Abstract
The objective of the present investigation was to design, optimize and characterize the gastro retentive floating levofloxacin tablets and perform in-vivo evaluation using radiographic imaging. The floating tablets were prepared by using polymers i.e hydroxy propyl methyl cellulose (HPMC-K4M) and carbopol-940 individually and in combination by nonaquous granulation method. All the Formulations were evaluated for swelling index (S.I), floating behavior and in-vitro drug release kinetics. The compatibility study of levofloxacin with other polymers was investigated by FTIR, DSC, TGA and XRD. Results from FTIR and DSC revealed no chemical interaction amongst the formulation components. The optimized formulation (F11) showed floating lag time (FLT), total floating time (TFT) swelling index (S.I) of 60 sec, >16h and approximately 75 %, respectively. Moreover, F11 showed zero order levofloxacin release in simulated gastric fluid over the period of 6 h. X-ray studies showed that total buoyancy time was able to delay the gastric emptying of levofloxacin floating tablets in rabbits for more than 4 hours. In conclusion the optimized formulation (F11) can be used for the sustained delivery of levofloxacin for the treatment of peptic ulcer.
Highlights
Peptic ulcer disorder is characterized by painful sores in stomach lining and affects the first part of small intestine
Pre-Compression Parameters of Levofloxacin Granules: Bulk density of the granular mass was recorded in the range of 0.45-0.54 g/ml which increased to 0.6 g/ml after tapping
The compressed tablet containing hydroxyl propyl methyl cellulose (HPMC) and polymeric combinations (i.e. HPMC and carbopol) had hardness 4-6 kg/cm3 while the formulations containing carbopol alone were harder than the counterparts containing HPMC
Summary
Peptic ulcer disorder is characterized by painful sores in stomach lining and affects the first part of small intestine. The carboxylic groups in the Carbopol molecule have affinity to water molecules and swells on hydration while remain insoluble in water (Singla, Chawla, Singh, 2000) This property makes the polymer valuable in the design of floating systems. HPMC and carbopol are used to develop floating drug delivery system, this study will explore the impact of individual as well as combination of polymer on the formulation properties such as swelling, drug release and in-vivo buoyancy. It is used as second line therapy for the treatment of peptic ulcer disease in combination with omeprazole and amoxicillin where the first line triple therapy (lanzoprazol, amoxicillin and clarithromycin) is failed (Blondeau et al, 2000; Verma et al, 2016) The effectiveness of this regime may be improved if levofloxacin is administered as gastro retentive drug delivery system. The in-vivo floating studies were performed by administering optimized formulation containing X–ray grade barium sulphate to rabbits to confirm prolong gastric residence
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
