期刊
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
卷 73, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.jddst.2022.103434
关键词
Dihydroartemisinin; beta-cyclodextrin; Spray drying; Inclusion complex; Antimalarial activity
资金
- Royal Golden Jubilee PhD Program [PHD/0073/2550]
- Strategic Basic Research Program [DBG 5080011]
- Thailand Research Fund, Thailand
- Faculty of Pharmacy, Mahidol University [PY-CIP6302]
This study optimized the process conditions for the production of spray-dried powder of dihydroartemisinin (DHA) with beta-cyclodextrin (beta-CD) using a factorial design. The results showed that the inclusion complex formation between DHA and beta-CD improved the dissolution rate of DHA without affecting its antimalarial activity. The spray-dried powder was also found to be chemically and physically stable during storage.
In this study a factorial design was used to optimize process conditions to produce spray-dried powder of dihydroartemisinin (DHA) with beta-cyclodextrin (beta-CD). Predicted conditions for maximum yield and minimum residual moisture were as follows: inlet temperature; 120 C, aspirator setting; 100%, feed rate; 25%, and molar ratio of DHA:beta-CD; 1:2. The higher percent inclusion yield was obtained in the spray-dried powder with lower molar ratio of DHA:beta-CD. DHA existed in amorphous state in the spray-dried powder with 1:2 M ratio of DHA:beta-CD whereas it was in crystalline state in the spray-dried powder with 2:1 M ratio of DHA:beta-CD. The inclusion complex formation between DHA and beta-CD was revealed by FTIR study. The spray-dried powder of DHA with beta-CD showed dramatically enhanced dissolution rate with unchanged antimalarial activity. Moreover, it was chemically and physically stable at 30 C, 75%RH for 3 months after storage.
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