D.V.R.N.Bhikshapathi

The aim of the current study was to formulate and characterize oral floating alginate microspheres of Rebamipide to sustain the gastric residence time and to target gastritis. The floating alginate microspheres were prepared by ionotropic gelation technique. Sodium alginate was used as polymer, sodium bicarbonate as gas generating agent, calcium chloride as cross-linking agent, HPMC K4, HPMC K15 as rate retarding agent. Microspheres were characterized for the Micromeretic properties, entrapment efficiency, buoyancy test, SEM analysis, FTIR, and in vitro release studies. The release studies were carried out in 0.1N HCl and the results were applied to various kinetic models.  Among the total 14 formulations F12 was optimized. The % yield of F12 formulation was found to be 93.73%. On the basis of optical microscopy, the particle size was 79.45±0.09µm. The % buoyancy, % entrapment efficiency and swelling index of F12 formulation was 94.2%, 95.5% and 96.16, respectively. The Cumulative % drug release of F12 formulation was 96.12±0.22% in 12h when compared with marketed product 95.15±0.23 in 1h.  SEM studies showed the particles were in spherical shape. Based on obtained results, floating alginate microspheres were of good candidate for targeting to GIT in the efficient management of gastritis.

Present work aimed at preparing quick onset of action of Granisetron HCl which is beneficial in emesis, aiding in the enhancement of bioavailability and is very convenient for administration without the problem of swallowing and using water. The films were prepared by using different grades of HPMC E3, E6 and E15, maltodextrin DE6 and other polymers by solvent casting method. They were evaluated for physical characteristics such as thickness, uniformity of weight, folding endurance, drug content, surface pH, percentage elongation and tensile strength and results were found to be satisfactory. The formulations were subjected to disintegration and in-vitro drug release test. The in vitro disintegration time of the optimized formulation F9 was 9 sec and drug release was found to be very fast i.e. 97.8% of within 8 min when compared with innovator product i.e 70.8%. In vivo studies confirmed that their potential as an innovative dosage form to improve the bioavailability and considered to be potentially useful for the treatment of emesis where quick onset of action is desirable. DSC and FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation. From the above results, it can be a good alternative to conventional Granisetron Hydrochloride tablets in the treatment of emesis. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Granisetron Hydrochloride.

The present study was an attempt to prepare and evaluate Zolmitriptan 9 different oral disintegrating tablets using superdisintegrants like SSG, Crospovidone and Croscarmellose sodium. Formulations were evaluated for their micromeretic properties and post compression studies and found to be within the limits. Based on the disintegrating time and dissolution studies F9 was found to be best formulation. It was found that the sodium starch glycolate is much more effective than the other super disintegrating agents in the preparation of Zolmitriptan oral disintegrating tablets. DSC and FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation.

Recently, fast dissolving films are gaining interest as an alternative of fast dissolving tablets. The present study aimed at preparing fast dissolving oral films of Naratriptan hydrochloride as a model drug which is used for the migraine treatment. Fast dissolving dosage forms have acquired great importance in pharmaceutical industry because of their unique properties like dissolve upon contact with a wet surface, such as the tongue, within a few seconds, meaning the consumer can take the product without need for additional liquid. This convenience provides both a marketing advantage and increased patient compliance. In the present investigation various trials were carried out using two grades of HPMC (E3 and E6), Propylene glycol, PEG-400 and other polymers by solvent casting method.  The prepared films were evaluated for film thickness, folding endurance, surface pH, morphological properties, %drug content and content uniformity, tensile strength, percent elongation, in vitro disintegration time and in vitro dissolution studies. The optimized formulation S11 prepared using HPMC E6 showed minimum disintegration time (10 sec), highest dissolution rate i.e. 98.23% of drug within 6 min and satisfactory physicochemical properties. Results of DSC and FTIR data of optimized formulation (S11) revealed that there was no incompatibility observed between the drug and excipients used in the formulation. These findings suggest that the fast dissolving oral film containing Naratriptan hydrochloride is considered to be potentially useful for the treatment of migraine where quick onset of action is desirable when compared with reference standard Naratrax conventional tablet.