Dissolution rate improvement of genistein by amorphous solid dispersion in PVP K-30
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Abstract
Amorphous solid dispersions of a poorly water-soluble drug genistein in PVP K-30 were prepared by solvent co-evaporation technique using organic solvent methanol. Solid dispersions system was prepared with several variations of drug to polymer 2:1, 1:1 dan 1:2 w/w. Solid state properties of solid dispersion system were evaluated by powder X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry, and microscopic SEM. Dissolution rate profile were conducted in distilled water medium by using dissolution tester apparatus type II USP. Base on X-ray diffractometry analysis, differential scanning calorimetry and microscopic SEM, crystalline phase of genistein decreased in crystallinity index and formation of amophous state. Dissolution rate profile showed that genistein in amorphous solid dispersion had a faster dissolution rate in comparison to intact genistein. This study proved that preparation of solid dispersion of genistein in PVP K-30 is an effective approach to improve dissolution rate of genistein.
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References
Lipinski, C. A. (2000). Drug-like properties and the causes of poor solubility and poor permeability. Journal of harmacological and oxicological ethods, 44(1), 235–249.
Setyawan, D., Fadhil, A. A., Juwita, D., Yusuf, H., & Sari, R. (2017). Enhancement of solubility and dissolution rate of quercetin with solid dispersion system formation using hydroxypropyl methyl cellulose matrix. Thai Journal of Pharmaceutical Sciences, 41(3), 112–116.
Amidon, G. L., Lennernäs, H., Shah, V. P., & Crison, J. R. (1995). A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharmaceutical esearch, 12(3), 413–420.
Bhatt, P. M., Ravindra, N. V., Banerjee, R., & Desiraju, G. R. (2005). Saccharin as a salt former. Enhanced solubilities of saccharinates of active pharmaceutical ingredients. Chemical Communications, (8), 1073–1075.
Putra, O. D., Umeda, D., Nugraha, Y. P., Furuishi, T., Nagase, H., Fukuzawa, K., ... & Yonemochi, E. (2017). Solubility improvement of epalrestat by layered structure formation via cocrystallization. CrystEngComm, 19(19), 2614–2622.
Zaini, E., Wahyu, D., Octavia, M. D., & Fitriani, L. (2017). Influence of milling process on efavirenz solubility. Journal of Pharmacy & Bioallied Sciences, 9(1), 22–25.
Srinarong, P., de Waard, H., Frijlink, H. W., & Hinrichs, W. L. (2011). Improved dissolution behavior of lipophilic drugs by solid dispersions: the production process as starting point for formulation considerations. Expert pinion on rug elivery, 8(9), 1121–1140.
Zielonka, J., Ge̦bicki, J., & Grynkiewicz, G. (2003). Radical scavenging properties of genistein. Free Radical Biology and Medicine, 35(8), 958–965.
Arliss, R. M., & Biermann, C. A. (2002). Do soy isoflavones lower cholesterol, inhibit atherosclerosis, and play a role in cancer prevention?. Holistic Nursing Practice, 17(1), 40–48.
Motlekar, N., Khan, M. A., & Youan, B. B. C. (2006). Preparation and characterization of genistein containing poly (ethylene glycol) microparticles. Journal of pplied olymer cience, 101(3), 2070–2078.
Tang, J., Xu, N., Ji, H., Liu, H., Wang, Z., & Wu, L. (2011). Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment. International ournal of anomedicine, 6, 2429–2435.
Xavier, C. R., Silva, A. P. C., Schwingel, L. C., Borghetti, G. S., Koester, L. S., Mayorga, P., ... & Sinisterra, R. D. (2010). Improvement of genistein content in solid genistein/-cyclodextrin complexes β. QuÃmica Nova, 33(3), 587–590.
Kwon, S. H., Kim, S. Y., Ha, K. W., Kang, M. J., Huh, J. S., Kim, Y. M., ... & Lee, J. (2007). Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery. Archives of Pharmacal esearch, 30(9), 1138–1143.
Fitriani, L., Haqi, A., & Zaini, E. (2016). Preparation and characterization of solid dispersion freeze-dried efavirenz–polyvinylpyrrolidone K-30. Journal of Advanced Pharmaceutical Technology & Research, 7(3), 105–109.
Zaini, E., Halim, A., Soewandhi, S. N., & Setyawan, D. (2011). Peningkatan laju pelarutan trimetoprim melalui metode ko-kristalisasi dengan nikotinamida. Jurnal Farmasi Indonesia, 5(4), 205–212.
El-Badry, M. (2011). Physicochemical characterization and dissolution properties of meloxicam-gelucire 50/13 binary systems. Scientia Pharmaceutica, 79(2), 375–386.
Wu, K. E., Li, J., Wang, W., & Winstead, D. A. (2009). Formation and characterization of solid dispersions of piroxicam and polyvinylpyrrolidone using spray drying and precipitation with compressed antisolvent. Journal of Pharmaceutical Sciences, 98(7), 2422–2431.
Vasconcelos, T., Sarmento, B., & Costa, P. (2007). Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discovery Today, 12(23), 1068–1075.
Konno, H., Handa, T., Alonzo, D. E., & Taylor, L. S. (2008). Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine. European Journal of Pharmaceutics and Biopharmaceutics, 70(2), 493–499.