Articles

Development and Characterization of Solid Dispersion of Rasagilline Mesylate for Improvement of Dissolution Rate Using Hydrophilic Carriers

/in /by

The aim of present study was to improve the solubility of Rasagilline mesylate, an Atypical Antipsychotic agent which is BCS Class III drug and thus has very low solubility and hence very poor bioavailability owing to less absorption. Moreover Rasagilline mesylate has a bitter taste. Thus in the present study an attempt was made to taste mask the bitter taste of drug and improve oral bioavailability of drug by formulating the drug into solid dispersion and then formulate the solid dispersions into Fast Dissolving Tablets. Solid Dispersions of Rasagilline mesylate were formulated using various polymers like Plasdone K30, plasdone K90, Eudragit RS100, Eudragit RL 100, Poloxamer 188 and Soluplus in different ratios viz., 1:1 and 1:2 by solvent evaporation method and evaluated for various physicochemical parameters. On the basis of evaluation parameters Solid Dispersion containing Drug : Soluplus :: 1 : 2 was optimized batch having Solubility 1.91 mg/ml, Drug content 102.75 % and % CDR of 98.43 % at 35 mins. For formulating Fast Dissolving Tablets, 32 factorial designs was applied where the batch SD12 and Concentration of Chitosan were taken as dependent variable X1 and X2, respectively and wetting time (sec.) and in vitro disintegration time (sec.) and % CDR were taken as an independent variables. All the formulation prepared by applying experimental design showed more than 93 % drug release in 15 mins. Batch F9 was selected as an optimized batch from the data of overlay plot, drug release kinetics and checkpoint batch. A stability study for optimized formulation was carried out as per ICH guidelines, showed no significant changes in the evaluation parameters. Thus from the study it can be concluded that Fast Dissolving Tablets of Rasagilline mesylate formulated from solid dispersions can provide rapid drug release within a short period of time.

Formulation and Evaluation of Ranitidine Hydrochloride Loaded Floating Microspheres for the Treatment of Gastric Ulcer

/in /by

The study was aimed to prepare gastro retentive floating microsphere of Ranitidine Hydrochloride by Ionotropic Gelation technique and solvent evaporation technique by using the different carriers’ ratios (Carbopol 934, Chitosan, and sodium alginate). Both natural and synthetic polymers have been used to prepare floating microspheres and evaluated the relevant parameters. There was no drug and carrier interactions assessed from FTIR. Depending upon the ratio, the percentage yield was found between 58.33% to 90.38%. in all formulations. The surface morphology of microspheres was characterized by SEM and it was discrete, spherical in shape with rough outer surface and showed free flowing properties. The mean particle size of microspheres significantly increases with increasing polymer concentration and the range between 99.92±1.221 to 168.23±1.963 µm. Among all the formulations, RF3 showed high drug entrapment efficiency (87.52%). The percentage in-vitro buoyancy of the floating microspheres was in the range of 66.92% to 81.52%. The in-vitro drug release study revealed that RF3, RF6 and RF9 Formulations having 89.97%,92.91%,93.68% drug released at the end of dissolution studies respectively. It could be concluded that the developed floating microsphere of Ranitidine Hydrochloride can be used for prolonged release in stomach. Therefore improving the bioavailability and patient compliance.