Preparation, characterization and antimalarial activity of dihydroartemisinin / β-cyclodextrin spray-dried powder

被引:7
|
作者
Pongsamart, Kasama [1 ]
Limwikrant, Waree [1 ]
Ruktanonchai, Uracha Rungsardthong [3 ]
Charoenthai, Nattawut [1 ,2 ]
Puttipipatkhachorn, Satit [1 ,2 ,4 ]
机构
[1] Mahidol Univ, Fac Pharm, Dept Mfg Pharm, Bangkok 10400, Thailand
[2] Mahidol Univ, Fac Pharm, Ctr Innovat Pharm Pharmaceut & Herbal Prod Dev, Bangkok 10400, Thailand
[3] Natl Nanotechnol Ctr, Natl Sci & Technol Dev Agcy, Pathum Thani 12120, Thailand
[4] Mahidol Univ, Dept Mfg Pharm, Fac Pharm, 447 Sri Ayudhya Rd, Bangkok 10400, Thailand
关键词
Dihydroartemisinin; beta-cyclodextrin; Spray drying; Inclusion complex; Antimalarial activity; SOLID DISPERSIONS; PHARMACEUTICAL APPLICATIONS; DISSOLUTION CHARACTERISTICS; PHYSICAL STABILITY; PROCESS VARIABLES; DRUG SOLUBILITY; COMPLEXATION; BIOAVAILABILITY; ENHANCEMENT; ARTEETHER;
D O I
10.1016/j.jddst.2022.103434
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
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页数:9
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