Stable Selenium Pharmaceutical Composition via Dichlorocarboxylic Acid Complexation

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Solution Overview

Problem

Existing pharmaceutical compositions for topical treatment of skin diseases face instability and selenium precipitation during storage, leading to decreased effectiveness and increased side effects due to chemical incompatibility and uncontrollable selenium concentration.

Innovation Solution

A method involving the interaction between alpha, alpha-dichlorocarboxylic acid stabilized by nitric acid and selenious acid, with the use of dimethylsulfoxide as an adjuvant, to create a stable selenium-comprising pharmaceutical composition that prevents selenium precipitation and maintains high selenium levels during long-term storage.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If selenium is added to pharmaceutical composition for topical treatment, then therapeutic effectiveness is improved, but selenium precipitation occurs during storage

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidselenium stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces alpha,alpha-dichlorocarboxylic acid as an intermediary substance that forms a stable complex with selenium. This complex acts as a mediator that prevents selenium precipitation while maintaining therapeutic effectiveness. The dichlorocarboxylic acid stabilizes selenium in solution through chemical complexation, allowing long-term storage without precipitation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical state of selenium from elemental or ionic form to a stabilized complex form with dichlorocarboxylic acid. This parameter change in selenium's chemical environment transforms it from a precipitating state to a stable, soluble complex that maintains therapeutic activity while preventing precipitation during storage.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If selenium concentration is increased to enhance therapeutic effect, then treatment effectiveness is improved, but chemical incompatibility and precipitation increase

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidchemical incompatibility
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The dichlorocarboxylic acid serves as a protective intermediary that enables high selenium concentrations to be maintained without chemical incompatibility. The acid forms stable complexes with selenium, acting as a buffer that prevents unwanted chemical reactions even at elevated selenium levels, thus allowing enhanced therapeutic effect without increased harmful effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite pharmaceutical composition where selenium is combined with dichlorocarboxylic acid in a stable complex. This composite structure allows high selenium content to be maintained while the dichlorocarboxylic acid component prevents chemical incompatibility and precipitation, enabling both high effectiveness and stability.

Inventive Principle:
Principle #40Composite materials

3Ease of manufacture

If conventional pharmaceutical compositions are used, then ease of manufacture is maintained, but storage stability and selenium control are compromised

Engineering Contradiction:
Improvemanufacturing simplicityVSAvoidselenium concentration control
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent modifies the manufacturing process by incorporating dichlorocarboxylic acid as a stabilizing agent. This parameter change in the formulation enables precise control of selenium concentration through stable complex formation. The acid-selenium complex has predictable stability characteristics that allow precise dosing and concentration control during manufacturing, while maintaining ease of production.

Inventive Principle:
Principle #35Parameter changes

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 method ensures the stability and effectiveness of the pharmaceutical composition, allowing for controlled selenium content and prolonged storage without precipitation, thereby enhancing therapeutic efficacy and safety.

Implementation Method 1

alpha, alpha-dichlorocarboxylic acid stabilized by nitric acid

Methodology Applied
Scientific EffectChemical stabilization:

Implementation Method 2

the interaction between alpha, alpha-dichlorocarboxylic acid stabilized by nitric acid and selenious acid

Methodology Applied
Scientific EffectChemical reaction: Chemical Bonding

Implementation Method 3

prevents selenium precipitation during a long-time storage dosage form

Methodology Applied
Scientific EffectPrecipitation prevention: Precipitation

Data Source

PatentUS9446068B2Method of production of the stable selenium-comprising pharmaceutical composition with a high selenium level
Publication Date: 2016.09.20 FONBET LLC

AI summary

The present disclosure relates to the new method of producing of the stable selenium-comprising pharmaceutical compositions with a high selenium level based on the mixing of nitric acid with therapeutically effective amounts of at least two active ingredients selected from the groups consisting of 2,2-dichlorocarboxylic acids, selenium-containing compound. As a selenium-containing compound the aqueous solution of selenious acid in the amount of no more than 20%, preferably 0.5-10.0%, is used. The group of 2,2-dichlorocarboxylic acids consists 2,2-dichloropropionic acid and their homologes The chemical process is carried out by adding of the concentrated nitric acid in amount of 1.0-5.0% into 2,2-dichlorocarboxylic acid purity of at least 98.5% and completing the redox-interaction under the isothermal conditions at a temperature not higher than 70° C., preferably at 20-30° C., and then an aqueous solution of the selenious acid in an amount of not more than 20.0% (and the other components if it is necessary) is added to form the result pharmaceutical product solution. The product can also contain additional 5-20% of dimethylsulfoxide. The claimed pharmaceutical product is useful for the treating of benign, viral, premalignant, and malignant non-metastasizing skin lesions, of dysplastic lesions of visible mucous coats, fungous and other skin diseases.