DEVELOPMENT OF FLOATING DRUG DELIVERY SYSTEM FOR LORATADINE: IN-VITRO AND IN-VIVO EVALUATION

The reason for this exploration was to develop gastro-retentive drug delivery systems (GRDDS) of loratadine (LTD) to lengthen the gastric residence time (GRT) by using different polymers like hydroxypropyl methyl celluloses (i.e., HPMC K4 M, HPMC K15 M, HPMCK 100 M), xanthan gum and other excipients such as microcrystalline cellulose (MCC), sodium bicarbonate (NaHCO₃), magnesium stearate. All LTD floating formulations (F1-F18) prepared by the direct compression technique and evaluated. Fourier Transformed Infrared Spectroscopy (FTIR) studies showed that there are no drug excipient interactions. All LTD effervescent floating matrix tablets (F1-F18) were assessed for various pre-and post-compression parameters like weight variation (mg), hardness (kg/cm²), thickness (mm), friability (%), drug content (%), in-vitro buoyancy (h), in-vivo buoyancy (h) and in-vitro dissolution (%) and resulted found within pharmacopoeial limits. The drug release and floating property depended upon the polymer type as well as polymer proportions. The floating lag time (FLT) and total floating time (TFT) of all prepared formulations (F1-F18) showed less than 90 seconds and ≥12 hours, respectively. The cumulative percentage (%) of drug release ranged from 57.03 ± 0.13% (F12) to 99.73 ± 0.38% (F5) and optimized formulation (F5) was showed 99.73 ± 0.38% of drug release in 12 h. The in-vitro drug release of LTD effervescent floating tablets followed the non-fickian diffusion-controlled release and is best explained by the Korsmeyer-Peppas equation. All the formulations were subjected to various kinetic models, and F5 formulation was optimized as it followed the zero-order kinetics. The optimized formulation (F5) subjected to an in-vivo study, and the results of radiographic images shown gastric resident time (GRT) of 4 ± 0.5 hours (n=3). From the in-vivo studies it was evident that the GRT increased by floating mechanism.