Optimization of Xiaoer Lingyin granule formulation using single-factor and response surface methodology

Area of Science:

• Pharmacology
• Traditional Chinese Medicine
• Pharmaceutical Sciences

Background:

• Acute pharyngitis is a common pediatric illness.
• Traditional Chinese Medicine (TCM) formulations require optimization for consistent efficacy and patient acceptance.
• Xiaoer Lingyin granules (XLGs) are a TCM preparation for pediatric acute pharyngitis.

Purpose of the Study:

• To develop and optimize the formulation and manufacturing process of Xiaoer Lingyin granules (XLGs) for pediatric acute pharyngitis.
• To enhance granule quality attributes including formability, flowability, dissolution, and palatability.
• To establish a quantitative optimization framework for pediatric TCM granules.

Main Methods:

• Integration of single-factor experiments, multi-index quality evaluation, and Response Surface Methodology (RSM).
• Systematic evaluation of key formulation variables (drug-to-excipient ratio, ethanol concentration/dosage) and process variables (drying temperature/time).
• Assessment of granule formability, flowability, dissolution, and palatability using sensory analysis and analytical techniques.

Main Results:

• Optimized XLG formulation: 1:1 drug-to-excipient ratio, 65% ethanol, 22.5% ethanol dosage, 70°C drying for 60 min, 0.2% sucralose, 0.8% strawberry flavoring.
• Optimized granules exhibited high molding ratios, acceptable flowability, and dissolution ratios ≥79.76%.
• The RSM model demonstrated good predictive reliability, validated through ANOVA and experimental verification.

Conclusions:

• A robust, quantitative framework for optimizing pediatric TCM granules was successfully established.
• The optimized XLG formulation demonstrates improved physicochemical properties and sensory acceptability.
• This approach enhances the standardization and patient compliance of TCM preparations.