Sugar-Drug Complexes for ED Therapeutics Solubility
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Solution Overview
Problem
Poorly water-soluble erectile dysfunction (ED) drugs, such as sildenafil and tadalafil, face challenges with delayed onset and variable bioavailability due to low water solubility, leading to inconsistent clinical effects and commercial viability issues.
Innovation Solution
Formation of water-soluble complexes by combining poorly soluble ED drugs with non-nutritive sugars like diterpene di-glycosides or stevioside, enhancing solubility through hydrogen bonding and host-guest chemistry, allowing for improved oral delivery and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If poorly water-soluble ED drugs are used, then the drug structure and potency are maintained, but water solubility is insufficient leading to delayed onset and poor bioavailability
Solution Approach 1:
The patent uses cyclodextrins as intermediary molecules that form inclusion complexes with ED drugs. The cyclodextrin host molecule has a hydrophilic exterior and hydrophobic interior cavity, allowing it to encapsulate the hydrophobic drug molecule while presenting a water-soluble exterior surface, thereby mediating between the insoluble drug and aqueous biological fluids to improve bioavailability
Solution Approach 2:
The patent creates composite materials by combining cyclodextrin molecules with ED drug molecules to form inclusion complexes. This composite structure combines the water-soluble properties of cyclodextrin with the pharmacologically active drug molecule, resulting in a composite material that maintains drug potency while gaining improved solubility and bioavailability
2Productivity
If poorly water-soluble ED drugs are administered, then the active pharmaceutical ingredient is delivered, but absorption into blood circulation is insufficient
Solution Approach 1:
Cyclodextrins serve as a mediator that facilitates the absorption process by forming soluble complexes with the drug, enabling the hydrophobic drug to be transported through aqueous gastrointestinal fluids and absorbed into the bloodstream more efficiently
Solution Approach 2:
The patent changes the physical-chemical parameters of the drug delivery system by modifying the solubility characteristics through complexation. The inclusion complex has different solubility parameters than the free drug, allowing it to dissolve and absorb at rates consistent with highly soluble compounds
3Reliability
If conventional ED drug formulations are used, then the drug is administered, but clinical effects are inconsistent due to variable bioavailability
Solution Approach 1:
The cyclodextrin intermediary provides a consistent and reliable dissolution and absorption mechanism, eliminating the variability associated with poorly soluble drugs. This leads to reproducible plasma concentration profiles and consistent clinical effects across different subjects and dosing conditions
Data Source
AI summary
A method is disclosed for improving the solubility of a poorly soluble drug compound such as by mixing the poorly water-soluble drug compound (such as alprostadil, sildenafil, tadalafil, vardenafil, avanafil, or a pharmaceutically acceptable salt of any thereof) with a non-nutritive sugar such as rubusoside, rebaudioside A, dulcoside B, dodecyl-β-D-maltoside (DDM), or stevioside, or any combination thereof in the presence of a pharmaceutically acceptable solvent such as ethanol and then removing the solvent to creating a water-soluble drug-sugar complex.