Kuldeep Singh, S. Jain, K. Razdan, Harmanpreet Singh, N. Sahajpal, Harjeet Singh, Amrinder Singh, Shubham Thakur
{"title":"Formulation and Evaluation of Ferrous Ascorbate Floating Tablets for the Treatment of Anaemia","authors":"Kuldeep Singh, S. Jain, K. Razdan, Harmanpreet Singh, N. Sahajpal, Harjeet Singh, Amrinder Singh, Shubham Thakur","doi":"10.2174/2210303109666190708151137","DOIUrl":null,"url":null,"abstract":"\n\nFerrous ascorbate (FA) is preferentially absorbed from the upper\ngastrointestinal (GI) track, and has low bioavailability due to less residence time of FA in upper GI\ntrack. In addition, FA has low solubility and stability at higher pH. The aim of this study was to prepare\ngastro-retentive tablets of FA in order to increase its gastric residence time and hence, bioavailability.\n\n\n\nFloating tablets of FA were prepared by wet granulation method using different retarding\npolymers, Povidone K30 as binder and sodium bicarbonate as effervescent agent. The prepared floating\ntablets were compared with immediate release (IR) tablets and characterized in detail for in vitro and in\nvivo studies.\n\n\n\nIn-vitro drug release study of the optimized batch showed 96% drug release in 12 h in 0.1 N\nHCl. The mechanism of drug release from the floating tablets was non-fickian and release kinetics was\nbest fit in peppas model. The gastric retention time of optimized was found to be significantly increased\n(6 h) in comparison with IR tablet (<1h). Further, bioavailability was also found significantly increased\n(>70%) in comparison with IR tablet (15-30%). X-ray studies carried on healthy rabbits suggested that\nthe optimized batch remained buoyant in gastric contents up to 6 h and pharmacokinetic study showed\nsustained released behaviour of optimized batch in comparison to conventional IR tablet.\n\n\n\nFloating tablet of FA improved the bioavailability of iron by increasing its gastric residence\ntime, hence it could be a better approach for treating iron deficiency and help in improving the\npatient compliance than IR tablets.\n","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2019-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Delivery Letters","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/2210303109666190708151137","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 1
Abstract
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.
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.
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.
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.