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Abstract

Eplerenone is a selective mineralocorticoid receptor antagonist employed to manage hypertension, central serous retinopathy, and chronic heart failure. It has a highly bitter taste, which reduces patient compliance with the drug.

The aim of this study was masking the very bitter taste of the eplerenone to improve patient compliance especially for geriatric patient.

The medication was encapsulated utilizing the ionic gelation process, in which a 1% w/w sodium alginate solution was utilized to form egg box structures.Two different concentrations of CaCl2 (0.5.1%w/v) were used as cross-linkers, and different drug: polymer ratios were tested. The formulas were evaluated based on their physical appearance, percentage yield, percentage drug loading, and in-vitro taste masking. The optimum formula (F4)was selected and characterized using Fourier-transform infrared spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and Energy Dispersive Spectroscopy (EDS).

Finally, this study suggests that the ionic gelation approach effectively masks the intense bitterness by lowering the drug's release through the mouth pH 6.8 within one minute. The optimum formula, F4, reduced eplerenone release to 3.2% as compared to pure eplerenone (57%), under similar conditions.

References

[1] Kafeef HK, Rajab NA. Eplerenone crystal nanosuspension for solubility enhancement: preparation and evaluation. Maaen J Med Sci 2023;2:73e80. https://doi.org/10.55810/ 2789-9136.1024.

[2] Japanese pharmacopeia. eighteenth ed. Tokyo Ministry of Health, Labour and Welfare;

[3] Łętocha A, Miastkowska M, Sikora E. Preparation and characteristics of alginate microparticles for food, pharmaceutical and cosmetic applications. Polymers 2022;14(18): 3834. https://doi.org/10.3390/polym14183834.

[4] Braccini I, Pe Arez S. Molecular basis of Ca2þ-induced gelation in alginates and pectins: the egg-box model revisited. Biomacromolecules 2001;2:1089e96.

[5] Suzi HM, Al-Khedairy EB. Formulation and in vitro evaluation of taste-masked prednisolone orodispersible tablets. J Fac Med 2023;65(3):192e8. https://doi.org/10.32007/ jfacmedbagdad.2057.

[6] Aldawsari MF, et al. Development and characterization of calcium-alginate beads of apigenin: invitro antitumor, antibacterial and antioxidant activities. Mar Drugs 2021;19:467. Q7 https://doi.org/10.3390/md19080467.

[7] Ahmed KK, Kassab HJ, Al Ramahi IJ, Alwan ZS. Taste masking of steroids for oral formulations. Turk J Pharm Sci 2023;20(6):352. https://doi.org/10.4274/tjps.galenos.2023.24968.

[8] Ali HM, Al-Khedairy EB. Formulation and evaluation of prednisolone-loaded alginate beads for taste masking. Egypt J Hosp Med 2023;90(2):2178e86. https://doi.org/10.21608/ EJHM.2023.285683.

[9] Wong RS, Dodou K. Effect of drug loading method and drug physicochemical properties on the material and drug release properties of poly (ethylene oxide) hydrogels for transdermal delivery. Polymers 2017;19;9(7):286. https://doi.org/10.3390/ polym9070286.

[10] Sharma M, Jain K, Dev SK, Choudhury PK. Formulation and evaluation of sodium alginate beads by emulsion gelation method. Asian J Pharm 2017;11(1):101e6. https://doi.org/ 10.22377/AJP.V11I01.1096.

[11] Sarecka B, Balwierz R, Ostrozka A, Dyja R, Lukowiec D, Jankowski A. Scanning electron microscopy and X-ray energy dispersive spectroscopyeuseful tools in the analysis of pharmaceutical products. J Phys 2017;931(1):012008. https://doi.org/10.1088/1742-6596/931/1/012008.

[12] Camus P, Buchhold R. Using accurate solid angle tools when comparing EDS detector geometries. Microsc Microanal 2014;20(3):900e1. https://doi.org/10.1017/S1431927614006229. [13] Thomas L, Khalil Y. Preparation and evaluation of atenolol floating beads as a controlled delivery system. Iraqi J Pharm Sci 2011;20(1):70e80. https://doi.org/10.31351/vol20iss1pp70- 80.

[14] Ali W, Mahmood A, Sabry H, et al. Preparation and evaluation of controlled release calcium alginate beads containing mefenamic acid. Al Mustansiriyah J Pharm Sci 2019;19(2): 9e16. https://doi.org/10.32947/ajps.v19i2.550.

[15] Deniz E, Toprak C, Gün G. Investigation of dry granulation and wet granulation effect on dissolution profile of the developed film coated tablets containing eplerenone. J Drug Res Dev 2021;7(2). https://doi.org/10.16966/2470-1009.164. 2470-1009.

[16] Kusuktham B, Prasertgul J, Srinun P. Morphology and property of calcium silicate encapsulated with alginate beads. Silicon 2014;6(3):191e7. https://doi.org/10.1007/s12633-013- 9173-z.

[17] Kaur N, Singh B, Sharma S. Hydrogels for potential food application: effect of sodium alginate and calcium chloride on physical and morphological properties. Pharm Innov 2018;7(7):142e8.

[18] Scoutaris N, Vithani K, Slipper I, Chowdhry B, Douroumis D. SEM/EDX and confocal Raman microscopy as complementary tools for the characterization of pharmaceutical tablets. Int J Pharm 2014;470(1e2):88e98. https://doi.org/10.1016/ j.ijpharm.2014.05.007.2021940e942.pdf.

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