Ibuprofen, a non-steroidal anti-inflammatory drug was formulated as microspheres by using Methocel K4M & Eudragit RSPO. These microspheres were prepared by emulsification solvent evaporation method to provide sustained action and to minimize local side effect of Ibuprofen by avoiding the drug release in the upper gastrointestinal tract. The prepared microspheres were subjected to various evaluation and in-vitro release studies. In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) using Phosphate buffer (pH 7.4) as the dissolution medium at 37.5 o C for 6 hours (paddle speed 50 RPM). The release mechanisms were explored and explained with Zero Order, First Order, Higuchi and Korsmeyer-Peppas equations. The correlation coefficients values of the trend lines of the graphs showed that the formulations best fit with Korsmeyer-Peppas release pattern. Microspheres' morphology and chemical integrity were studied by a scanning electron microscope (SEM) and Fourier transforms infrared spectroscopy (FTIR) respectively.
Fexofenadine HCl immediate release tablets were designed to increase the dissolution rate by using superdisintegrants. Different formulations of Fexofenadine HCl were prepared by direct compression method. These formulations were evaluated for hardness, thickness, friability, weight variation, disintegration time, and in vitro dissolution study. The drug release from the formulations were studied according to USP specification (USP paddle method at 50 rpm for 60 minutes) maintaining the temperature to 37 0 C. Sodium starch glycolate, cross carmellose sodium, crospovidone (kollidon CL), ludiflash and xanthan gum were used in 3%, 6% and 8% concentrations as superdisintegrants. Thus, the ratio of superdisintegrants was changed whereas all the other excipients as well as the active drug (Fexofenadine HCl) remained same in every formulation. Here, 0.001N HCl was used as dissolution medium according to USP and absorbances were determined by using UV spectrophotometer at 217 nm. The F-3 and F-6 formulation prepared by 8% of Sodium starch glycolate and 8% of Cross carmellose sodium showed 99.99% drug release within 30 minutes and 45 minutes, respectively. The disintegration times of F-3 and F-6 formulation were within 9 seconds. The interactions between drug and excipients were characterized by FTIR spectroscopic study.
ABSTRACT:The purpose of the present studies was to develop and characterize sustained release tablets of Carbamazepine, an antiepileptic drug. Tablets were prepared by direct compression method. In the formulation, the active drug was taken 200 mg in every formulation. Methocel K4M, Methocel K15M CR, Methocel K100LV CR, Eudragit RSPO and Eudragit RLPO polymers were used as rate retarding agents in twenty four formulations (F-1 to F-24). The effect of hydrophilic polymer PEG 6000 as channeling agent with Methocel K4M was observed in four formulations (F-5 to F-8). The granules were evaluated for angle of repose, bulk density, tapped density. The tablets were subjected to average weight, diameter, thickness, weight variation, hardness, friability and in vitro dissolution studies. The granules showed satisfactory flow properties, compressibility and drug content. The in vitro dissolution study was carried using USP Apparatus-I (Rotating basket method apparatus) for 6 to 12 hours in distilled water with 1% sodium lauryl sulphate as the dissolution medium. The release mechanisms were explored and explained by Zero order, First order, Higuchi, Korsmeyer-Peppas and Hixson-Crowell equations. Primarily twelve formulations were prepared by using four variable amount of three polymers; Methocel K4M (50, 100, 150 and 200 mg) in the formulations from F-1 to F-4, Methocel K15M CR (50, 100, 150 and 200 mg) in the formulations from F-9 to F-12 and Methocel K100LV CR (50, 100, 150 and 200 mg) in the formulations from F-13 to F-16. Then four formulations were prepared where Methocel K4M amount was same but using variable amount of hydrophilic polymer PEG 6000 (50, 100, 150 and 200 mg). After that another eight formulations were prepared by using polymer Eudragit RSPO and Eudragit RLPO by using variable amount. In F-17 to F-20 the use of Eudragit RSPO was in variable amount (50, 100, 150 and 200 mg) and in F-21 to F-24 the use of Eudragit RLPO was in variable amount (50, 100, 150 and 200 mg). Other excipients remained same in the formulations. Among these twenty four formulations' sustainability was studied and compared with three market product of 200 mg tablet. It was found that effect of PEG 6000 as channeling agent subsequently decreased the sustaining action (Formulation F5-F8).
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