Losartan Mini-Tablet Enteric Coating for Pediatric Dose Precision
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Solution Overview
Problem
Existing pediatric formulations of losartan, such as the LORZAAR® suspension, face challenges with stability, precise dosing, sedimentation, bitter taste masking, and cumbersome administration, making it difficult to adjust doses according to a child's changing body weight.
Innovation Solution
Development of losartan mini-tablets with a high surface area to volume ratio, coated to delay release, and containing excipients for taste masking, allowing precise dose adjustment and swallowability, suitable for pediatric use.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If losartan is formulated as an oral suspension for pediatric use, then the dosage form can be administered to children, but the formulation requires preservatives to maintain stability and the suspension tends to sediment requiring repeated shaking
Solution Approach 1:
The patent transforms the physical state of losartan from liquid suspension to solid mini-tablets, fundamentally changing the formulation parameters. This eliminates sedimentation issues inherent in suspensions while maintaining pediatric suitability through small size and adjustable dosing.
Solution Approach 2:
The mini-tablets are designed as single-use units with low active ingredient content (0.5-2 mg), allowing precise dosing for children. Each tablet is a disposable unit that eliminates the need for preservatives and shaking, as each tablet is independently stable.
2Object-affected harmful factors
If losartan is formulated as a suspension with viscosity enhancers and sweeteners to mask bitter taste, then the taste is improved, but the formulation becomes more complex and requires multiple additives
Solution Approach 1:
The patent extracts the bitter taste problem by using enteric coating on the mini-tablets. The coating isolates the losartan from oral contact, preventing bitter taste perception while the tablet dissolves in the intestine. This eliminates the need for taste-masking additives like sweeteners and flavorings.
Solution Approach 2:
The enteric coating acts as an intermediary barrier between the bitter losartan and the child's taste receptors. This coating layer prevents direct contact in the mouth while allowing drug release in the intestine, solving the taste problem without adding formulation complexity.
3Measurement precision
If losartan mini-tablets with low active ingredient content are used, then precise dose adjustment is possible, but the mini-tablets require high compression forces during manufacturing
Solution Approach 1:
The patent uses composite granulate materials with optimized composition (including microcrystalline cellulose, pregelatinized starch, and other excipients) that provide adequate compressibility and flow properties. This composite formulation allows manufacturing of low-dose mini-tablets with sufficient mechanical strength despite the low losartan content (0.5-2 mg).
Solution Approach 2:
The losartan is segmented into very small mini-tablet units containing minimal active ingredient (0.5-2 mg each). This segmentation enables precise dosing by administering whole tablets only, while the granulate composition is optimized to ensure these small tablets can be manufactured with adequate mechanical properties.
4Object-affected harmful factors
If enteric coating is applied to delay losartan release and mask bitter taste, then taste masking is improved, but the manufacturing process becomes more complex
Solution Approach 1:
The patent applies enteric coating to the mini-tablets, changing the surface properties to create a pH-dependent release profile. This coating technique is a well-established pharmaceutical process that, while adding a manufacturing step, provides reliable taste masking and controlled release without requiring complex custom manufacturing procedures.
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 mini-tablets provide precise dose adjustment, improved swallowability, and enhanced stability, eliminating the need for preservatives and simplifying dosing, while effectively masking the bitter taste of losartan.
Implementation Method 1
enteric coating which delays the release of the losartan from the mini-tablet by at least 30 seconds, preferably by at least 1 minute, more preferably by at least 2 minutes
Implementation Method 2
granulate composition that can be compressed to form the mini-tablet under high compression forces of from 50 MPa to 200 MPa, preferably of from 80 MPa to 150 MPa
Data Source
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AI summary
The present invention relates to micro tablets for pediatric applications, containing losartan or one of its pharmaceutically acceptable salts.