• 약학회지
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• 제44권6호
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• pp.528-533
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• 2000

This study was to develop an effective itraconazole liquid preparation which exhibits an enhanced bioavailability. The solubility of itraconazole was increased (72-fold) in itraconazole liquid preparation as compared with itraconazole powder. The dissolution rate of itraconazole was higher for itraconazole liquid preparation filled into a hard gelatin capsule with 90% release within 20 min as compared to 55% for $Sporanox^{\circledR}$capsules. The oral absorption of itraconazole liquid preparation and $Sporanox^{\circledR}$tablets were studied in the rat. The area under the concentration-time curve $(AUC_{0-24hr})$ of itraconazole liquid preparation ($90.25\;{\pm}\;8.36\;{\mu}g{\cdot}hr/ml$) increased by 6.2 times compared to that of Sporanox tablets ($14.58\;{\pm}\;1.26\;{\mu}g{\cdot}hr/ml$) after oral administration of itraconazole 15 mg/rat each. $C_{max}$ also increased to $6.87\;{\pm}\;1.15\;{\mu}g/ml$ after administration of liquid preparation $1.58\;{\pm}\;0.16\;{\mu}g/ml$ of $Sporanox^{\circledR}$tablets. These results indicate that in vivo bioavailability of itraconazole liquid preparation was significantly enhanced as compared with $Sporanox^{\circledR}$tablets.

• Journal of Pharmaceutical Investigation
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• 제32권4호
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• pp.299-303
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• 2002

The oral bioavailability of itraconazole is variable and low in fasting state. This is mainly due to the low solubility of this drug. Bioavailability can be improved by changing the formulation and it is general that the liquid preparations show greater bioavailability than the solid dosage forms such as tablets and capsules do. Benzyl alcohol-water binary mixture showed the excellent solubilizing capacity for itraconazole but the release of the drug from the preparation needs to be enhanced. In this study, various nonionic surfactants and hydrophilic polymers, poloxamers, were screened to investigate their effects on the releasε of itraconazole from the liquid preparations. Poloxamer 407 showed the most enhancing effect on the drug release and the release rate was proportional to thε amount of poloxamer 407 added. A liquid preparation of itraconazole, consisting of benzyl alcohol/water/poloxamer 407 ternary solvent system, releasεd more than 80% of the total drug amount at 5 min and showεd the possibility of a new formulation development.

• Bulletin of the Korean Chemical Society
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• 제27권2호
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• pp.291-294
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• 2006

A highly sensitive high-performance liquid chromatographic-tandem mass spectrometric method (HPLC-MSMS) has been developed to quantify itraconazole in human plasma for the purpose of pharmacokinetic studies. Sample preparation was carried out by liquid-liquid extraction using loratadine as an internal standard. Chromatographic separation used a YMC $C_{18}$ column, giving an extremely fast total run time of 3 min. The method was validated and used for the bioequivalence study of itraconazole tablets in healthy male volunteers (n = 31). The lower limit of detection proved to be 0.2 ng /mL for itraconazole.