Preparation and characterization of a gastric floating dosage form of capecitabine

Biomed Res Int. 2013:2013:495319. doi: 10.1155/2013/495319. Epub 2013 Oct 29.

Abstract

Gastrointestinal disturbances, such as nausea and vomiting, are considered amongst the main adverse effects associated with oral anticancer drugs due to their fast release in the gastrointestinal tract (GIT). Sustained release formulations with proper release profiles can overcome some side effects of conventional formulations. The current study was designed to prepare sustained release tablets of Capecitabine, which is approved by the Food and Drug Administration (FDA) for the treatment of advanced breast cancer, using hydroxypropyl methylcellulose (HPMC), carbomer934P, sodium alginate, and sodium bicarbonate. Tablets were prepared using the wet granulation method and characterized such that floating lag time, total floating time, hardness, friability, drug content, weight uniformity, and in vitro drug release were investigated. The sustained release tablets showed good hardness and passed the friability test. The tablets' floating lag time was determined to be 30-200 seconds, and it floated more than 24 hours and released the drug for 24 hours. Then, the stability test was done and compared with the initial samples. In conclusion, by adjusting the right ratios of the excipients including release-retarding gel-forming polymers like HPMC K4M, Na alginate, carbomer934P, and sodium bicarbonate, sustained release Capecitabine floating tablet was formulated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylic Resins / administration & dosage
  • Acrylic Resins / chemistry
  • Alginates / administration & dosage
  • Alginates / chemistry
  • Breast Neoplasms / complications
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / pathology
  • Capecitabine
  • Chemistry, Pharmaceutical*
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / adverse effects
  • Deoxycytidine / analogs & derivatives*
  • Deoxycytidine / chemistry
  • Drug Dosage Calculations
  • Female
  • Fluorouracil / administration & dosage
  • Fluorouracil / adverse effects
  • Fluorouracil / analogs & derivatives*
  • Fluorouracil / chemistry
  • Gastrointestinal Diseases / chemically induced
  • Gastrointestinal Diseases / pathology
  • Glucuronic Acid / administration & dosage
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / administration & dosage
  • Hexuronic Acids / chemistry
  • Humans
  • Hypromellose Derivatives
  • Methylcellulose / administration & dosage
  • Methylcellulose / analogs & derivatives
  • Methylcellulose / chemistry
  • Sodium Bicarbonate / administration & dosage
  • Sodium Bicarbonate / chemistry
  • United States
  • United States Food and Drug Administration

Substances

  • Acrylic Resins
  • Alginates
  • Hexuronic Acids
  • Deoxycytidine
  • Hypromellose Derivatives
  • carbopol 940
  • Capecitabine
  • Glucuronic Acid
  • Sodium Bicarbonate
  • Methylcellulose
  • Fluorouracil