Evaluation methods for aerodynamic particle size distribution of fine particles in inhaled products

doi:10.19803/j.1672-8629.20230411

Abstract

Abstract: Objective To improve the quality, safety, and effectiveness of drugs by evaluating the aerodynamic particle size distribution (APSD) of inhaled formulations. Methods The methods and related standards for detecting APSD specified in different national pharmacopoeias were compared and contrasted. APSD was characterized using multiple econometric parameters. The size of the fine particle dose and its proportion in the total collected dose were used as the key indicators for evaluating inhaled products. Results The Anderson cascade impactor (ACI) and the next generation impactor (NGI) were currently the most widely used and included in the US Pharmacopoeia. The Chinese Pharmacopoeia also included a glass twin impinger while the European Pharmacopoeia also included a multi-stage liquid impactor. The mass median aerodynamic diameter (MMAD) was an important variable to control the deposition position of particles in the lung. The geometric standard deviation (GSD) represented the shape of the drug particle size distribution curve. The closer to 1 the distribution curve, the narrower the distribution of particles. The changes in APSD could be detected by measuring both the ratio of the large particle mass (LPM) to the small particle mass (SPM) and the impactor-sized mass (ISM) in effective data analysis (EDA). The size and distribution of drug particles largely determined the location and amount of particle deposition in the respiratory system, thereby affecting the efficacy of drugs. The delivery of active pharmaceutical ingredients (APIs) in the inhaled formulations to the lungs through the respiratory system required that the aerodynamic particle size of aerosols range from 1 to 5 μm. Conclusion Appropriate testing methods can ensure the quality, safety, and effectiveness of inhaled products. Well-designed dosages and drug particle sizes are the key indicators that determine the performance of inhaled formulations. Therefore, successive improvement of testing methods for fine particles and in-depth research on the correlation between in vitro and in vivo use can facilitate the research and development of inhaled products.

Key words: inhaled products, aerodynamic diameter, cascade impactor, characterization methods, data analysis, safety, consistency evaluation, standard

CLC Number:

R917.4

JIA Yinyin, ZHANG Caishu, ZHOU Ying, LIU Li, GENG Ying, WEI Ningyi, NIU Sijing, CHEN Hua, XU Hui. Evaluation methods for aerodynamic particle size distribution of fine particles in inhaled products[J]. Chinese Journal of Pharmacovigilance, 2024, 21(2): 141-146.

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https://zgywjj.magtechjournal.com/EN/Y2024/V21/I2/141

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