Guaifenesin Extended Release Liquid Composition
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Solution Overview
Problem
Current guaifenesin formulations, particularly immediate release preparations, require frequent dosing due to short plasma half-life and are affected by food intake, leading to bioavailability issues and inconvenience, especially for pediatric and geriatric patients, while extended release solid forms pose swallowing difficulties and dose compliance challenges.
Innovation Solution
Development of an extended release liquid composition of guaifenesin with a balanced extended and immediate release portion, coated with release-controlling excipients, providing a consistent release profile and reduced food effect, suitable for once or twice daily administration, and easy to administer in both fasting and fed states.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If immediate release liquid formulation is used, then the formulation is easy to administer and suitable for pediatric population, but the plasma half-life is short requiring multiple times daily dosing
Solution Approach 1:
The liquid formulation is segmented into distinct functional components: extended-release particles (providing sustained release over 12-24 hours) and immediate-release guaifenesin (providing rapid onset). This segmentation allows the formulation to simultaneously achieve both prolonged duration of action and ease of administration as a liquid, resolving the contradiction between these two parameters.
2Ease of operation
If immediate release liquid formulation is used, then the formulation is easy to administer, but food intake significantly affects bioavailability
Solution Approach 1:
The formulation uses a composite approach by combining extended-release particles with a specific vehicle system containing surfactants and co-solvents. This composite formulation reduces food effect on bioavailability while maintaining the liquid form's ease of administration, resolving the contradiction between ease of operation and reliability of drug absorption.
3Duration of action of moving object
If extended release solid formulations are used, then the duration of therapeutic effect is prolonged, but swallowing difficulty arises especially for pediatric and geriatric patients
Solution Approach 1:
The invention changes the physical state parameter from solid (tablets) to liquid form while incorporating extended-release particles. This parameter change allows the formulation to be easily administered to pediatric and geriatric patients who have difficulty swallowing solids, while still providing prolonged therapeutic effect through the extended-release mechanism.
4Duration of action of moving object
If high amount of release controlling excipients is used to achieve extended release in liquid form, then prolonged release is achieved, but solid content per ml increases leading to dosing and palatability challenges
Solution Approach 1:
The formulation applies local quality by concentrating the release-controlling excipients specifically on the surface of the extended-release particles rather than distributing them uniformly throughout the entire liquid volume. This approach achieves prolonged release functionality while minimizing the overall solid content concentration in the liquid formulation, thereby maintaining palatability and ease of dosing.
Data Source
AI summary
The present invention relates to extended release liquid compositions of guaifenesin. The extended release liquid compositions are in the form of suspensions which are ready-to-use or suspensions which are reconstituted from powder. It also relates to processes for the preparation of said extended release liquid compositions.