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KMID : 0614020060210010073
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Journal of Pharmaceutical Sciences (C.N.U.)
2006 Volume.21 No. 1 p.73 ~ p.78
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Formulation design and evaluation of itraconazole for oral dosage form
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Chang Hye-Jin
Kim Jeong-Soo
Lee Gye-Won
Jee Ung-Kil
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Abstract
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We prepared oral formulations of itraconazole by hot-melt process to increase dissolution rate of this drug. Oral liquid preparations of drug were prepared by melt method with lactic acid and blended with co-solvent, antioxidant and surfactant. Glycofurol and isopropyl alcohol were used as co-solvents, and ascorbic acid and as-corbyl palmitate were used as antioxidants, and TPGS and Gelucire 44/14 were used as surfactants. The final preparations contained 10% of itracnoazole as drug content percentage. The dissolution profiles of itraconazole from liquid preparation were determined at 37±0.5℃ at a stirring rate of 100 rpm using the paddle method. The oral absorption of itraconazole liquid preparation was studied in the rabbits. Major pharmacokinetic parameters (AUC_(0-48hr), C_(max), T_(max)) were calculated from the plasma concentration-time data. The dissolution rate of itraconazole was higher for itraconazole liquid preparation filled into a hard gelatin capsule with 90% release within 20min as compared to 20% for Sporanox capsules. Both the AUC_(0-48hr) and C_(max) values of liquid formulation prepared with isopropyl alcohol were higher than those of itraconazole prepared with glycofurol. The dissolution rate of itraconazole liquid preparation was higher as compared to Sporanox capsules. The bioavailability of drug prepared with isopropanol were higher than those of drug prepared with glycofurol.
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KEYWORD
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itraconazole, liquid preparations, pharmacokinetics, dissolutions, bioavailability
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