcholine (LPTC) instead of conventional absorption enhancers. This parameter change allows the substance to enhance absorption while reducing toxicity. The specific chemical structure and properties of LPTC provide a safer profile while maintaining absorption-enhancing capabilities
Solution Approach 2:
The patent creates a composite inhalation formulation containing LPTC in combination with polypeptide or protein drugs. This composite material approach allows the LPTC to work synergistically with the therapeutic agent, enhancing absorption while the specific composition maintains safety. The formulation integrates multiple components (LPTC, drug, and excipients) into a unified system that achieves both efficacy and safety
2Ease of operation
If polypeptide and protein drugs are administered orally, then convenience for patients is improved, but bioavailability decreases due to degradation and poor absorption
Solution Approach 1:
The patent uses L-α-lysophosphatidylcholine (LPTC) as an intermediary substance that facilitates the absorption of polypeptide and protein drugs through pulmonary mucosa. This mediator overcomes the natural barriers to absorption (mucosal resistance, enzymatic degradation) without requiring oral administration, thus maintaining high bioavailability while providing a convenient non-invasive delivery route
3Productivity
If polypeptide and protein drugs are injected, then bioavailability is improved, but side effects and toxicity increase
Solution Approach 1:
The patent replaces the mechanical injection system with a pulmonary inhalation system. Instead of using needles and syringes to deliver the drug directly into the bloodstream (which causes tissue trauma and side effects), the invention uses the respiratory system to absorb the drug through mucosal surfaces, achieving high bioavailability through natural physiological pathways without the harmful effects of injection
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 significantly increases the bioavailability of polypeptides and proteins, reducing lung toxicity and improving therapeutic efficacy by avoiding stomach degradation and liver first-pass effects, while maintaining safety through the use of non-toxic absorption enhancers.
Implementation Method 1
an absorption enhancer selected from the group consisting of L-α-Lysophosphatidylcholine (LPTC) and derivatives thereof, and water-soluble surfactants
Data Source
AI summary
An aqueous inhalation pharmaceutical composition comprising a polypeptide or protein is provided. The composition of the present invention can improve the bioavailability of the polypeptide and protein, and avoid inducing toxicity in the lung.