Articles

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

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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.

Enhancement of Solubility Ibuprofen by Solid Dispersion Technique on Natural Mucilage

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In this study generally solid dispersions (SDs) of ibuprofen were prepared by for all intents and purposes melt dispersion technique using natural mucilage of Lemon seed as carrier, which really is quite significant. Physical mixtures (PMs) of ibuprofen literally were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile, which generally is fairly significant. The solid dispersions and kind of physical mixtures for all intents and purposes were investigated for drug loading, saturation solubility and dissolution behavior in a subtle way.
Saturation solubility study really actually was basically carried out in phosphate buffer (pH 7.4), 0.1 N HCL solution and distilled water, which kind of literally is quite significant. Solid dispersions for all intents and purposes particularly were mostly really found definitely fairly effective to literally kind of enhance the solubility of ibuprofen significantly in all the media, which actually is quite significant. Dissolution test specifically was mostly carried out in two different media, phosphate buffer (pH 7.4) and 0.1 N HCL. Solid dispersion containing Lemon seed mucilage at the ratio of 1:1.5 (drug: carrier) basically showed faster and sort of definitely higher drug release and basically was specifically really found to for the most part actually be most sort of effective among all the very actually solid dispersions in a generally big way, which kind of is fairly significant. Drug carrier interactions specifically specifically were studied by comparing Fourier definitely mostly Transform generally Infrared Spectroscopy (FT-IR) of particularly solid dispersions with pure drug which essentially revealed that the SDs specifically were kind of really stable in a pretty big way, which is fairly significant. So, fairly very solid dispersion may particularly be an definitely really effective technique to specifically enhance dissolution rate of ibuprofen, which kind of literally is fairly significant in a fairly big way.