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Drug Delivery Letters

Editor-in-Chief

ISSN (Print): 2210-3031
ISSN (Online): 2210-304X

Research Article

Formulation and Evaluation of Ferrous Ascorbate Floating Tablets for the Treatment of Anaemia

Author(s): Kuldeep Singh, Subheet K. Jain*, Karan Razdan, Harmanpreet Singh, Nikhil S. Sahajpal, Harjeet Singh, Amrinder Singh and Shubham Thakur

Volume 9, Issue 4, 2019

Page: [299 - 307] Pages: 9

DOI: 10.2174/2210303109666190708151137

Price: $65

Abstract

Background and Objective: Ferrous ascorbate (FA) is preferentially absorbed from the upper gastrointestinal (GI) track, and has low bioavailability due to less residence time of FA in upper GI track. In addition, FA has low solubility and stability at higher pH. The aim of this study was to prepare gastro-retentive tablets of FA in order to increase its gastric residence time and hence, bioavailability.

Methods: Floating tablets of FA were prepared by wet granulation method using different retarding polymers, Povidone K30 as binder and sodium bicarbonate as effervescent agent. The prepared floating tablets were compared with immediate release (IR) tablets and characterized in detail for in vitro and in vivo studies.

Results: In-vitro drug release study of the optimized batch showed 96% drug release in 12 h in 0.1 N HCl. The mechanism of drug release from the floating tablets was non-fickian and release kinetics was best fit in peppas model. The gastric retention time of optimized was found to be significantly increased (6 h) in comparison with IR tablet (<1h). Further, bioavailability was also found significantly increased (>70%) in comparison with IR tablet (15-30%). X-ray studies carried on healthy rabbits suggested that the optimized batch remained buoyant in gastric contents up to 6 h and pharmacokinetic study showed sustained released behaviour of optimized batch in comparison to conventional IR tablet.

Conclusion: Floating tablet of FA improved the bioavailability of iron by increasing its gastric residence time, hence it could be a better approach for treating iron deficiency and help in improving the patient compliance than IR tablets.

Keywords: Ferrous ascorbate, anemia, gastroretentive, floating, pharmacokinetics, bioavailability.

Graphical Abstract
[1]
Brady, P.G. Iron deficiency anemia: a call for aggressive diagnostic evaluation. South. Med. J., 2007, 100(10), 966-967.
[http://dx.doi.org/10.1097/SMJ.0b013e3181520699] [PMID: 17943034]
[2]
Johnson, G.; Jacobs, P. Bioavailability and the mechanisms of intestinal absorption of iron from ferrous ascorbate and ferric polymaltose in experimental animals. Exp. Hematol., 1990, 18(10), 1064-1069.
[PMID: 2209759]
[3]
Pereira, D.I.A.; Bruggraber, S.F.A.; Faria, N.; Poots, L.K.; Tagmount, M.A.; Aslam, M.F.; Frazer, D.M.; Vulpe, C.D.; Anderson, G.J.; Powell, J.J. Nanoparticulate iron(III) oxo-hydroxide delivers safe iron that is well absorbed and utilised in humans. Nanomedicine (Lond.), 2014, 10(8), 1877-1886.
[http://dx.doi.org/10.1016/j.nano.2014.06.012] [PMID: 24983890]
[4]
Zariwala, M.G.; Elsaid, N.; Jackson, T.L.; Corral López, F.; Farnaud, S.; Somavarapu, S.; Renshaw, D. A novel approach to oral iron delivery using ferrous sulphate loaded solid lipid nanoparticles. Int. J. Pharm., 2013, 456(2), 400-407.
[http://dx.doi.org/10.1016/j.ijpharm.2013.08.070] [PMID: 24012860]
[5]
Hurrell, R.; Egli, I. Iron bioavailability and dietary reference values. Am. J. Clin. Nutr., 2010, 91(5), 1461S-1467S.
[http://dx.doi.org/10.3945/ajcn.2010.28674F] [PMID: 20200263]
[6]
Vikas, K.; Sinha, A.K.; Makkar, H.P.S. Dietary roles of phytate and phytase in human nutrition: a review. Food Chem., 2010, 120, 945-959.
[http://dx.doi.org/10.1016/j.foodchem.2009.11.052]
[7]
Mazur, A.; Green, S.; Carleton, A. Mechanism of plasma iron incorporation into Hepatic ferritin. J. Biochem., 1960, 595-603.
[8]
Srinivasu, B.Y.; Mitra, G.; Muralidharan, M. Beneficiary effect of nanosizing ferric pyrophosphate as food fortificant in iron deficiency anemia: evaluation of bioavailability, toxicity and plasma biomarker. RSC Advances, 2015, 5, 61678-61687.
[http://dx.doi.org/10.1039/C5RA07724A]
[9]
Wu, H.; Zhu, S.; Zeng, M.; Liu, Z.; Dong, S.; Zhao, Y.; Huang, H.; Lo, Y.M. Enhancement of non-heme iron absorption by anchovy (Engraulis japonicus) muscle protein hydrolysate involves a nanoparticle-mediated mechanism. J. Agric. Food Chem., 2014, 62(34), 8632-8639.
[http://dx.doi.org/10.1021/jf5018719] [PMID: 25074419]
[10]
Mottaghitalab, F.; Farokhi, M.; Shokrgozar, M.A.; Atyabi, F.; Hosseinkhani, H. Silk fibroin nanoparticle as a novel drug delivery system. J. Control. Release, 2015, 206, 161-176.
[http://dx.doi.org/10.1016/j.jconrel.2015.03.020] [PMID: 25797561]
[11]
Mandal, U.K.; Chatterjee, B.; Senjoti, F.G. Gastro-retentive drug delivery systems and their in vivo success: A recent update. Asian. J. Pharm. Sci., 2016, 11(5), 575-584.
[12]
Anand, T.; Rahi, M.; Sharma, P.; Ingle, G.K. Issues in prevention of iron deficiency anemia in India. Nutrition, 2014, 30(7-8), 764-770.
[http://dx.doi.org/10.1016/j.nut.2013.11.022] [PMID: 24984990]
[13]
Beutler, E. History of iron in medicine. Blood Cells Mol. Dis., 2002, 29(3), 297-308.
[http://dx.doi.org/10.1006/bcmd.2002.0560] [PMID: 12547220]
[14]
Nielsen, O.H.; Soendergaard, C. Vikner; M.E.; Weiss, G. Rational Management of Iron-Deficiency Anaemia in Inflammatory Bowel Disease. J. Nutr., 2018, 10, 1-25.
[15]
Hanaa, E.; Sayed, A.; Eman, A.; Kawkab, A. Treatment of anemia progression via magnetite and folate nanoparticles in vivo; ISRN Nanotechnol, 2014, pp. 1-13.
[16]
Mehta, B.C. Failure of oral iron therapy in treatment of iron deficiency anemia: pharmaceutical iatrogenic cause. Indian J. Med. Sci., 2001, 55(3), 157-158.
[PMID: 11482169]
[17]
Ebube, N.K.; Hikal, A.H.; Wyandt, C.M.; Beer, D.C.; Miller, L.G.; Jones, A.B. Sustained release of acetaminophen from heterogeneous matrix tablets: Influence of polymer ratio, polymer loading, and co-active on drug release. Pharm. Dev. Technol., 1997, 2(2), 161-170.
[http://dx.doi.org/10.3109/10837459709022621] [PMID: 9552442]
[18]
Cooper, J.; Gunn, C. Powder flow and compaction: Tutorial pharmacy, 6th ed; CBS Publishers and Distributiors: New Delhi, 1986, pp. 211-213.
[19]
Baskar, G.V.; Narayanan, N.; Gaikwad, R.; Abdul, S. Formulation and evaluation of gastro-retentive floating multi-particulate system of metoprolol tartarate. Trop. J. Pharm. Res., 2010, 9, 181-186.
[http://dx.doi.org/10.4314/tjpr.v9i2.53707]
[20]
Al-Taani, B.M.; Tashtoush, B.M. Effect of microenvironment pH of swellable and erodable buffered matrices on the release characteristics of diclofenac sodium. AAPS PharmSciTech, 2003, 4(3)E43
[http://dx.doi.org/10.1208/pt040343] [PMID: 14621975]
[22]
Ravindran, V.K.; Vasa, S.; Subadhra, S.; Banji, D.; Banji, O.; Rao, Y.M. Comparative study of mucoadhesive polymers carbopol 974P and sodium carboxymethyl cellulose for single unit dosage of imatinib mesylate. Malays. J. Pharm. Sci., 2012, 10(1), 61-77.
[23]
Baskar, G.V.; Narayanan, N.; Gaikwad, R.; Abdul, S. Formulation and evaluation of gastro-retentive floating multi-particulate system of metoprolol tartarate. Trop. J. Pharm. Res., 2010, 9(2), 181-186.
[http://dx.doi.org/10.4314/tjpr.v9i2.53707]
[24]
Thakar, K.; Joshi, G.; Sawant, K.K. Bioavailability enhancement of baclofen by gastroretentive floating formulation: statistical optimization, in vitro and in vivo pharmacokinetic studies. Drug Dev. Ind. Pharm., 2013, 39(6), 880-888.
[http://dx.doi.org/10.3109/03639045.2012.709249] [PMID: 22901056]
[25]
Ahmed, Y.; Hashem, F.; Nasr, M. Preparation and Evaluation of Iron oxide Nanoparticles for Treatment of Iron Deficiency Anemia. Int. J. Pharm. Pharm. Sci., 2018, 10, 142-146.
[http://dx.doi.org/10.22159/ijpps.2018v10i1.22686]

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