Trientine Liquid Formulation for Stable Oral Dosing
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Solution Overview
Problem
Existing solid formulations of Trientine, such as tablets and capsules, pose challenges for patients with swallowing difficulties, including children, elderly, and those with conditions like phagophobia, leading to non-compliance and inaccurate dosing, especially in treating conditions like Wilson's disease.
Innovation Solution
Development of a Trientine liquid dosage form that can be prepared by reconstituting solid formulations like powders, granules, or effervescent tablets in a liquid carrier, incorporating excipients for stability, flavor, and palatability, packaged in suitable containers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If solid formulations (tablets, capsules) are used, then chemical stability is maintained, but patient compliance deteriorates due to swallowing difficulties
Solution Approach 1:
The patent transforms Trientine from solid crystalline form to liquid solution form, fundamentally changing the physical state parameter. This enables easy administration to patients with swallowing difficulties while maintaining stability through controlled pH (2.0-9.0) and concentration (10-200 mg/ml) parameters
Solution Approach 2:
The patent introduces liquid carriers and excipients as intermediary substances to dissolve Trientine, creating a stable liquid formulation. These intermediaries enable the drug to be administered in liquid form while maintaining chemical stability through proper formulation
2Ease of operation
If liquid dosage form is developed, then ease of administration improves, but chemical stability deteriorates due to hydrolysis and degradation
Solution Approach 1:
The patent controls pH within 2.0-9.0 range and maintains Trientine concentration at 10-200 mg/ml to prevent hydrolysis and degradation. These parameter controls enable liquid formulation while maintaining chemical stability
Solution Approach 2:
The patent converts the potential harm of water-induced degradation into benefit by using controlled aqueous solutions with pH adjustment and stabilizing excipients, transforming the degradation risk into a stable liquid formulation that improves administration
3Ease of operation
If Trientine is formulated as liquid, then palatability improves, but manufacturing complexity increases
Solution Approach 1:
The patent adjusts pH to 2.0-9.0 and selects appropriate excipients to mask the bitter taste of Trientine, improving palatability. The formulation process, while more complex than solids, follows established liquid dosage form manufacturing protocols
Data Source
AI summary
A pharmaceutical liquid dosage form of Trientine and/or pharmaceutically acceptable salts thereof is provided, which are suitable for oral administration. A process of preparing the liquid dosage form and use for treatment of Wilson's disease and related diseases are also provided.