PENINGKATAN KELARUTAN KETOKONAZOL DENGAN TEKNIK DISPERSI PADAT MENGGUNAKAN EUDRAGIT® E 100

  • Angga Cipta Narsa
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.

Keywords : ketoconazole, solid dispersion, Eudragit® E 100

 

ABSTRAK

Ketokonazol merupakan zat antijamur sintetik golongan azol yang merupakan turunan imidazol.Ketokonazol praktis tidak larut dalam air dan ketersediaan hayati melalui rute oral sangat beragam tergantung dari kondisi pH saluran pencernaan.Penelitian ini bertujuan untuk meningkatkan kelarutan ketokonazol dengan cara pembuatan dispersi padat mengunakan Eudragit® E 100, PEG 6000, serta gliserol. Dispersi padat di evaluasi dengan uji kelarutan jenuh, kristalinitas, kompleksasi, dan morfologinya.Formula optimal dengan peningkatan kelarutan tertinggi dihasilkan oleh perbandingan dispersi padat ketokonazol - Eudragit® E 100 - gliserol 1:8:0,5. Pengujian difraksi sinar-X menunjukkan adanya perubahan kristalinitas ketokonazol yaitu sama seperti Eudragit® E 100.Hasil ini juga didukung oleh hasil pengujian spetkrofotometer infra merah dan puncak endotermik differential scanning calorimetry.Berdasarkan hasil scanning electrom microscopyterlihat morfologi dari Eudragit® E 100 murni dan dispersi padatnya yang hampir sama..Pembentukan dispersi padat ketokonazol dengan Eudragit® E 100 dan gliserol dapat meningkatkan kelarutan.

Kata Kunci : ketokonazol, dispersi padat, Eudragit® E 100

Downloads

Download data is not yet available.

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.
Published
2012-12-31
How to Cite
Narsa, A. C. (2012). PENINGKATAN KELARUTAN KETOKONAZOL DENGAN TEKNIK DISPERSI PADAT MENGGUNAKAN EUDRAGIT® E 100. Journal of Tropical Pharmacy and Chemistry, 2(1), 1-7. https://doi.org/10.25026/jtpc.v2i1.42