title: Design and in vitro/in vivo evaluation of sustained-release floating tablets of itopride hydrochloride.
abstract: OBJECTIVE
  The aim of the present study was to improve the bioavailability of itopride (ITO) and sustain its action by formulating as a floating dosage form.
  
  
  METHODS
  Sustained-release floating tablets of ITO hydrochloride (HCl) were prepared by direct compression using different hydrocolloid polymers such as hydroxypropyl methylcellulose and ethylcellulose and/or methacrylic acid polymers Eudragit RSPM and Carbopol 934P. The floating property was achieved using an effervescent mixture of sodium bicarbonate and anhydrous citric acid (1:1 mol/mol). Hardness, friability, content uniformity, and dissolution rate of the prepared floating tablets were evaluated. The formulation F10composed of 28.5% Eudragit RSPM, 3% NaHCO3, and 7% citric acid provided sustained drug release.
  
  
  RESULTS
  In vitro results showed sustained release of F10where the drug release percentage was 96.51%±1.75% after 24 hours (P=0.031). The pharmacokinetic results indicated that the area under the curve (AUC0-∞) of the prepared sustained-release floating tablets at infinity achieved 93.69 µg·h/mL compared to 49.89 µg·h/mL for the reference formulation (Ganaton®) and the relative bioavailability of the sustained-release formulation F10increased to 187.80% (P=0.022).
  
  
  CONCLUSIONS
  The prepared floating tablets of ITO HCl (F10) could be a promising drug delivery system with sustained-release action and enhanced drug bioavailability.
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut.
authors.forename: Sayed M
authors.initials: SM
authors.lastname: Ahmed
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt.
authors.forename: Adel
authors.initials: A
authors.lastname: Ahmed Ali
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia.
authors.forename: Ahmed Ma
authors.initials: AM
authors.lastname: Ali
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, Deraya University, El-Minia Gadida, Egypt.
authors.forename: Omiya A
authors.initials: OA
authors.lastname: Hassan
mesh_terms: D000179:Acrylates / Q000737:chemistry*; D000284:Administration, Oral; D001549:Benzamides / Q000008:administration & dosage* / Q000737:chemistry; D001593:Benzyl Compounds / Q000008:administration & dosage* / Q000737:chemistry; D001682:Biological Availability; D019343:Citric Acid / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry; D015195:Drug Design; D065546:Drug Liberation; D011109:Polymethacrylic Acids / Q000737:chemistry*; D017693:Sodium Bicarbonate / Q000737:chemistry; D013607:Tablets
chemical_list: D000179:Acrylates; D001549:Benzamides; D001593:Benzyl Compounds; D003692:Delayed-Action Preparations; D011109:Polymethacrylic Acids; D013607:Tablets; D019343:Citric Acid; C102254:itopride; D017693:Sodium Bicarbonate; C453622:carbopol 934P
keywords: bioavailability; itopride HCl; oral drug delivery; stability study