Browse > Article
http://dx.doi.org/10.4333/KPS.2002.32.4.299

Formulation of Liquid Oral Preparations Containing Itraconazole  

Jung, Ki-Seop (College of Pharmacy, Sungkyunkwan University)
Hong, Ji-Woong (College of Pharmacy, Sungkyunkwan University)
Choi, Ki-Song (College of Pharmacy, Sungkyunkwan University)
Chi, Sang-Cheol (College of Pharmacy, Sungkyunkwan University)
Park, Eun-Seok (College of Pharmacy, Sungkyunkwan University)
Publication Information
Journal of Pharmaceutical Investigation / v.32, no.4, 2002 , pp. 299-303 More about this Journal
Abstract
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.
Keywords
Itraconazole; Liquid oral preparation; Solubility; Poloxamer;
Citations & Related Records
연도 인용수 순위
  • Reference
1 Sepcification Report No. A163 (860516) - R51211, Janssen Pharmaceutica
2 A.H. Kibbe, Handbook of Pharmaceutical Excipients, 3rd Ed., Pharmaceutical Press, London, United Kingdom, 41-43 (2000)
3 P. Simamora, M. Alvarez, S.H. Yalkowsky, Solubilization of rapamycin, Int. J. Pharm., 213, 25-29 (2001)   DOI   ScienceOn
4 H.-J. Kim, K.A. Yoon, M. Hahn, E.-S. Park, S.-C. Chi, Preparation and in vitro evaluation of self-microemulsifying drug delivery systems containing idebenone, Drug Dev. Ind. Pharm., 26, 523-529 (2000)   DOI   ScienceOn
5 D.W. Warnock, Itraconazole and fluconazole: new drugs for deep fungal infection, J. Antimicro. Chemother., 24, 275-277 (1989)   DOI
6 B.L.E. Colette, V. Geert, T. Dany, Antifungal compositions of improved bioavailability, US2001007678 (2001)
7 M. Skinner, I. Kanfer, Comparative bioavailability of josamycin, a macrolide antibiotic, from a tablet and solution and the influence of dissolution on in vivo release, Biopharm. Drug Dispos., 19, 21-29 (1998)   DOI   ScienceOn
8 I. Setnikar, K. Schmid, L.C. Rovati, B. Vens-Cappell, D. Mazur, I. Kozak, Bioavailability and pharmacokinetic profile of dihydroergotoxine from a tablet and from an oral solution formulation, Arzneimittelforschung, 51, 2-6 (2001)
9 T. Gershanik, S. Benita, Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs, Eur, J. Pharm. Biopharm., 50, 179-188 (2000)   DOI   ScienceOn
10 J.A. Barone, B.L. Moskovitz, J. Guarnier, A.E. Hassell, J.L. Colaizzi, R.H. Bierman, L. Jessen, Enhanced bioavailability of itraconazole in hydroxypropyl-beta-cyclodextrin solution versus capsules in healthy volunteers, Antimicrob. Agents Chemother., 42, 1862-5 (1998)
11 A.K. Singla, A. Garg, D. Aggarwal, Paclitaxel and its formulations, Int, J. Pharm., 235, 179-192 (2002)   DOI   ScienceOn
12 M. Trotta, M. Gallaratea, F. Pattarinob, S. Morelb, Emulsions containing partially water-miscible solvents for the preparation of drug nanosuspensions, J. Control. Rel., 76, 119-128 (2001)   DOI   ScienceOn