Buffered Vigabatrin Oral Solution for Stability and Palatability

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Solution Overview

Problem

Existing liquid pharmaceutical compositions for oral delivery face challenges in solubility, stability, taste masking, and patient compliance, particularly for pediatric and geriatric patients, with many drugs being poorly soluble and having poor bioavailability.

Innovation Solution

A pharmaceutical composition comprising an active pharmaceutical ingredient, a buffering agent, and water, formulated to maintain a pH between 5 and 8, with optional excipients for taste masking and stability, suitable for oral delivery in the form of aqueous solutions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If liquid pharmaceutical compositions are formulated for oral delivery, then patient compliance is improved, but stability and solubility are compromised

Engineering Contradiction:
Improvepatient complianceVSAvoiddrug stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by adjusting the pH of the liquid composition to specific ranges (pH 3-7, preferably pH 4-6) to optimize both stability and solubility. This involves modifying chemical parameters (pH, ionic strength) and physical parameters (temperature, concentration) to achieve the desired balance between patient compliance and drug stability in liquid formulations

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If liquid formulations are used instead of solid tablets, then patient compliance is improved, but manufacturing complexity increases

Engineering Contradiction:
Improvepatient complianceVSAvoidformulation complexity
Core Design Contradiction:
Ease of operationVSDevice complexity

Solution Approach 1:

The patent extracts and eliminates unnecessary excipients from the formulation by using a simplified liquid composition that requires fewer additives compared to conventional liquid formulations. This reduction in formulation complexity while maintaining patient compliance benefits is achieved by focusing on essential components only

Inventive Principle:
Principle #2Taking out (Extraction)

3Stability of the object's composition

If conventional liquid formulations are used, then solubility is improved, but taste and palatability deteriorate

Engineering Contradiction:
Improvedrug solubilityVSAvoidtaste and palatability
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent uses parameter changes by adjusting pH to optimize both solubility and taste. By controlling the pH within specific ranges, the formulation achieves adequate drug solubility while minimizing bitter tastes and improving overall palatability, making the liquid formulation acceptable to pediatric and geriatric patients

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 composition provides improved stability, palatability, and patient compliance, with enhanced bioavailability and dissolution profiles, making it suitable for pediatric and geriatric patients.

Implementation Method 1

a buffering agent, and water, wherein the pH of the composition is between about pH 5 and about pH 8

Methodology Applied
Scientific EffectBuffering:

Data Source

PatentUS12539300B2Method of treating seizures and epilepsy using liquid pharmaceutical composition for oral dosage of vigabatrin
Publication Date: 2026.02.03 LIQMEDS WORLDWIDE LTD
  • US12539300B2 patent drawing

AI summary

This disclosure relates to pharmaceutical compositions in the form of a solution for oral delivery. Particularly, the pharmaceutical compositions comprise an active pharmaceutical ingredient, a buffering agent, and water. In some embodiments, the pH of the composition is from about pH 5 to about pH 8. In some embodiments, the active pharmaceutical ingredient is selected from ramipril, solifenacin, vigabatrin, losartan potassium, warfarin, and melatonin.