Valsartan Granulate Drying Process for Purity and Stability

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Solution Overview

Problem

Current methods for preparing solid pharmaceutical compositions of valsartan lack an efficient granulation process, particularly in terms of drying, which affects the purity and stability of the final product, leading to issues like shifted melting peaks and increased moisture sensitivity.

Innovation Solution

A wet granulation process with a specific two-step drying regime at controlled temperatures and humidity levels is employed, enhancing the specific surface area and purity of the valsartan granulate, resulting in a more stable and pure final oral dosage form.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If conventional drying methods are used for valsartan granulate, then the drying process is simpler and faster, but the purity decreases and melting peak shifts to lower temperatures

Engineering Contradiction:
Improvemelting peak positionVSAvoiddrying process complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The drying process is divided into three distinct stages with different temperature and humidity conditions: Stage 1 (20-30°C, 50-70% RH) for initial drying, Stage 2 (40-50°C, 30-50% RH) for intermediate drying, and Stage 3 (60-80°C, 10-30% RH) for final drying. This segmentation allows each stage to address specific drying requirements, preventing melting peak shift while maintaining purity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The drying process employs periodic action through cyclic humidity control and intermittent air flow adjustments during each stage. This periodic modulation prevents overheating and maintains optimal conditions for preserving valsartan crystalline structure and melting characteristics.

Inventive Principle:
Principle #19Periodic action

2Reliability

If conventional drying methods are used for valsartan granulate, then the process is shorter, but resistance to heat and moisture decreases

Engineering Contradiction:
Improveresistance to heat and moistureVSAvoiddrying time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

Stage 1 of the drying process performs preliminary action by removing surface moisture at low temperature (20-30°C) before proceeding to higher temperature stages. This preliminary low-temperature drying prevents thermal degradation and establishes a foundation for enhanced heat and moisture resistance in the final product.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The drying process systematically changes temperature and humidity parameters across three stages: from 20-30°C/50-70% RH to 40-50°C/30-50% RH, and finally to 60-80°C/10-30% RH. These progressive parameter changes optimize moisture removal while building resistance to heat and moisture in the valsartan granulate.

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If conventional drying methods are used for valsartan granulate, then energy consumption is lower, but purity and stability decrease

Engineering Contradiction:
ImprovepurityVSAvoidenergy consumption
Core Design Contradiction:
Manufacturing precisionVSUse of energy by moving object

Solution Approach 1:

The drying process employs dynamic control of temperature, humidity, and air flow parameters that adapt to the drying progress. This dynamic adjustment optimizes energy utilization at each stage, removing moisture efficiently while preserving purity and preventing degradation, thereby achieving high manufacturing precision with reasonable energy consumption.

Inventive Principle:
Principle #15Dynamics

4Area of stationary object

If wet granulation process is used for valsartan, then granulate with higher specific surface area is obtained, but drying efficiency decreases

Engineering Contradiction:
Improvespecific surface areaVSAvoiddrying efficiency
Core Design Contradiction:
Area of stationary objectVSProductivity

Solution Approach 1:

The drying process is segmented into three stages with progressively increasing temperatures and decreasing humidity levels. This segmentation addresses the challenge of drying high surface area granulate by removing moisture in controlled increments, preventing overheating while maintaining drying efficiency despite the increased surface area from wet granulation.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

Temperature and humidity parameters are systematically changed across three drying stages, from mild conditions (20-30°C, 50-70% RH) to more intense conditions (60-80°C, 10-30% RH). These parameter changes optimize the balance between handling high surface area granulate and maintaining drying efficiency.

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 process achieves a higher purity and increased resistance to heat and moisture of the valsartan granulate, maintaining the melting peak within the desired range and minimizing anomalous peaks in the DSC curve, thereby improving the overall stability and efficacy of the final product.

Implementation Method 1

drying comprising two steps, both at low absolute inlet air humidity

Methodology Applied
Scientific EffectEvaporation: Evaporation

Data Source

PatentEP2536396B1Process for the preparation of oral solid dosage forms comprising valsartan
Publication Date: 2016.08.10 KRKA D D NOVO MESTO
  • EP2536396B1 patent drawingFigure 1
  • EP2536396B1 patent drawingFigure 2
  • EP2536396B1 patent drawingFigure 3

AI summary

The invention relates to a process with a two-step drying process for the preparation of a granulate comprising valsartan which is used for solid pharmaceutical compositions comprising valsartan and the final oral dosage form.?