Cefuroxime Axetil Suspension Gel Formation
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Solution Overview
Problem
Cefuroxime axetil, a broad-spectrum cephalosporin antibiotic, tends to form a gelatinous mass when contacted with water, leading to poor dissolution and low absorption, and has a bitter taste that is difficult to mask, posing challenges for oral administration.
Innovation Solution
A suspension formulation of cefuroxime axetil using a combination of citric acid and trisodium citrate as pH agents in specific ratios, along with additional excipients, to prevent gel formation and bitter taste, enhancing solubility and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If cefuroxime axetil is formulated as solid dosage forms, then it provides convenient administration, but it forms gelatinous mass when contacted with water leading to poor dissolution and low absorption
Solution Approach 1:
The patent changes the physical state parameter of the dosage form from solid (tablets, capsules) to liquid suspension. This parameter change prevents the gelatinous mass formation that occurs in solid forms when contacted with water, thereby improving dissolution and absorption while maintaining administration convenience through oral suspension formulation.
Solution Approach 2:
The patent uses a composite system combining cefuroxime axetil with specific excipients including sweeteners (sucrose, saccharin sodium, aspartame), flavors (fruity flavors), and suspending agents. This composite formulation masks the bitter taste and prevents gel formation, resolving the contradiction between administration convenience and dissolution/absorption reliability.
2Stability of the object's composition
If cefuroxime axetil is formulated as solid dosage forms, then it provides stable composition, but it has extremely bitter taste that cannot be easily masked
Solution Approach 1:
The patent introduces intermediary substances (sweeteners and flavors) that mediate between the bitter cefuroxime axetil and the patient's taste receptors. Sweeteners like sucrose, saccharin sodium, and aspartame along with fruity flavors act as intermediaries to mask the extremely bitter taste, making the formulation acceptable for oral administration while maintaining composition stability.
Solution Approach 2:
The patent changes the dosage form parameter from solid to liquid suspension, which inherently provides better taste masking capabilities. The liquid matrix allows for incorporation of taste-modifying excipients that can effectively mask the bitter taste, while the suspension formulation maintains stable composition through proper selection of suspending agents and pH control.
3Object-affected harmful factors
If lipid coating is applied to cefuroxime axetil particles, then it masks bitter taste and prevents gel formation, but it retards dissolution and delays absorption
Solution Approach 1:
The patent extracts or removes the lipid coating approach entirely and replaces it with a direct suspension formulation. Instead of coating particles with lipid that would retard dissolution, the invention uses uncoated or differently coated particles in a suspension matrix with taste-masking excipients, thereby eliminating the dissolution delay while still masking bitter taste and preventing gel formation through the suspension medium.
Solution Approach 2:
The patent replaces the complex lipid coating process with a simpler, more direct suspension formulation approach. The suspension formulation achieves taste masking and gel prevention through its matrix composition rather than through protective coatings, resulting in faster dissolution and absorption while achieving the same protective effects against bitter taste and gel formation.
4Object-affected harmful factors
If conventional coating processes are used for cefuroxime axetil, then it provides taste masking and gel prevention, but the process is complicated and time consuming
Solution Approach 1:
The patent extracts or eliminates the complex conventional coating process entirely. Instead of requiring separate coating steps with atomization, drying, and cooling, the invention formulates cefuroxime axetil directly as a suspension with taste-masking excipients incorporated into the suspension matrix. This eliminates multiple manufacturing steps, reducing both complexity and time while achieving the same functional outcomes of taste masking and gel prevention.
Solution Approach 2:
The patent merges multiple functions (taste masking, gel prevention, and dosage delivery) into a single suspension formulation step. Instead of separate processes for coating and formulation, the invention combines these functions into one integrated suspension preparation process, significantly reducing manufacturing time and complexity while achieving all necessary protective and delivery functions.
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 effectively prevents gel formation, improves solubility, and significantly reduces the bitter taste of cefuroxime axetil, ensuring higher absorption and better mouth feel, as demonstrated by higher dissolution rates and lower bitterness values in taste trials.
Implementation Method 1
Cefuroxime axetil in both crystalline form and the amorphous form has a tendency to form a gelatinous mass when contacted with water
Implementation Method 2
Cefuroxime axetil has a very bitter taste which is highly durable and which cannot be easily masked by adding sweeteners, taste regulating agents and flavors
Data Source
AI summary
The present invention relates to pharmaceutical compositions comprising cefuroxime axetil and the use of these compositions in the treatment of bacterial infections.