Preparation of amorphous solid dispersion of azithromycin dihydrate with hydroxypropyl methylcellulose (HPMC)
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Abstract
The aim of present study is to develop solid dispersion system of azithromycin dihydrate with hydroxypropyl methylcellulose E5 LV (HPMC) for improving the dissolution rate of azithromycin dihydrate. Amorphous solid dispersions were prepared by solvent method at 1:1; 1:2 and 2:1 (w/w) drug to polymer ratios. Solid state properties of amorphous solid dispersion were evaluated by X-ray powder diffraction (XRPD), scanning electron microscopy and spectroscopy FT-IR. Furthermore, the dissolution rate profile was investigated by type II USP dissolution apparatus. Based on X-ray powder diffractometry analysis, azithromycin dihydrate was transformed partially from the crystalline phase to the amorphous state as confirmed by significant reduction of the crystalline peaks intensity. FT-IR spectroscopy analysis revealed the absence of chemical interaction between azithromycin dihydrate and HPMC. The dissolution rate of azithromycin dihydrate from amorphous solid dispersion was substantially higher than azithromycin dihydrate intact and its physical mixture. The dissolution rate of azithromycin dihydrate increased with an increasing drug to polymer ratio.
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References
Adeli, E., & Mortazavi, S. A. (2014). Design, formulation and evaluation of Azithromycin binary solid dispersions using Kolliphor series for the solubility and in vitro dissolution rate enhancement. Journal of Pharmaceutical Investigation, 44(2), 119-131.
Adeli, E. (2014). A comparative evaluation between utilizing SAS supercritical fluid technique and solvent evaporation method in preparation of Azithromycin solid dispersions for dissolution rate enhancement. The Journal of Supercritical Fluids, 87, 9-21.
Vogt, M., Kunath, K., & Dressman, J. B. (2008). Dissolution enhancement of fenofibrate by micronization, cogrinding and spray-drying: comparison with commercial preparations. European Journal of Pharmaceutics and Biopharmaceutics, 68(2), 283-288.
Dwichandra Putra, O., Yonemochi, E., & Uekusa, H. (2016). Isostructural Multicomponent Gliclazide Crystals with Improved Solubility. Crystal Growth & Design, 16(11), 6568-6573.
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.
Chiou, W. L., & Riegelman, S. (1971). Pharmaceutical applications of solid dispersion systems. Journal of pharmaceutical sciences, 60(9), 1281-1302.
Serajuddin, A. (1999). Solid dispersion of poorly waterâ€soluble drugs: Early promises, subsequent problems, and recent breakthroughs. Journal of pharmaceutical sciences, 88(10), 1058-1066.
Lipinski, C. A. (2000). Drug-like properties and the causes of poor solubility and poor permeability. Journal of pharmacological and toxicological methods, 44(1), 235-249.
Kalepu, S., & Nekkanti, V. (2015). Insoluble drug delivery strategies: review of recent advances and business prospects. Acta Pharmaceutica Sinica B, 5(5), 442-453.
Leuner, C., & Dressman, J. (2000). Improving drug solubility for oral delivery using solid dispersions. European journal of Pharmaceutics and Biopharmaceutics, 50(1), 47-60.
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.
Yadav, P. S., Kumar, V., Singh, U. P., Bhat, H. R., & Mazumder, B. (2013). Physicochemical characterization and in vitro dissolution studies of solid dispersions of ketoprofen with PVP K30 and d-mannitol. Saudi Pharmaceutical Journal, 21(1), 77-84.
El-Badry, M. (2011). Physicochemical characterization and dissolution properties of meloxicam-gelucire 50/13 binary systems. Scientia pharmaceutica, 79(2), 375-386.
Jung, J. Y., Yoo, S. D., Lee, S. H., Kim, K. H., Yoon, D. S., & Lee, K. H. (1999). Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique. International journal of pharmaceutics, 187(2), 209-218.