Development and evaluation of gastroretentive norfloxacin floating tablets.
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 hydroxypropyl methylcellulose (HPMC K4M, HPMC K100M) 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 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 the absorption window drugs.
Bomma
Ramesh
R
University College of Pharmaceutical Sciences, Kakatiya University, Warangal-506009 (A.P.), India.
Swamy Naidu
Rongala Appala
RA
Yamsani
Madhusudan Rao
MR
Veerabrahma
Kishan
K
D000284:Administration, Oral; D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004058:Diffusion; D004337:Drug Carriers; D005746:Gastric Emptying; D005753:Gastric Mucosa / Q000378:metabolism*; D006244:Hardness; D006801:Humans; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D008954:Models, Biological; D009643:Norfloxacin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011108:Polymers / Q000737:chemistry*; D011135:Polysaccharides, Bacterial / Q000737:chemistry; D011859:Radiography; D012995:Solubility; D013270:Stomach / Q000000981:diagnostic imaging; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods; D055815:Young Adult
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011108:Polymers; D011135:Polysaccharides, Bacterial; D013607:Tablets; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D009643:Norfloxacin; C002563:xanthan gum