SAIB Solvent System for Controlled Release

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Solution Overview

Problem

Biodegradable systems for controlled release of medicinally active substances face challenges due to the high viscosity of sucrose acetate isobutyrate (SAIB), requiring dilution with solvents for parenteral administration, and existing solvents may not provide optimal solvency for all active ingredients.

Innovation Solution

The use of glycerol formal and Solketal as solvents with SAIB in biodegradable pharmaceutical systems, which improves solvency for active ingredients like fluoroquinolones and analgesics, allowing for controlled release formulations with varying release characteristics by adjusting SAIB concentrations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If SAIB is used as active ingredient carrier, then controlled release is achieved, but high viscosity requires dilution with solvent

Engineering Contradiction:
Improvecontrolled release durationVSAvoidadministerability
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent changes the chemical composition parameters of the solvent system by selecting specific solvents (glycerol formal, Solketal, ethyl lactate) with appropriate solubility characteristics for SAIB and active ingredients. This parameter optimization enables the formulation to achieve both adequate viscosity for controlled release and sufficient fluidity for parenteral administration without requiring excessive dilution.

Inventive Principle:
Principle #35Parameter changes

2Duration of action of moving object

If SAIB concentration is increased for sustained release, then release duration is extended, but formulation becomes more viscous and harder to administer

Engineering Contradiction:
Improvesustained release durationVSAvoidinjectability
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent creates a composite solvent system combining glycerol formal and/or Solketal with ethyl lactate in specific ratios. This composite approach leverages the complementary properties of each solvent: glycerol formal and Solketal provide high solvency for SAIB and active ingredients, while ethyl lactate contributes to fluidity and injectability. The synergistic combination enables sustained release formulations with optimized administration characteristics.

Inventive Principle:
Principle #40Composite materials

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

This combination enhances the solubility and stability of active ingredients, enabling effective controlled release formulations with improved tolerability and stability, particularly for fluoroquinolones and analgesics, and allows for adjustments in release profiles through SAIB concentration variations.

Implementation Method 1

Addition of glycerol formal and/or Solketal improves the solvency for many active ingredients

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentUS8231903B2Controlled release system
Publication Date: 2012.07.31 BAYER INTPROP GMBH
  • US8231903B2 patent drawing
  • US8231903B2 patent drawing
  • US8231903B2 patent drawing

AI summary

The invention relates to a system for controlled release of medicinally active substances, which comprises sucrose acetate isobutyrate (SAIB) and a further solvent.