Micronization and Encapsulation of Pharmaceutical Compounds Using Supercritical Anti-Solvent Precipitation Process
Date Issued
2006
Date
2006
Author(s)
Chen, Jiun-Jen
DOI
zh-TW
Abstract
The purpose of this study was to apply the technique, supercritical anti-solvent (SAS) to the preparation of micronized polymers and drugs. In the SAS process, supercritical CO2 acts as an anti-solvent for the solution. The supercritical CO2 causes supersaturation of the solution, leading to nucleation and precipitation of the solute rapidly. The polymers such as PMMA, CA, HPC were successfully micronized using the SAS process. At the same time, the size of drugs such as Hydrochlorothiazide (HCT), Tolazamide, Succinic acid and Naringin were also greatly reduced after the SAS process.
In this research, the effect of the process parameters was discussed using HCT as model drug. The operating parameters that have an effect on the size of the drug, such as pressure, temperature, concentration of solution and flow rate of solution, were systematically studied to find the optimum operating parameters. We got the smallest average particle size, 0.67µm of HCT at the condition that P=120bar, T=45℃,solution concentration=10% sat., solution flow rate=0.25mL/min.
Encapsulation of fine particles with polymer using the supercritical antisolvent coating process was also investigated in this research. The diuretic drug, HCT particles were used as host particles and PLA, a biodegradable polymer used for controlled release of drugs, was chosen as the coating material. This study also discussed the dissolution rates of original, micronized and encapsulated drugs. The dissolution rate of micronized HCT which were obtained after continuous SAS was 3 times greater than that of the original drug. The encapsulated drug allows a slow and prolonged drug release and the release profile of the encapsules matches the Higuchi matrix release kinetic model.
Subjects
微粒化
包覆
超臨界反溶劑法
Micronization
Encapsulation
Supercritical antisolvent
Type
thesis
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