Peningkatan Kelarutan Ketokonazol dengan Teknik Dispersi Padat Menggunakan Eudragit® E 100

Authors

  • Angga Cipta Narsa Fakultas Farmasi, Universitas Mulawarman, Samarinda, Kalimantan Timur, Indonesia Author

Keywords:

ketoconazole, solid dispersion, Eudragit® E 100

Abstract

Ketoconazole is an antifungal azole synthetic which derivatived from imidazole. Ketoconazole is practically insoluble in water and its bioavailability depend on pH condition of the gastrointestinal tract. The purpose of the research is to increase the solubility of ketoconazole by solid dispersion method using Eudragit® E 100, PEG 6000, and glycerol. Solid dispersion was evaluated with respect to solubility, cristalinity, complexation and morphology of solid dispersion. The optimum formulation with the highest solubility was resulted by solid dispersion with ratio ketoconazole - Eudragit® E 100 - glycerol of 1:8:0.5. X-ray diffraction test revealed the change of crystalline ketoconazole and similar to Eudragit® E 100. This result was also supported by spectrum of infrared and endothermic peak of differential scanning calorimetry. Based on scanning electron microscopy morphology of pure Eudragit® E 100 and solid dispersion was similar. Solid dispersion of ketoconazole with Eudragit® E 100 and glycerol improved solubilty.

References

1.Chiou et al, 1971, Pharmaceutical Application of Solid Dispersion Systems, Journal of Pharmaceutical Sciences, 1281-1302.

2.Felisiak T, 2009, Solubility Enhancement, in: Eudragit®ApplicationGuidelines 11thed,. Evonik Rohm Gmbh, Darmstadt, 1-10

3.Heo M. Y. et al, 2005, Effect of Solubilizing and Microemulsifying

Excipients in Polyethylen Glycol 6000 Solid Dispersion on Enhanced Dissolution and Bioavailability of Ketoconazole, Arch. Pharm. Res., 28 (5) : 604-611.

4.Kumar P et al, 2011, Physicochemical Characterization and Release Rate Studies of Solid Dispersion of Ketoconazole with Pluronic F127 and PVP K-30, IJPR, 10 (4): 685-694.

5.Martin et al, 1993, Interfacial phenomenon In: Physical Pharmacy, 3rd edition, Lea and Febiger, Philadelphia. 362 – 392.

6.M.T. Esclusa-Diaz, M et al, 1996, Characterization and In Vitro Dissolution Behavior of Ketoconazole/β-and 2-Hydroxypropyl-β-Cyclodextrin Inclusion Coumpounds, Int. J. Pharm., 143, 203-210.

7.Leuner et al, 2000, Improving drug solubility for oral delivery using solid dispersions, Eur. J. Pharm. Biopharm. 50: 47-60.

8.Rowe, C.R. et al, 2006, Handbook of Pharmaceutical Exipients, 5th Edition, London: Pharmaceutical Press, Electronic version.

9.Six K et al, 2004, Increased physical stability and improved dissolution properties of itraconazole, a class II drug, by solid dispersions that combine fast- and slow-dissolving polymers, J. Pharm. Sci., Jan;93(1):124-31.

10.Sweetman, S. C., 2007, Martindale: The Complete Drug Reference, 35th ed., The Pharmaceutical Press, London.

11.The Council of Pharmaceutical Society of Great Britain, 2008, British Pharmacopeia 2008, vol 3, The Pharmaceutical Press, London.

Downloads

Published

2012-12-31

How to Cite

Peningkatan Kelarutan Ketokonazol dengan Teknik Dispersi Padat Menggunakan Eudragit® E 100. (2012). Journal of Tropical Pharmacy and Chemistry , 2(1), 1–7. https://jtpc.ff.unmul.ac.id/index.php/jtpc/article/view/39

Most read articles by the same author(s)