Formulation and In Vitro Evaluation of Taste- Masked Prednisolone Orodispersible Tablets
DOI:
https://doi.org/10.32007/jfacmedbagdad.2057Keywords:
External ionic gelation method,, oro- dispersible tablets,, prednisolone, , sodium alginate- beads, , taste masking.Abstract
Background: prednisolone is a corticosteroid with a very bitter taste acts as anti-inflammatory and immune suppressant drug and is used at any age.
Objective: To improve patient compliance by masking the bitter taste of the drug to be delivered as orodispersible tablets.
Methods: External ionic gelation using sodium alginate (0.5%w/v) and calcium chloride (1% w/v) in the presence of 0.5% w/v carbopol 940 was used to prepare taste-masked beads loaded with prednisolone to be compressed as orodispersible tablets.
Results: The bitter taste was masked by preparing beads composed of 1:1:1 (sodium alginate: Carbopol 940: prednisolone) releasing only 0.77 % of the drug in pH 6.8 (pH of the oral cavity).
The ODT prepared by direct compression using taste-masked beads equivalent to 5 mg PRD, 3% crospovidone, 2% PVP, 1% talc, 1% magnesium stearate, and a combination of Avcil® PH 102 and mannitol at (1:1) ratio was the optimum formula (T6) with the hardness of 3.9± 0.32 kg, friability 0.45%, thickness 2.5 ± 0.05 mm, % drug content 98.2% ± 1.8, wetting time 18.7 ± 1.3 sec, water absorption 41 ± 2.1%, disintegration time 15.3 ± 0.5 sec. and released only 0.75% ± 0.01 of PRD in an oral pH of 6.8 within one minute (indicating good taste masking). Its release in the stomach (pH 0.1N HCl) and intestine (pH 6.8) was continued for up to two hours.
Conclusion: it can be concluded that the external ionic gelation method was successful in masking the bitter taste of prednisolone and also can be formulated as taste-masked orodispersible tablets by direct compression method.
Received: Jan. 2023
Accepted: May 2023
Published: Oct.2023
Downloads
References
BNF. BNF81 for other requests email : Br Natl Formul. 2021;1500.
Celebioglu A, Wang N, Kilic ME, Durgun E, Uyar T. Orally Fast Disintegrating Cyclodextrin/Prednisolone Inclusion-Complex Nanofibrous Webs for Potential Steroid Medications. Mol Pharm. 2021; 18(12):4486-500. https://doi.org/10.1021/acs.molpharmaceut.1c00677
Suza H, Al-Khedairy E. Formulation and Evaluation of Prednisolone -Loaded Alginate Beads for Taste Masking. ejhm. 2023; 90(2): 2178-2186. https://doi.org/10.21608/ejhm.2023.285683.
Leong J, Lam W, Ho K et al. Advances in fabricating spherical alginate hydrogels with controlled particle designs by ionotropic gelation as encapsulation systems. Particuology. 2016; 24: 44-60. https://doi.org/10.1016/j.partic.2015.09.004.
Hazzaa S, Abd-Alhameed S. Formulation and evaluation of optimized zaltoprofen lyophilized. Iraqi J Pharm Sci, 2017;.26(1): 40-49. https://doi.org/10.31351/vol26iss1pp40-49.
Mali R, Pawar H, Mali K, Dias R. Fast disintegrating tablets of olmesartan medoxomil using solid dispersion technique. Asian J Pharm. 2017;11(2):S425-433.
Ghumman S, Mahmood A, Noreen S, Rana M, Hameed H, Ijaz B, et al. Formulation and evaluation of quince seeds mucilage - sodium alginate microspheres for sustained delivery of cefixime and its toxicological studies. Arab J Chem. 2022;15(6):1- 16. https://doi.org/10.1016/j.arabjc.2022.103811.
Alhagiesa A, Ghareeb M. Formulation and evaluation of nimodipine nanoparticles incorporated within orodispersible tablets. Int J Drug Deliv Technol. 2020;10(4):547-552.
Ehaasn M, Abd Al Hamid S. Formulation and evaluation of rosuvastin orodispersible tablet. Int J Pharm.2013, 5(12): 339-346.
Abdulqader A, .Al-Khedairy E. Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion. Iraqi J Pharm Sci. 2017;26(1):50-60.
https://doi.org/10.31351/vol26iss1pp50-60.
Abed K, Hussein A, Ghareeb M and Abdulrasool A. Formulation and Optimization of Orodispersible Tablets of Diazepam. AAPS PharmSciTech. 2010;11(1): 356- 361. https://doi.org/10.1208/s12249-010-9387-y.
Aulton M, Taylor K. Powder flow. In: Aulton's Pharmaceutics: The Design and Manufacture of Medicines. 5th ed. London: Elsevier Ltd; 2018.
Rada S, Kumar V. A review on Fast Dissolving Tablets: A new era of water less orally administered dosgeform. Ymer. 2022;21(8):1317-1342.
Abouzeid A, Essa E and Eldin E. Formulation and evaluation of mouth dispersible tablets of simvastatine using novel excipents. Biomedical European of and Pharmaceutical sciences .2019;6(6):532-541.
Nikam V, Shete S, Khapare J. Most promising solid dispersion technique of oral dispersible tablet. Beni-Suef Univ J Basic Appl Sci. 2020; 9(1). https://doi.org/10.1186/s43088-020-00086-4.
Trisopon K, Kittipongpatana N, Wattanaarsakit P, Kittipongpatana O. Formulation study of a co-processed, rice starch-based, all-in-one excipient for direct compression using the sedem-odt expert system. Pharmaceuticals. 2021; 14(10). https://doi.org/10.3390/ph14101047.
Driany R, Anwar E, Andrajati R, Hanafi M. Formulation of orodispersble tablet of luffa acutangula (L) roxb using co-processed via spray dried excepient. Innovare Academic Sciences. 2015;7(1).
The United State Pharmacopeia (USP) 37 NF 32. 2014.
Muhsin Z, Ghareeb M. Preparation and characterization of Oro-dispersible tablets of Bromhexine hydrochloride. J. Pharm. Sci. & Res. 2018;10(9): 2258- 2262.
Chen Y etal . Development of oral dispersible tablets containing prednisolone nanoparticles for the management of pediatric asthma. Dovepress. 2015;9:5815-5825. https://doi.org/10.2147/DDDT.S86075.
Pratap R, Kumar S. Formulation and Evaluation of Prednisolone Loaded Microsponges for Colon Drug Delivery: in-Vitro and Pharmacokinetic Study. Int J Pharm Sci Res. 2014;5(5):1994-2005.
Dave V, Yadav R, Ahuja R, Sahu A. Formulation and evaluation of orally dispersible tablets of Chlorpheniramine maleate by fusion method. Marmara Pharm J. 2017; 21: 67-77. https://doi.org/10.12991/marupj.259883.
Sivadasan D, Sultan M, Madkhali O, Javed S, Jabeen A. Formulation and in vitro evaluation of orodispersible tablets of fexofenadine hydrochloride. Trop J Pharm Res. 2020;19(5):919-25.
https://doi.org/10.4314/tjpr.v19i5.2.
Akdag Y, Gulsun T, Izat N, Cetin M, Oner L, Sahin S. Evaluation of preparation methods for orally disintegrating tablets. Med Sci. 2020; 9(1):259 . https://doi.org/10.5455/medscience.2019.08.9167.
Rowe R, Sheskey P and Quinn M. Handbook of pharmaceutical excipients. sixth edition, london, shigago, 2009.
Elgahmi S, Alrishei N, Algaraboly R, Altrablesy A, El-Mahdi I. The redesign of amoxicillin capsules as a tablet dosage form using direct compression. Libyan. Int Med Univ J. 2019;04(01):33-38. https://doi.org/10.4103/LIUJ.LIUJ_45_18.
Apeji Y, Olowosulu A. Quantifying the effect of glidant on the compaction and tableting properties of paracetamol granules. J Res Pharm. 2020;24(1):44-55. https://doi.org/10.35333/jrp.2020.112.
Chen P, Ansari M, Bokov D, Suksatan W, Rahman M, Sarjadi M. A review on key aspects of wet granulation process for continuous pharmaceutical manufacturing of solid dosage oral formulations. Arab J Chem. 2022;15:1-9. https://doi.org/10.1155/2022/1799772.
Smrdel P, Bogataj M, Mrhar A. The influence of selected parameters on the size and shape of alginate beads prepared by ionotropic gelation. Sci Pharm. 2008;76(1):77-89. https://doi.org/10.3797/scipharm.0611-07.
Nofrerias I, Nardi A, Sune-Pou M, Sune-Negre J, García-Montoya E, Perez-Lozano P, et al. Comparison between Microcrystalline Celluloses of different grades made by four manufacturers using the SeDeM diagram expert system as a pharmaceutical characterization tool. Powder Technol. 2019; 342: 780-788. https://doi.org/10.1016/j.powtec.2018.10.048.
Fernandes R, Regina M, Glenn G. Thermal, microstructural and spectroscopic analysis of Ca +2 alginate/ clay nanocomposite hydrogel beads. j.molliq. 2018; 265: 327-336. https://doi.org/10.1016/j.molliq.2018.06.005.
Thomas L, Khalil Y. Preparation and Evaluation of Atenolol Floating Beads as a Controlled Delivery System. Iraqi J Pharm Sci. 2011; 20(1):70-80. Available from: http://bijps.com/LionImages/News/70-80.pdf https://doi.org/10.31351/vol20iss1pp70-80.
Patel N, Lalwani D, Gollmer S, Injeti E, Sari Y, Nesamony J. Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation. Prog Biomater. 2016;5(2):117-133
https://doi.org/10.1007/s40204-016-0051-9.
Chakraborty S, Dinda SC, Patra CN, Khandai M. Fabrication and characterization of algino-carbopol microparticulate system of aceclofenac for oral sustained drug delivery. Int J Pharm Sci Rev Res.2010;4(2):192-199
Downloads
Published
Issue
Section
License
Copyright (c) 2023 Hiba mohammed Suza ali, Eman B. H. Al-Khedairy
This work is licensed under a Creative Commons Attribution 4.0 International License.
How to Cite
Creative Commons Attribution 4.0 International license..
