Empagliflozin Metformin Film Coated Tablet Compressibility
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Solution Overview
Problem
Formulations of empagliflozin and metformin hydrochloride face challenges due to low solubility and poor compressibility of empagliflozin, and metformin's high amounts cause issues with compressibility, homogeneity, flowability, and dissolution profile, leading to ineffective oral pharmaceutical dosage forms.
Innovation Solution
A film coated tablet formulation using croscarmellose sodium or other disintegrants, along with diluents like lactose monohydrate, binders such as hydroxypropyl cellulose, and glidants/lubricants like anhydrous colloidal silicon dioxide, which improves compressibility, dissolution profile, and stability, and is prepared through a simple and cost-effective wet granulation process.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If empagliflozin and metformin hydrochloride are formulated together, then the combination provides synergistic glycemic control, but low solubility of empagliflozin and poor compressibility of metformin lead to difficulties with disintegration, dissolution times, compressibility, homogeneity, flowability and dissolution profile
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by selecting specific excipients with optimized properties. The disintegrant content is set at 1-15% and binder at 2-15% to improve dissolution and compressibility. The use of film coating with specific polymer ratios changes the surface properties to enhance solubility and disintegration while maintaining the synergistic glycemic control efficacy of the drug combination
Solution Approach 2:
The patent creates a composite tablet formulation combining empagliflozin, metformin hydrochloride, and multiple excipients (disintegrant, binder, lubricant, film coating polymers) in specific ratios. This composite structure addresses the poor compressibility of metformin and low solubility of empagliflozin by integrating them with functional excipients that provide the necessary mechanical and dissolution properties while maintaining the therapeutic synergism
2Reliability
If metformin is present in high amounts in the composition, then glycemic control is enhanced, but compressibility, homogeneity, flowability and dissolution profile deteriorate
Solution Approach 1:
The patent introduces disintegrants and binders as intermediary substances that mediate between metformin particles. The disintegrant (1-15%) acts as a spacer that prevents metformin crystal aggregation and improves flowability, while the binder (2-15%) provides bridging between particles to enhance compressibility and homogeneity without compromising the high metformin content needed for glycemic control
Solution Approach 2:
The patent optimizes the physical parameters of metformin by controlling particle size distribution and using specific excipient ratios. The film coating with controlled polymer composition changes the dissolution rate parameter, allowing high metformin content to be maintained while achieving acceptable dissolution profile and homogeneity through parameter optimization
3Device complexity
If empagliflozin is formulated with low solubility, then the formulation is simpler, but disintegration and dissolution times increase
Solution Approach 1:
The patent applies a film coating to the tablet surface using hydrophilic polymers (hydroxypropyl methylcellulose, polyvinyl alcohol, or carboxymethyl cellulose) in specific ratios. This thin film layer acts as a flexible barrier that controls drug release while the hydrophilic nature of the polymers promotes rapid wetting and disintegration, reducing dissolution time without significantly increasing formulation complexity
Solution Approach 2:
The disintegrant serves as an intermediary substance that facilitates rapid water penetration into the tablet matrix. By selecting disintegrant types and optimizing content at 1-15%, the formulation achieves fast disintegration that overcomes the low solubility of empagliflozin, reducing dissolution time while maintaining formulation simplicity
Data Source
AI summary
The present invention relates to a film coated tablet comprising empagliflozin and metformin hydrochloride wherein comprising at least one disintegrant which is croscarmellose sodium, sodium starch glycollate, sodium alginate, starch, magnesium aluminum silicate or a mixture thereof. The present invention also relates to a simple, rapid, cost effective, time-saving and industrially convenient method of preparing the tablet.