Design & Evaluation of Norfloxacin Gastro Retentive effervescent floating tablets Abstract: Norfloxacin gastro retentive effervescent floating

tablets were developed to prolong gastric residence time, leading to an increase in drug bioavailability. The purpose of this study was to design a floating drug delivery system with swelling and floating properties. Six tablet formulations (FA1, FA2, FA3, FB!, FB2, FB3)were prepared by wet granulation technique using HPMC K4 M and HPMC K100 M as release retarding polymers in different ratios and sodium bi carbonate as gas generating agent. The tablets were evaluated for their physico chemical properties, Buoyancy lag time, thickness, IR spectra analysis, content uniformity, swelling index, floating time, hardness, friability and Invitro dissolution studies Key words: Norfloxacin, floating tablets, HPMC & FDDS Introduction: Norfloxacin is a second generation flouroquinolone (quinolone), broad spectrum antibiotic developed by Kyorin Seiyaku.K.K. It is used in the treatment of urinary tract infection, prostatitis and gonorrhea. It is least absorbed from the lower part of the gastrointestinal tract and is better absorbed from the stomach (bio availability is 30 to 40 %). floating drug delivery system float and can be retained in the stomach due to their lower bulk density then the gastric contents and remain buoyant in the stomach for prolonged period of time without affecting the gastric emptying rate of the other contents. In the presence study floating tablets of Norfloxacin are prepared with hydrophilic gelling polymers (HPMC K4 M and HPMC K100 M) and an effervescent agent (sodium bi carbonate) to provide sustained release in the gastric medium. Thus the study aims to improve the bio availability of the drug and to achieve extended retention in the stomach which may result in prolonged absorption. Materials and Methods: Materials: Norfloxacin was received as a gift sample from Relax Pharmaceuticals, Vadodara (Gujarat). Hydroxy propyl methyl cellulose K4 M, Hydroxy propyl methyl cellulose K100 M, dicalcium phosphate and polyvinyl pyrrolidone K30 was procured from Yarrow Chemical Products, Mumbai. Magnesium stearate, iso propyl alcohol and sodium bi carbonate from S D Fine chemicals Limited, Mumbai. Talc was procured from Nagpal Pharmaceutical Pvt Limited, Mumbai. All the other chemicals used were of analytical reagent grade Method: Six formulations of Norfloxacin floating tablets were prepared according to the design depicted in Table-1 by wet granulation technique. Table-1

Composition of Norfloxacin gastro retentive effervescent floating tablets The respective powders namely Norfloxacin (200 mg) , release rate retarding polymers (HPMC K4 M and HPMC K100 M), a gas generating agent (Sodium bi carbonate) were passed through sieve no. 20 PVPK-30 was dissolved in iso propyl alcohol to prepare binder solution and added to the dry blend gradually with constant kneading to form a homogenous mass. The dough mass was passed through sieve no. 16 and dried the granules at room temperature. The dried granules were passed through sieve no. 22 and lubricated with magnesium stearate (2 % w/w) and talc (2 % w/w). Granules were compressed into tablets using 10 station tablet punching machine (Rimek, India) with flat faced punches. I. Determination of physico chemical parameters 1. Hardness Test: Monsanto hardness tester was used for the determination of hardness of tablets. 2. Friability: 20 tablets were accurately weight and placed in the friabilator (Roches Friabilator) and operated for 100 revolutions. The tablets were dedusted and reweighed and percentage of loss in tablets weight is determined 3. Weight variation: 10 tablets were selected at random and calculated the average weight. Not more than the percentage as given in IP and none deviates by more than twice that percentage. 4. Thickness: A vernier caliper (For-bro engineers, India) was used to determine thickness of 10 randomly selected tablets. II Determination of floating properties 1. Swelling study: Formulated tablets were weighed individually (WO) and placed separately in petridish containing 50ml of 0.1N HCl. The petridishes were placed in an incubator maintained at 37 0 .5 C. at regular one hour time intervals until 4 hrs, the tablets were removed from the petridish and pressed with filter paper. The tablets were re weighed (Wt) and the percentage swelling index was calculated using the formula % WU = (Wt WO/ WO) X 100 Wu = water uptake Wt = weight of tablet at time t Wo = weight of tablet before immersion 2. Invitro buoyancy studies: Invitro buoyancy was determined by the floating lag time. The tablets were placed in a 100ml beaker containing 0.1mol L-1 HCl. The time required for the tablet to rise to the surface for floating was determined as the floating lag time and further floating duration of all the tablets was determined by visual observation.

3. Drug content uniformity: Ten tablets were individually weighed and crushed. Quantity of powder equivalent to the mass of one tablet was extracted in 100 ml of 0.1N HCl the solution was filtered through a cellulose acetate membrane (0.4m). The drug content was determined by UV spectroscopy (Shimadzu, Japan) at a wave length of 280nm after a suitable dilution with 0.1N HCl. 4. Invitro Dissolution Studies: The Invitro drug release studies were conducted using the USP type II (paddle) dissolution apparatus (TDT-08L, Electrolab, India). Hydrochloric acid (pH 1.2), 750ml, was used as medium. The study was conducted at 37 0 .5 C and at paddle rotation of 50 rpm. Samples pf 5ml were collected at predetermined time intervals and replaced with fresh hydrochloric acid. The samples were filtered and diluted and the drug content in the samples was estimated at 278nm.