DEVELOPMENT OF ZOLMITRIPTAN MOUTH DISSOLVING FILMS: FORMULATION VARIABLES, MECHANICAL PROPERTIES, AND IN VITRO DRUG RELEASE STUDIES

Objective: The objective of the present investigation is to prepare zolmitriptan (ZOL) mouth dissolving films (MDFs) and to investigate the influence of formulation variables on physicomechanical, chemical, and drug release properties of the prepared MDFs. Methods: The MDFs were prepared by solvent casting technique using wet film applicator. The impact of hydroxypropyl methylcellulose of different viscosity grades (hydroxy propyl methyl cellulose [HPMC] E3, E5, and E15), plasticizers (glycerol and polyethylene glycol [PEG]-400), and solubilizing agents (polyvinyl pyrrolidone [PVP K30] and sodium lauryl sulfate [SLS]) on physicomechanical, chemical, and drug release properties were evaluated. The MDFs were also characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry studies. Results: The MDFs prepared were transparent and smooth and showed no recrystallization. The tensile strength of the MDFs increased significantly with an increase in polymer viscosities, and about a 2.63-fold increase in tensile strength was observed for HPMC E15 MDFs compared to E3, whereas an increase in film thickness resulted in brittle MDFs with low tensile strength. Similar results were observed with percent elongation and folding endurance of the MDFs. In vitro, drug release studies indicate that higher film thickness and polymer viscosities delayed the MDF disintegration and, in turn, the ZOL release. Addition of PVP K30 and SLS to HPMC E3 formulations resulted in 1.66- and 1.53-fold increase in ZOL release rates. Conclusion: Overall, F7 formulation showed quicker disintegration (within 11 s) and ZOL release rates (within 180 s) along with good physicomechanical properties. These results indicated that the disintegration and drug release of ZOL can be enhanced to a greater extent by optimizing formulation variables in MDFs

Development of Capecitabine Floating Tablet Dosage Forms for Treating Stomach Cancer

Objective: In the present research work, oral gastro retentive dosage forms (GRDFs) of capecitabine (CPC) were formulated using floating concept. Methods: GRDFs were formulated using hydroxypropyl methyl cellulose (HPMC K4M and K15M) as drug release retardant, sodium bicarbonate (NaHCO3) and calcium carbonate (CaCO3) as gas generating agents, and micro crystalline cellulose (MCC), dicalcium phosphate (DCP), spray dried lactose (SDL), and pre gelatinized starch (PGS) as fillers. The tablets were prepared by direct compression method and evaluated for various parameters. The GRDFs were also characterized by Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Results and Discussion: All the formulations were subjected for pre and post compression parameters, shows all the data within the limits. The lag times of GRDFs has decreased significantly for formulations containing calcium carbonate when compared to sodium bicarbonate as gas generating agent. In vitro drug release studies indicate that higher polymer concentration delayed the CPC release, and the sustaining effect was in the order K4M > K15M > LVCR 100. Addition of MCC, DCP, SDL, and PGS as fillers further affected the lag time and in turn the CPC release rates. Conclusion: The formulation (F9) containing 10%w/w HPMC K4M as the release retardant, microcrystalline cellulose as filler and 20%w/w CaCO3 as gas generating agent fulfilled regulatory requirements in terms of percent drug release at the end of 24h. Keywords: Capecitabine, Gastro retentive floating tablets, floating drug delivery systems, FTIR, DSC