Determination of deferasirox particle size distribution via laser diffraction and its application in establishing a correlation between particle size and drug dissolution in vitro

doi:10.5246/jcps.2021.11.079

Abstract

Abstract:

Deferasirox is the first-line drug for iron overload due to thalassemia in adults and pediatric patients. It is classified as a type II compound in the Biopharmaceutics Classification System, and thus the particle size of its active pharmaceutical ingredient (API) should be strictly controlled during the manufacturing process. In the present study, laser diffraction was adopted to measure the particle size distribution of deferasirox API. We also developed and validated an accurate and convenient method by investigating important optical parameters and sample dispersing conditions. The relative standard deviation values, namely, d (0.1), d (0.5), d (0.9), and d (4,3), measured via methodology validation and actual sample measurement were < 3%. The dissolution curves of several batches of dispersible tablets prepared using deferasirox with different particle sizes were compared in the four dissolved media to investigate the influence of particle size on drug dissolution in vitro. Results indicated that the particle size distribution of deferasirox API significantly affected the release of its dispersible tablet.

Key words: Deferasirox, Particle size distribution, Laser diffraction, Dissolution curve

Supporting: http://www.jcps.ac.cn/attached/file/20211129/20211129190139_832.pdf

Yuyuan Chen, Song Wu, Liqing Chen, Yuanyuan Zhang, Zhonggao Gao, Tianlei Li, Wei Huang, Qingyun Yang. Determination of deferasirox particle size distribution via laser diffraction and its application in establishing a correlation between particle size and drug dissolution in vitro[J]. Journal of Chinese Pharmaceutical Sciences, 2021, 30(11): 912-923.

Figures/Tables 6

Table 1. Investigation results of the NP-40 solutions (n = 3).

Table 2. Investigation results of optical parameters and sample dispersing conditions (n = 3).

Table 3. Summary of the validation report.

Table 4. Measurement results of the deferasirox API particle size distribution (n = 3).

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