Micronization of Allopurinol and Dapsone by Using Supercritical Anti-solvent Method
Date Issued
2012
Date
2012
Author(s)
Liu, Chun-Hung
Abstract
In order to enhance the dissolution rate and bioavailability in human beings, this study focused on the micronization of poor water soluble pharmaceuticals by using supercritical antisolvent method (SAS). The target pharmaceuticals used in this research are Allopurinol and Dapsone. Allopurinol is an oral drug for gout treatment and Dapsone is an oral durg for leprosy. Both two drugs have poor water solubility and low dissolution rate. Therefore, the purpose of this study is trying to make these two drugs micronized and enhance their dissolution rate.
In this study, supercritical carbon dioxide was used as antisolvent. Different experimental results were obtained by different effect parameters, including solvent, operation temperature, pressure, solution flow rate, nozzle diameter and solution concentration.
About the micronization of Allopurinol, it could be successfully micronized from 8.9 μm to 0.8 μm at the optimal operating conditions.
About the micronization of Dapsone, it could also be successfully micronized from 40.9 μm to 2.2 μm at the optimal operating conditions. From the DSC result we can find another crystalline form after SAS processed.
After the micronization process, the processed and unprocessed pharmaceuticals were tested by using a dissolution tester. The results of dissolution rate test, both the processed drugs have higher dissolution rate than the original drugs.
Subjects
supercritical anti-solvent
micronization
Allopurinol
Dapsone
Type
thesis
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