Benidipine Tablet Composition With PVA for Uniform Dissolution
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Solution Overview
Problem
Benidipine, a poorly water-soluble calcium channel blocker, faces challenges in achieving desired dissolution profiles, stability, content uniformity, and homogeneity due to its low solubility and low amounts in formulations, complicating mixing and formulation processes.
Innovation Solution
A tablet composition comprising benidipine or its pharmaceutical salt combined with polyvinyl alcohol and a low amount of disintegrant, such as pregelatinized starch, along with excipients like lactose monohydrate and magnesium stearate, to enhance dissolution, stability, and content uniformity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If benidipine is formulated in low amounts to achieve desired dosage, then therapeutic efficacy is maintained, but content uniformity and mixing homogeneity deteriorate
Solution Approach 1:
The patent combines benidipine with polyvinyl alcohol to create a composite granule system. This merging of the active ingredient with a hydrophilic polymer enhances mixing homogeneity and content uniformity while maintaining the low dosage requirement for therapeutic efficacy.
Solution Approach 2:
The invention uses composite materials by formulating benidipine with polyvinyl alcohol and disintegrants to create a homogeneous mixture. This composite approach ensures uniform distribution of the low amount of benidipine throughout the tablet matrix, resolving the content uniformity issue.
2Duration of action of moving object
If conventional disintegrant amounts are used to ensure tablet disintegration, then disintegration is achieved, but dissolution profile of benidipine deteriorates due to poor water solubility
Solution Approach 1:
The patent changes the parameter of disintegrant amount from conventional levels to a reduced range (0.1-10.0% w/w). This parameter change, combined with polyvinyl alcohol, achieves both tablet disintegration and improved dissolution profile by controlling the release kinetics of poorly water-soluble benidipine.
Solution Approach 2:
Polyvinyl alcohol acts as an intermediary substance that facilitates both tablet disintegration and controlled dissolution of benidipine. This hydrophilic polymer mediates between the disintegrant and the poorly water-soluble active ingredient, ensuring both disintegration and acceptable dissolution profile.
3Strength
If benidipine is formulated with conventional excipients to achieve tablet structure, then tablet integrity is maintained, but stability and content uniformity deteriorate
Solution Approach 1:
The invention employs composite materials by combining benidipine with polyvinyl alcohol and specific disintegrants in controlled amounts. This composite formulation maintains tablet integrity while improving content uniformity and stability through homogeneous mixing and controlled release characteristics.
Data Source
AI summary
The present invention relates to a tablet composition comprising benidipine or pharmaceutical acceptable salt thereof, polyvinyl alcohol and at least one disintegrant, wherein the amount of disintegrant is between 0.1% and 10.0% by weight in the total composition. The present invention also relates to a simple, rapid, cost-effective, time-saving and industrially suitable process for the preparation of a tablet composition.