Development of Sustained Release Floating Drug Delivery System for Norfloxacin: In Vitro and In Vivo Evaluation

Abstract

Norfloxacin is a broad-spectrum antibiotic used to treat bacterial infections such as respiratory and urinary tract infections. Conventional norfloxacin tablets show incomplete drug absorption resulting in lower bioavailabilty. Norfloxacin is better absorbed in the stomach. The dosage forms that remain in the stomach are referred to as gastroretentive drug delivery systems. Gastroretentive floating tablets of norfloxcin were developed by employing three different polymers, which prolonged the drug release from the dosage forms. Tablet floatation was achieved by an effervescent mechanism. Citric acid at different concentrations was used in formulations to provide an acidic microenvironment. The prepared tablets were characterized for hardness, weight variation, thickness, friability, floating lag time, and dissolution. Around 12 tablet formulations were prepared as a continuation of the previous work. The best formulation (F4c) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent. The tablets remained in the stomach for about 205 ± 8.4 min. Bioavailability studies were conducted in healthy male human volunteers, and the pharmacokinetic parameters of the best formulation were compared with that of the marketed conventional (Norbid) tablet. The increased bioavailability of the developed formulation was found to be 16.27%.

Formulation and In Vitro, In Vivo Evaluation of Effervescent Floating Sustained-Release Imatinib Mesylate Tablet

“…The desiccator was placed in oven at 40°C for six months. At pre-determined time intervals, the stored tablet was studied for the following parameters: drug content, hardness value and floating behavior and matrix integrity, which was observed visually [ 39 ]. Statistical analysis was done using paired Student’s t-test, at a significance of p<0.05.…”

Novel Drug Delivery Systems for Modulation of Gastrointestinal Transit Time

“…Tracking the in vivo floating behavior and location of dosage form through GI tract providing a broad insight for formulating the optimal floating drug delivery system could be established via radiography, gamma scintigraphy, gastroscopy, ultrasonography and magnetic resonance imaging. Considering the majority of the surveys in this case, not only the relevant correlation between in vivo and invitro assessments was confirmed but also effectiveness and reliability of these floating systems as an excellent strategy for controlled delivery of drugs was ascertained [Jain et al, 2006;Ali et al, 2007;Wei & Zhao, 2008;Guguloth et al, 2011].…”

Multi‐Drug‐Loaded Microcapsules with Controlled Release for Management of Parkinson's Disease

“…In order to increase drug bioavailability, these microcapsules should possess good buoyancy, so as to prolong their gastric retention time and allow for drugs to be released in the upper gastrointestinal tract. For example, it was reported that floating tablets exhibited higher bioavailability (162.7%) of Norfloxacin in healthy male human volunteers as compared to conventional non‐floatable tablet forms . In addition, it was also reported that propranolol HCl loaded into a floating gum showed a significant improvement in its bioavailability (132%) as compared with commercial propranolol tablets (Ciplar LA 80) .…”