Liquid Hypoglycaemic Sulfonamide Formulation for Pediatric Dosing
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Solution Overview
Problem
Current formulations of hypoglycaemic sulfonamides, such as glibenclamide, are unsuitable for young children and the elderly due to their tablet form, leading to inaccurate dosing and potential hypoglycaemic side effects, and lack a suitable ophthalmic administration route, necessitating a liquid formulation with stable particle size and acceptable organoleptic properties.
Innovation Solution
A liquid pharmaceutical formulation comprising micronised particles of hypoglycaemic sulfonamide with 90% of particles less than 30 μm, combined with thickeners like hydroxyethylcellulose and xanthan gum, and a buffer system maintaining pH between 4 and 8, ensuring accurate dosing and stability for oral and ophthalmic administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If glibenclamide is formulated as tablets, then it is suitable for adult administration, but it is unsuitable for pediatric and geriatric patients who cannot take tablets
Solution Approach 1:
The invention changes the physical form parameter from solid tablets to liquid suspension, making the medication suitable for pediatric and geriatric patients who cannot swallow tablets while maintaining the same active ingredient and therapeutic effect
Solution Approach 2:
The invention divides the patient population into different groups (adults who can take tablets vs. pediatric/geriatric patients who need liquid form) and provides appropriate formulations for each group, with the liquid suspension specifically addressing the needs of those who cannot take solid dosage forms
2Ease of operation
If tablets are crushed and dissolved in liquid, then oral administration becomes possible, but dosing accuracy decreases and particle size variation increases
Solution Approach 1:
The active ingredient is pre-micronized during manufacturing to a controlled size range (90% < 30 μm) before formulation, eliminating the need for crushing tablets at home and ensuring consistent particle size and dosing accuracy
Solution Approach 2:
The invention introduces a thickening agent as an intermediary substance that prevents particle settling and maintains uniform suspension, ensuring accurate dosing without requiring tablet crushing
3Shape
If glibenclamide is suspended in water, then liquid formulation is achieved, but particle settling increases due to low solubility
Solution Approach 1:
The invention introduces a thickening agent as an intermediary substance that increases the viscosity of the suspension medium, thereby reducing particle settling and maintaining stable suspension of the micronized glibenclamide particles
Solution Approach 2:
The invention changes the physical parameter of the suspension medium by adding thickening agents to increase viscosity, which counteracts the settling tendency of the low-solubility glibenclamide particles and maintains compositional stability
4Adaptability or versatility
If no ophthalmic formulation exists, then ocular disorder treatment opportunity is lost, but formulating for ophthalmic use requires meeting specific pH and stability criteria
Solution Approach 1:
The invention creates a universal liquid suspension formulation that can be administered through multiple routes (oral and ophthalmic), allowing the same product to treat both systemic diabetes and ocular disorders caused by diabetic retinopathy
Solution Approach 2:
The invention adjusts the formulation parameters (pH buffer system maintaining pH 4-8, inclusion of thickening agents) to meet the specific requirements for ophthalmic administration while maintaining the same active ingredient and therapeutic mechanism
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 formulation provides accurate and stable delivery of hypoglycaemic sulfonamides, reducing the risk of hypoglycaemic accidents and enabling ophthalmic administration, with improved pharmacokinetic properties and acceptance for pediatric and geriatric patients.
Implementation Method 1
a buffer system allowing the pH of said formulation to be maintained between 4 and 8
Implementation Method 2
at least one thickener, and a buffer system allowing the pH of said formulation to be maintained between 4 and 8
Implementation Method 3
micronised particles of hypoglycaemic sulfonamide, preferably 90% of the particles having a size less than 30 μm
Data Source
AI summary
The present invention relates to a liquid pharmaceutical formulation of hypoglycaemic sulfonamide, intended for oral or ophthalmic administration. The present invention relates in particular to an oral formulation particularly suitable for paediatric use.