Micronization and Amorphization of Lapatinib and Nitrofurantoin Using Supercritical Anti-solvent Method
Date Issued
2011
Date
2011
Author(s)
Yu, Wen-Lin
Abstract
This study is focus on the micronization and amorphization of poorly water soluble pharmaceuticals using supercritical anti-solvent method to enhance the dissolution rate and bioavailability in human. The target pharmaceuticals used in this research include lapatinib ditosylate and nitrofurantoin. Lapatinib ditosylate is an orally active drug for breast cancer and nitrofurantoin is an antibiotic which is usually used in treating urinary tract infection. Both the drugs has poor water solubility and hence the low dissolution rate and low bioavailability in human. Therefore, the object of this study is to assess the possibility of micronization and amorphization of these two target drugs.
The supercritical carbon dioxide was employed as the anti-solvent in this study. The effects of six process parameters were compared and discussed, including solvent, operation temperature, pressure, solution concentration, solution flow rate and nozzle diameter.
About the micronization of lapatinib ditosylate, it could be successfully micronized from original 11.87 μm to 0.32 μm at the optimal operating conditions. From the results of XRD, the micronized lapatinib ditosylate was almost become amorphous since there were no characteristic peak in the XRD patterns.
About the micronization of nitrofurantoin, it could also be successfully micronized from original 202 μm to 2.93 μm at the optimal operating conditions. And from the result of XRD, the micronized nitrofurantoin had lower crystallinity compared with the original drug since several characteristic peaks were weakended or disappeared in the XRD patterns.
After the micronization process, the processed and unprocessed pharmaceuticals were tested using a dissolution tester. From the results of dissolution rate test, both the processed lapatinib ditosylate and nitrofurantoin has higher dissolution rate than the original drug.
Subjects
supercritical anti-solvent
micronization
amorphization
lapatinib
SDGs
Type
thesis
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