Effervescent Cefdinir Formulation with PVP Binder

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Solution Overview

Problem

Cefdinir's poor solubility in common solvents and organic solvents hinders the development of effervescent formulations, leading to issues with tablet hardness and dispersion time, affecting bioavailability and product fragility.

Innovation Solution

Effervescent cefdinir formulations comprising 2-5% polyvinylpyrrolidone and trometamol, achieving tablet hardness of 7-8 kP and dispersion in less than 120 seconds, with polyvinyl pyrrolidone playing a crucial role in optimizing these properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If tablet hardness is increased to prevent breaking during handling, then mechanical strength is improved, but dispersion time increases and dissolution becomes slower

Engineering Contradiction:
Improvetablet hardnessVSAvoiddispersion time
Core Design Contradiction:
StrengthVSLoss of time

Solution Approach 1:

The patent optimizes the concentration of polyvinylpyrrolidone binder to 2-5% of total formulation weight, which achieves the optimal balance between tablet hardness (7-8 kP) and rapid dispersion time (less than 120 seconds). This precise parameter control resolves the contradiction by finding the optimal point where mechanical strength is sufficient for handling while dissolution remains rapid.

Inventive Principle:
Principle #35Parameter changes

2Strength

If cefdinir is formulated with conventional binders to achieve adequate hardness, then mechanical strength is improved, but solubility and bioavailability deteriorate due to poor solubility of cefdinir

Engineering Contradiction:
Improvetablet hardnessVSAvoidbioavailability
Core Design Contradiction:
StrengthVSReliability

Solution Approach 1:

Polyvinylpyrrolidone acts as a solubility-enhancing binder that mediates between the poor solubility of cefdinir and the need for adequate tablet hardness. This intermediary substance improves the wettability and dissolution characteristics of cefdinir while providing sufficient binding strength, thereby resolving the contradiction between mechanical strength and bioavailability.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Device complexity

If effervescent formulation is developed without optimal binder selection, then formulation complexity is reduced, but physical properties such as hardness and dispersion become unoptimized

Engineering Contradiction:
Improveformulation complexityVSAvoidphysical properties optimization
Core Design Contradiction:
Device complexityVSManufacturing precision

Solution Approach 1:

The patent establishes specific parameter ranges for polyvinylpyrrolidone (2-5% of total weight) that simultaneously achieve optimal tablet hardness (7-8 kP) and rapid dispersion time (less than 120 seconds). This precise parameter specification resolves the contradiction by providing clear formulation guidelines that ensure optimized physical properties without excessive formulation complexity.

Inventive Principle:
Principle #35Parameter changes

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 ensures tablets do not break during handling, dissolves rapidly in water, and maintains optimal physical properties, enhancing bioavailability and usability.

Implementation Method 1

polyvinylpyrrolidone in an amount in the range of 2-5% with respect to the total weight of the unit dose

Methodology Applied
Scientific EffectAdhesion: Adhesive

Implementation Method 2

effervescent formulations comprising cefdinir as an active agent... disperse in water in less than 120 seconds

Methodology Applied
Scientific EffectEffervescence:

Implementation Method 3

polyvinyl pyrolidone... dispersed in a short time, that is less than 120 seconds, in water

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP2515859B1Rapidly dispersing effervescent formulation
Publication Date: 2015.09.16 BILGIC MAHMUT
  • EP2515859B1 patent drawing

AI summary

Present invention is related to water dispersible pharmaceutical dosage forms comprising cefdinir as active agent and methods for preparation of these.