Formulation, Optimization, in vitro and in-vivo evaluation of levofloxacin hemihydrate Floating Tablets

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.

Polymeric Excipients in the Technology of Floating Drug Delivery Systems

“…Co-processing aid based on xanthan gum and acacia gum [33] Xanthan gum, a polysaccharide isolated from Orchis morio [43] Xanthan Gum, Polysaccharide from Tamarindus indica seeds [43] NaCMC, HPMC K15 M [57] Carbomer (Carbopol 940), HPMC K4M [120] HPMC K15 M, HPMC K100 M [121] Carbomers (Carbopol 934P; 971 P) HPMC K4M [122] HPMC K4 M, Carbomer, Chitosan [123] EC, Eudragit RS PM [124] NA, HPMC K4 M, Carbomer (Carbopol 974P) [125] Polysaccharide from Tamarindus indica seeds, HPMC K4 M, PVP [126] HPMC K4 M, NA, Carbomer (Carbopol 934P), PEG 3500 [127] Tablets (wet granulation, film coating) HPMC K4 M [128] Tablets (wet granulation, pressed coatings) HPC, NA [119] HPMC K15 M, PEO (Polyox 303 SWR) [129] Bilayer tablets (wet granulation) Eudragit RL 100, CMC [130] Tablets (dry granulation) HPMC K4 [131] Minitablets (wet granulation) encapsulated HPMC K100 M [132] Granules or "spheroids" (extrusion-pelletization) HPMC K4 M, Carbomer (Carbopol 934P) [133] Film (solvent removal) encapsulated CA [61] Incorporation of swelling substances…”

Formulation and characterization of floating biphasic tablet consisting of cefdinir nanosuspension

“…The constituents of the formula are mixed and milled by mortar and pestle for 5 min the add a magnesium stearate as a lubricant before compression by tablet machine with 10 mm punch and die. Table (2) shows the composition of the floating layers. Total weight 655 720…”

“…Fourier transforms infrared spectroscopy (FTIR) spectra of cefdinir pure drug, Soluplus® , physical mixture of cefdinir nanosuspension and lyophilized cefdinir nanosuspension are shown in figure (2). IR spectrum of Cefdinir (a) is characterized by principal absorption peaks at 3352.28 cm−1 (O ̶ H stretch COOH), 3120.57 cm-1 (amino group), 2898 cm−1 (C ̶ H stretch), 1621.84 cm-1 (oxime group), 1766.…”

“…The produced bilayer tablets demonstrated the tablet generally recognized floating features and post-compression properties, as given in Table (5). (2). The floating tablets of the cefdinir lyophilized powder were prepared using sodium bicarbonate as gas generating agent, lactose as diluent.…”

“…Many medications' oral bioavailability is hampered by their poor physicochemical properties or absorption in a specific region of the gastrointestinal tract (GIT), known to as the "absorption window." Extended stomach persistence improves bioavailability, decreases drug waste, and increases solubility for medicines that are less soluble in a high pH environment (2). As a result, formulation experts are constantly working to improve oral drug delivery systems by creating novel techniques.…”