Complexing Agent Drug Salts Without Excess Ion Osmolality
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Solution Overview
Problem
Pharmaceutical compounds with basic nitrogen atoms face challenges in formulation due to properties like limited solubility, hydrophobicity, and inherent ionic functional groups, leading to difficulties in widespread use, particularly in subcutaneous, sublingual, and intranasal administrations.
Innovation Solution
Formulating pharmaceutical compounds with basic nitrogen atoms as salts using complexing agents like cyclodextrins in their free acid form, creating ionically associated complexes that eliminate excess ions and enhance solubility, stability, and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional salt formulations using alkali metal salts of complexing agents are used, then solubility and stability are improved, but excess ions are introduced leading to high osmolality
Solution Approach 1:
The patent extracts and removes the harmful alkali metal ions from the formulation by using free acid forms of complexing agents that form salts with the pharmaceutical compound without introducing excess ions. This selective extraction of the harmful component (alkali metal ions) resolves the contradiction between achieving solubility/stability and avoiding high osmolality.
Solution Approach 2:
The patent converts the potentially harmful interaction between alkali metal salts and complexing agents into a beneficial formulation by using the free acid form of the complexing agent. This approach maintains the solubility and stability benefits while eliminating the harmful excess ion effect, turning a problematic traditional formulation approach into an optimized solution.
2Quantity of substance
If pharmaceutical compounds with basic nitrogen atoms are formulated as traditional salts, then solubility is improved, but hydrophobicity and ionic functional groups create formulation difficulties
Solution Approach 1:
The patent changes the chemical parameters of the formulation by using free acid forms of complexing agents instead of traditional alkali metal salts. This parameter change in the formulation approach (from ionic salt to free acid complex) resolves the formulation difficulties created by hydrophobicity and ionic functional groups while maintaining improved solubility.
3Object-generated harmful factors
If complexing agents with multiple acidic functional groups are used in free acid form, then excess ions are eliminated, but the formulation requires careful control of ion association
Solution Approach 1:
The patent applies the self-service principle by allowing the complexing agent with multiple acidic functional groups to automatically form ion associations with the pharmaceutical compound in a controlled manner. The system self-regulates the ion association process, eliminating the need for external control mechanisms while maintaining precise formulation characteristics and eliminating excess ions.
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 resulting salts improve solubility, stability, and bioavailability, allowing for effective subcutaneous, sublingual, and intranasal delivery without additional buffers, while reducing osmolality and enabling long-term storage as powders.
Implementation Method 1
creating ionically associated complexes that eliminate excess ions
Implementation Method 2
enhance solubility
Implementation Method 3
reducing osmolality
Data Source
AI summary
Provided herein are pharmaceutical formulations and pharmaceutical compound salts which utilize complexing agents as counterions. Such formulations and salts are useful for treating a variety of disease and disorders.