Tag Archive for: Effervescent method

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.