Fosfomycin Trometamol Tablet Formulation for Veterinary Use
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Solution Overview
Problem
Formulating fosfomycin trometamol tablets for veterinary use, particularly for companion animals like cats and dogs, is challenging due to high hygroscopicity and poor stability, which affects palatability and pharmacotechnical properties, and existing formulations with high active ingredient content result in large, unpalatable tablets.
Innovation Solution
The use of anhydrous calcium hydrogen phosphate and microcrystalline cellulose as diluents in fosfomycin trometamol formulations improves flow and compressibility, stability, and palatability, allowing for the creation of tablets with reduced excipient content and adaptable dosing based on animal weight.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If fosfomycin trometamol is formulated with high active ingredient content to reduce excipient amount, then the amount of excipients is reduced, but the tablet size becomes too large and palatability deteriorates
Solution Approach 1:
The tablet is divided into multiple segments or pieces with break marks, allowing the total dose to be divided into smaller, more palatable portions for veterinary administration while maintaining the required high active ingredient content
Solution Approach 2:
The formulation changes the physical parameters of the tablet including size, shape, and incorporation of palatability enhancers to improve acceptance by animals while maintaining high fosfomycin trometamol content
2Speed
If fosfomycin trometamol is formulated as a solution, then absorption rate is improved, but stability deteriorates due to high hygroscopicity and poor stability in water
Solution Approach 1:
The formulation transitions from a liquid solution phase to a solid dispersed phase using superdisintegrants and specific excipients, maintaining rapid disintegration and absorption characteristics while achieving stability in the solid state for storage and administration
3Stability of the object's composition
If fosfomycin trometamol is formulated as a granulate for human use, then stability is improved, but ease of operation deteriorates for veterinary use due to difficulty in dose adaptation
Solution Approach 1:
The granulate formulation is divided into multiple tablets with break marks, enabling veterinarians to easily adapt the dose to animal weight by administering appropriate numbers of tablets or fractions thereof, while maintaining the stability benefits of the granulate structure
4Device complexity
If fosfomycin trometamol tablets are manufactured with no excipients other than lubricant, then manufacturing complexity is reduced, but manufacturing precision deteriorates due to lack of flow and compressibility properties
Solution Approach 1:
Superdisintegrants and specific excipients are introduced as intermediary substances that facilitate tablet manufacturing by improving flow and compressibility properties, enabling precise manufacturing while maintaining a relatively simple formulation overall
Data Source
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AI summary
The present invention concerns tablet formulations of fosfomycin trometamol, methods of manufacturing and using thereof. More specifically, it relates to an oral pharmaceutical composition in tablet form comprising or consisting of: a. fosfomycin trometamol; b. a low moisture diluent selected from the group consisting of anhydrous calcium hydrogen phosphate, anhydrous microcrystalline cellulose and combinations thereof; c. optionally, a lubricant; and d. optionally, other pharmaceutically acceptable excipients.