High-Loading SGLT2 Inhibitor Tablet Formulation
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Solution Overview
Problem
Current treatments for diabetes mellitus and obesity lack effective inhibitors of sodium-dependent glucose transporters, leading to inadequate management of associated complications and metabolic disorders.
Innovation Solution
A tablet formulation containing a 1-(β-D-glucopyranosyl)-3-(phenylthienylmethyl)benzene derivative or its pharmaceutically acceptable salt, which acts as an inhibitor of sodium-dependent glucose transporters, is developed, allowing for high drug loading and efficient treatment of diabetes mellitus and obesity-related conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional tablet formulations are used for SGLT2 inhibitors, then the tablets can be manufactured with standard additives, but the drug loading is low and tablet size becomes large
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using specific excipients with optimized proportions, adjusting the drug-to-excipient ratio to achieve high drug loading (70-85% w/w) while maintaining acceptable tablet size and manufacturing feasibility
Solution Approach 2:
The patent employs a composite formulation system combining the SGLT2 inhibitor with a specific mixture of excipients including microcrystalline cellulose, croscarmellose sodium, and magnesium stearate, creating a optimized composite material that achieves both high drug loading and proper tablet characteristics
2Ease of operation
If high drug loading is achieved in the tablet, then the tablet size is reduced improving compliance, but the manufacturing complexity increases
Solution Approach 1:
The patent optimizes manufacturing parameters including compression force, granulation moisture content, and mixing time to enable production of high drug loading tablets using conventional equipment, thereby reducing manufacturing complexity despite the high active ingredient content
3Ease of manufacture
If more excipients are added to the tablet formulation, then the tablet can be manufactured with proper characteristics, but the drug loading decreases
Solution Approach 1:
The patent carefully adjusts the quantity and type of excipients to minimal levels necessary for manufacturability, using optimized concentrations of binders, disintegrants, and lubricants that maintain tablet quality attributes while maximizing the proportion of active pharmaceutical ingredient
Solution Approach 2:
The patent applies different excipients at specific locations and in specific proportions within the tablet formulation - using microcrystalline cellulose as the primary filler and binder, croscarmellose sodium as disintegrant, and magnesium stearate as lubricant - each serving its specific function with optimized local concentration to achieve high overall drug loading
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 tablet provides effective inhibition of sodium-dependent glucose transporters, effectively treating and preventing the progression of diabetes mellitus, obesity, and related complications, with improved patient compliance due to its compact size and superior tablet characteristics.
Implementation Method 1
a 1-(β-D-glucopyranosyl)-3-(phenylthienylmethyl)benzene derivative represented by formula (A) or a pharmaceutically acceptable salt thereof which acts as an inhibitor of sodium-dependent glucose transporters
Data Source
AI summary
The present invention is directed to a tablet containing a 1-(ß-D-glucopyranosyl)-3-(phenylthienylmethyl)benzene compound in high drug loading, in particular, containing the compound ranging from 30 to 95% by weight of tablet and pharmaceutically acceptable additives.