Micronization of Pharmaceutical Compounds Using Supercritical Anti-Solvent Precipitation Process
Date Issued
2005
Date
2005
Author(s)
Chang, Yun-Ping
DOI
zh-TW
Abstract
Micronization of the antibiotics (Sulfamethoxazole and Sulfaphenazole) and the non-steroidal anti-inflammatory drugs (Acetaminophen and Sulindac) were investigated in this study using the batch and continuous supercritical carbon dioxide anti-solvent (SAS) precipitation method. Particles produced by the continuous SAS are smaller than those produced by the batch ones. Crystal structure of sulfamethoxazole analyzed by XRD showed the solid-solid transition after the batch SAS process.
The effect of the process parameters were compared using sulfamethoxazole as model drug. In the batch SAS process, using ethyl acetate as solvent at low concentration favors smaller particle formation while in the continuous SAS process, acetone as solvent was suggested and operating at lower solution flow rate and higher concentration favored smaller particle formation. The micronized sulfamethoxazole exhibits a higher dissolution rate and antibacterial performance. The dissolution test demonstrated the use of additives in drug formulation can be avoided when the SAS processed drug is used. Coprecipitation of sulfamethoxazole and hydroxypropylcellulose (HPC) by the continuous SAS process was also investigated. The dissolution rate of sulfamethoxazole was dramatically enhanced after Coprecipitating with HPC.
Subjects
超臨界反溶劑
藥物
微粒化
Supercritical
Antisolvent
Pharmaceutical
Micronization
Type
thesis
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