• Journal of the Korean Chemical Society
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• v.43 no.6
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• pp.676-681
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• 1999

Itraconazole is an important drug for oral treatment of histoplasmosis and blastomycosis. ltraconazole has been the targets of many synthetic efforts due to their diverse antifungal activities. ln this study, an efficient synthetic route for Itraconazole intermediates has been developed using new procedures. Also, ltraconazole analogues introducing 2- and 3-methoxy group instead of ltraconazole intermediates with 4-methoxy group were synthesized.

• KSBB Journal
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• v.18 no.1
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• pp.1-7
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• 2003

Screening of a strain was carried out to produce an enantioselective lipase toward the precursor of ltraconazole as azole-containg compounds, which are well known as antifungal drug agents. An Acinetobacter sp. SY-01 strain which can selectively hydrolyze the racemic substrates was isolated and the racemic substrate was resolved to the S-ester in 95.6% enantiomeric excess after 74.8% hydrolysis. The optimum temperature and pH for the conversion were $50^{\circ}C$, pH 7.0. However, the temperature and pH had no effect on the enantiomeric excess. Addition of solvents decreased the conversion and slightly increased the enantiomeric excess. However, the kind of solvents had no effect on enantiomeric excess. The substrate concentration decrease enantiomeric excess and this is confirmed by the products generated from hydrolysis, and also enantiomeric excess could be increased by the removal of reaction products.

• Applied Chemistry for Engineering
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• v.17 no.1
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• pp.106-110
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• 2006

If drugs are made from nanoparticles, their formulations can be more effective than the conventional ones. Especially, water insoluble drugs having low absorption rates into our body could show improvement in their adsorption and bioavailability by decreasing their particle sizes to nanometers. In this study, polyvinylpyrrolidone (PVP) and various sugars were employed as stabilizers for the nanoparticles of a water insoluble drug, Itraconazole. Nanoparticles were successfully produced by the wet slurry process for five days. Then, spray drying converted the aqueous dispersions into dry powders, and the redispersibility of dried nanoparticles into water was investigated. The effects of temperature, pressure, and flow rate were studied to understand the importance of processing variables on redispersibility. It was found in particle size analysis that nanoparticles containing sugars have better redispersibility than those without sugars. Additionally, the mainly spherical morphology of dried nanoparticles was identified by SEM (Scanning Electron Microscopy) and AFM (Atomic Force Microscopy).