Semi-Solid Pharmaceutical Carrier for Dual-Solubility Bioavailability

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Solution Overview

Problem

Existing technologies face challenges in effectively dissolving and emulsifying both water-soluble and fat-soluble active substances, leading to low bioavailability and requiring high doses for therapeutic efficacy, while also lacking uniformity and high purity in semi-solid mixtures.

Innovation Solution

A pharmaceutical carrier comprising a strongly solvating aprotic solvent, such as dimethyl sulfoxide, carbonic acid amides like urea, and vegetable oils with unsaturated fatty acids, along with natural emulsifiers, is used to create a semi-solid mixture that enhances the dissolution and emulsification of both types of active substances, ensuring high homogeneity and uniformity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional carriers are used for active substances, then the formulation is simple to prepare, but the bioavailability of active substances is low and high doses are required

Engineering Contradiction:
Improvebioavailability of active substancesVSAvoiddose reduction capability
Core Design Contradiction:
Quantity of substanceVSLoss of substance

Solution Approach 1:

The patent uses a composite carrier system comprising multiple components: a glycerol derivative (first component), a surfactant (second component), and optionally a co-solvent (third component). This composite structure enables simultaneous dissolution of both water-soluble and fat-soluble active substances, significantly improving bioavailability and enabling dose reduction.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent modifies the chemical and physical parameters of the carrier system by selecting specific glycerol derivatives with particular molecular structures and properties. By changing the parameters of the carrier components (such as hydrophilic-lipophilic balance, solubility characteristics), the system achieves enhanced bioavailability and reduced dosing requirements.

Inventive Principle:
Principle #35Parameter changes

2Manufacturing precision

If separate carriers are used for water-soluble and fat-soluble active substances, then each substance can be dissolved effectively, but the formulation complexity increases and uniformity decreases

Engineering Contradiction:
Improvehomogeneity and uniformity of semi-solid mixtureVSAvoidcarrier composition complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent creates a universal carrier system that can simultaneously dissolve both water-soluble and fat-soluble active substances. The glycerol derivative-based carrier performs multiple functions: it acts as a solubilizing agent, emulsifier, and stabilizer, eliminating the need for separate carriers and achieving homogeneous semi-solid formulations.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent merges the functions of multiple separate carriers into a single integrated carrier system. By combining the glycerol derivative, surfactant, and co-solvent into one formulation, the system achieves both water-soluble and fat-soluble substance dissolution while maintaining manufacturing simplicity and mixture uniformity.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If high doses of active substances are administered to achieve therapeutic efficacy, then the therapeutic effect is sufficient, but the impurity level in the formulation increases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidimpurity level in formulation
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

By changing the parameters of the carrier system to include optimized ratios of glycerol derivative, surfactant, and co-solvent, the patent achieves high bioavailability that allows therapeutic efficacy to be obtained at lower doses, thereby reducing impurity levels in the final formulation.

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 carrier significantly increases the bioavailability of active substances, allowing for reduced doses and enhanced therapeutic activity, while maintaining a low impurity level and uniform distribution in semi-solid formulations.

Implementation Method 1

a strongly solvating aprotic solvent from the group of sulfoxides, carbonic acid amide, and vegetable oil with a high content of unsaturated fatty acids

Methodology Applied
Scientific EffectSolvation: Solvation

Implementation Method 2

vegetable oil with a high content of unsaturated fatty acids... ensures dissolution and emulsification of both water-soluble active substances and fat-soluble active substances

Methodology Applied
Scientific EffectEmulsification: Emulsion

Implementation Method 3

along with natural emulsifiers, is used to create a semi-solid mixture that enhances the dissolution and emulsification

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Data Source

PatentUS12478679B2Pharmaceutical carrier for active substances and a pharmaceutical composition containing said carrier
Publication Date: 2025.11.25 BIOTTS SA
  • US12478679B2 patent drawing
  • US12478679B2 patent drawing
  • US12478679B2 patent drawing

AI summary

The present invention relates to a pharmaceutical carrier for active substances characterized in that it contains a strongly solvating aprotic solvent from the group of sulfoxides, a carbonic acid amide, and a vegetable oil with a high content of unsaturated fatty acids, and a pharmaceutical composition containing the carrier.