Complexing Agent Salt Formulations for Low-Osmolality Drug Delivery
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Solution Overview
Problem
Pharmaceutical compounds with basic nitrogen atoms face challenges in formulation due to physico-chemical properties such as basic amines, limited solubility, and hydrophobicity, which hinder their widespread use as pharmaceutical agents, particularly in subcutaneous, sublingual, and intranasal administrations.
Innovation Solution
Formulations using complexing agents like cyclodextrins with acidic functional groups to create salts with pharmaceutical compounds, eliminating excess ions and enhancing solubility, stability, and bioavailability, especially for sublingual and intranasal delivery.
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 increasing osmolality
Solution Approach 1:
The patent extracts and removes the unwanted alkali metal counterions from the complexing agent salts, using only the essential acidic functional groups to form 1:1 salts with the pharmaceutical compound. This eliminates excess ions while maintaining the beneficial solubility and stability properties.
Solution Approach 2:
The patent changes the ionic composition parameters by transitioning from traditional alkali metal salt formulations to custom 1:1 salt formulations where the complexing agent's acidic groups are paired exclusively with the pharmaceutical compound's basic nitrogen atoms, eliminating excess ions.
2Reliability
If pharmaceutical compounds with basic nitrogen atoms are used, then therapeutic activity is achieved, but solubility and bioavailability are limited
Solution Approach 1:
The patent changes the physical-chemical parameters of the pharmaceutical compound by forming salt complexes with complexing agents that have acidic functional groups. This ionic interaction significantly improves solubility and bioavailability while preserving the compound's therapeutic activity.
Solution Approach 2:
The complexing agent acts as an intermediary substance that bridges the pharmaceutical compound and the formulation medium. The acidic functional groups of the complexing agent interact with the basic nitrogen atoms of the pharmaceutical compound to create soluble salt complexes that enhance bioavailability.
3Productivity
If complexing agents with multiple acidic functional groups are used, then multiple pharmaceutical compounds can be associated with one complexing agent, but formulation complexity increases
Solution Approach 1:
The complexing agents with multiple acidic functional groups serve multiple functions: they can associate with multiple different pharmaceutical compounds, provide solubility enhancement, and maintain stability. This multi-functionality increases productivity without proportionally increasing formulation complexity.
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 enhance solubility and stability, reduce osmolality, and increase bioavailability of pharmaceutical compounds, allowing for effective subcutaneous, sublingual, and intranasal administrations without the need for additional buffers or excipients.
Implementation Method 1
the resulting salts have multiple molecules of protonated pharmaceutical compounds ionically associated with a single complexing agent
Implementation Method 2
Such an approach can be used with any pharmaceutical compound or potential pharmaceutical compound to form a salt with such a complexing agent which can provide numerous advantages in a variety of formulations, including subcutaneous, sublingual, and intranasal formulations
Implementation Method 3
In some instances, the salts and pharmaceutical compositions can be stored as powders for long term storage, thus increasing stability of such salts and compositions
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.