Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

Background  and  Objectives:  The  prevention  and  treatment  of  peptic  ulcers  has  become  an important challenge in the current medicine  world.   Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time.  Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated. Materials  and  Methods:  Nine  batches  of  the  light  liquid  paraffin  entrapped  emulsion  gel  beads were  prepared  by  a  new  emulsion  gelation  technique  using  sodium  alginate  and  xanthan  gum  as polymers.  The  polymeric  solution  was  extruded  into  Calcium  chloride  solution  by  the  use  of  21G needles.  Morphology  of  beads,  drug  content,  drug  entrapment  efficiency,  floating  lag  time  and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR. Results: Mean  surface  diameter  were  between  1.220  ±  2.259%  (F1)  to  1.230  ±  2.316%  (F9)  and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric  fluid  at  37oC.  The  drug  content  and  drug  entrapment efficiency  among  the  formulations  were  between  17.48%~19.68%  and  71.06%  ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile. Conclusion: The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug.  Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12

[1]  Pharmaceutical Press,et al.  Handbook of Pharmaceutical Excipients , 2012 .

[2]  P. Opanasopit,et al.  Biodegradable alginate microparticles developed by electrohydrodynamic spraying techniques for oral delivery of protein , 2008, Journal of microencapsulation.

[3]  D. Patel,et al.  Floating granules of ranitidine hydrochloride-gelucire 43/01: Formulation optimization using factorial design , 2007, AAPS PharmSciTech.

[4]  A. Bhosale,et al.  Recent advances in proton pump inhibitors and management of acid-peptic disorders. , 2007, Bioorganic & medicinal chemistry.

[5]  D. Bandyopadhyay,et al.  Involvement of reactive oxygen species in gastric ulceration: protection by melatonin. , 2002, Indian journal of experimental biology.

[6]  J. H. Baron,et al.  Pathophysiology of duodenal and gastric ulcer and gastric cancer , 2001, BMJ : British Medical Journal.

[7]  L. Lacey,et al.  Colonic metabolism of ranitidine: implications for its delivery and absorption. , 2001, International journal of pharmaceutics.

[8]  Donald L. Wise,et al.  Handbook of Pharmaceutical Controlled Release Technology , 2000 .

[9]  Brahma N. Singh,et al.  Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[10]  T. Bhardwaj,et al.  Natural Gums and Modified Natural Gums as Sustained-Release Carriers , 2000, Drug development and industrial pharmacy.

[11]  J. Pentland.  Elements of Pharmacology , 1888, Edinburgh Medical Journal.

[12]  R. Bhimavarapu,et al.  Design , development and in vitro evaluation of gastro retentive alginate floating beads for ranitidine hydrochloride , 2013 .

[13]  Ey,et al.  Formulation and evaluation of floating microbeads of ciprofloxacinHCl by emulsion gelation method , 2013 .

[14]  A. Tiwari,et al.  FORMULATION AND EVALUATION OF FLOATING MICROSPHERE H 2 RECEPTOR BLOCKER RANITIDINE HCl BY IONIC GELATION METHOD , 2012 .

[15]  A. Khan,et al.  Formulation and Evaluation of Floating beads of Verapamil hydrochloride , 2011 .

[16]  H. Sharma,et al.  Preparation and in vitro evaluation of enteric controlled release Pantoprazole loaded microbeads using natural mucoadhesive substance from Dillenia indica L. , 2010 .

[17]  D. Chandra,et al.  FORMULATION AND EVALUATION OF OIL ENTRAPPED FLOATING ALGINATE BEADS OF RANITIDINE HYDROCHLORIDE , 2009 .

[18]  C. T. Rhodes,et al.  Optimization of Sotalol Floating and Bioadhesive Extended Release Tablet Formulations , 1995 .

[19]  M. Langman.  Histamine H2 antagonists. , 1979, The Practitioner.