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

来源：

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY | 2022年 / 73卷

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

页数：9

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