Acta Pharm. 59 (2009) 211-221

full paper

Original research paper

Development and evaluation of gastroretentive norfloxacin floating tablets

RAMESH BOMMA, RONGALA APPALA SWAMY NAIDU, MADHUSUDAN RAO YAMSANI and KISHAN VEERABRAHMA

vbkishan@yahoo.com

¹ University College of Pharmaceutical Sciences, Kakatiya University, Warangal-506009 (A.P.), India

² Natco Pharma Ltd., Kotthur, Mahaboobnagar District, India

Accepted April 22, 2009

Floating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxy propyl methylcellulose (HPMCK4M, HPMCK100M) and xanthan gum. Tablets were evaluated for their physical characteristics viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied for in vitro drug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and the polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based on in vitro characteristics and was used in vivo radiographic studies by incorporating BaSO₄. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for absorption window drugs.

Keywords: norfloxacin, floating tablets, gastric residence time, gastroretentive drug delivery system