Effect of Sodium Starch Glycolate on Formulation of Fexofenadine Hydrochloride Immediate Release Tablets by Direct Compression Method (original) (raw)
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Fexofenadine HCl Immediate Release Tablets: In vitro Characterization and Evaluation of Excipients
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.
Formulation Development & Optimization of Immediate Release Tablet of fexofenadine Hydrochloride
2013
The investigation was concerned with design and characterization of oral immediate release tablets of Anti allergic drug, in order to improve efficacy and better patient compliance. The API is selective 2 nd generation, non sedative, Histamine H1 receptor blocker. The API has become first line drug in the pharmacotherapy of allergic rhinitis. This is because the drug possesses tolerability and safety advantages over the Histamine H1 receptor blocker. The aim was to formulate various formulations of immediate release tablet of Anti allergic drug using different disintegrant and superdisintegrants (Sodium Starch Glycolate, Croscarmellose sodium) and by using different methods dry granulation and wet granulation. The drug-excipients interaction was investigated by FTIR showed no interaction of API with excipients. The granules and tablets of API were evaluated for various pre and post compression parameters like Angle of repose, Compressibility index, Hausner’s ratio, Tablet hardness, ...
Formulation and Evaluation of Immediate Release Tablets of Fexofenadine Hydrochloride
The present research work is to develop immediate release tablets of Fexofenadine hydrochloride. The rate of dissolution and bioavailability of the Fexofenadine HCL has been increased by using superdisintegrants in its immediate release tablets. Direct compression method was adapted to prepare the tablets by using Sodium lauryl sulphate, microcrystalline cellulose as filler, crospovidone and sodium starch glycolate as superdisintegrant in different concentration (2-8%). Tablets were prepared and evaluated pre and post compressional parameters. In-Vitro Disintegration study shows that as there is increase in disintegration time with increase in concentration of sodium starch glycolate while there is decrease in disintegration time with increase in the level of crospovidone. The results indicate that the selected batch of tablet formulation containing crospovidone provides disintegration time between 3-6 minutes with sufficient crushing strength and accepted friability. It was concluded that immediate release tablet for Fexofenadine hydrochloride can be formulated for fast treatment of allergic rhinitis. INTRODUCTION 1,2 In the last 15 to 20 years, there has been a huge resource in both academia and industry devoted to the development of drug delivery systems that target drugs more effectively to their therapeutic site. Much of this work has been successful and is reported within this text. In spite of this, oral solid dosage forms such as tablets and hard gelatin capsules, which have been in existence since the nineteenth century, remain the most frequently used dosage forms. This is not simply a reflection of the continued use of established products on the market, tablets and capsules still account for about half of all new medicines licensed.
DESIGN AND CHARACTERIZATION OF DISPERSIBLE TABLET OF FEXOFENADINE HCl
ABSTRACT The objective of the work was to Design and evaluate the Dispersible drug delivery system containing Fexofenadine HCl (FEX) as a model drug. FEX tablets were prepared by direct compression and wet granulation method incorporating Crospovidone, cross caramellose sodium, Doshion-Ds, Doshion-D as disintegrants. MCC and lactose were used as diluents, magnesium stearate and talc used as lubricant and glidant. Aspartame as sweetening agent, vanilla as flavoring agent, Erythrosine supra as coloring agent, Aerosil, Pregelatinised starch as suspending and binding agent respectively. Dissolution profiles were studied in 0.1N HCl medium. Tablets were also evaluated for standards of dispersible tablets and were compared with marketed products. The optimized formulation was checked for stability at 30ºC, 65% RH and 40ºC, 75% RH which was found to be stable. The drug release profile of the both formulations was well released within 30 minutes and uniform drug release as compared with marketed formulation. KEYWORDS: Fexofenadine (FEX), Disintegrants, Drug release, Dissolution profile.
Journal of Pharmacy and Pharmacology 7 (2019) 527-540, 2019
Objectives: To improve the aqueous solubility and dissolution of fexofenadine HCl, an attempt was made to prepare its fast dissolving tablets by lyophilization technique. Methods: For the preparation of lyophilized tablets (F1-F32), the drug was dispersed in a hydrated solution of water-soluble polymers (gelatin/maltodextrin/acacia) containing glycine and mannitol. The blend was pelted down into the patches of a blister pack, frozen down and then lyophilized. Different characterization parameters viz. differential scanning calorimetry, hardness, weight variation, X-ray diffraction (XRD), scanning electron microscopy (SEM), mercury porosimetry, solubility, wetting time and water absorption ratio, lyophilization tablet index, drug content, in vitro dissolution and stability were evaluated. Key findings: Tablets (F32) containing acacia were found to have fast disintegration and relatively higher mechanical strength with improved drug solubility. X-ray diffractogram and scanning electron micrograph indicated decrease in crystallinity of drug and a good porous structure property for prepared tablet, respectively. Dissolution study showed complete drug released within 5 min. Moreover, tablets (F32) were found to be stable for one month at 25 ± 2 °C/60 ± 5% relative humidity.
Formulation and in vitro evaluation of orodispersible tablets of fexofenadine hydrochloride
Tropical Journal of Pharmaceutical Research
Purpose: To develop orodispersible tablets (ODTs) of fexofenadine hydrochloride using three different superdisintegrants in various ratios and to compare their disintegration properties.Methods: Direct compression technique was used for the preparation of ODTs. Mannitol and Avicel CE-15 (microcrystalline cellulose and guar gum) were used as direct compression diluents. The disintegration time of tablets using each polymer (superdisintegrant) was evaluated as well as othertablet properties including weight fluctuation, hardness, friability, wetting time and water absorption ratio.Results: Satisfactory values were obtained for all the evaluated parameters. As the polymer concentration increased, there was a decrease in disintegration time. A comparison of the three different polymers used revealed that CCM3 formulated with 12 % croscarmellose sodium and 14.66 % lactose had the least disintegration time of 32.33 ± 3.23 s. In vitro release studies showed that the maximum drug release of...
Formulation Development and Evaluation of Once Daily Fexofenadine Hydrochloride Microsponge Tablets
Trends in Sciences, 2022
The objective of present study was to formulate and develop once daily Fexofenadine Hydrochloride tablets to improve the aqueous solubility by microsponge technology. Fexofenadine Hydrochloride is an antihistamine and belongs to BCS class-III with low permeability and poor bioavailability about 30-35 %. The microsponges were prepared by Quashi emulsion solvent diffusion method with Quality by design approach. The study of effect of independent variables Eudragit EPO (500 to 1,000 mg), internal phase volume (DM: ETH) (5 to 10 mL) and RPM (500 to 1,000) on responses were analyzed to optimize the formulation with desirable results by using central composite design and response surface method. Optimized formulation F22 showed percent production yield (99.10 %), percent drug entrapment (99.45 %), particle size (94.12 µm) and percent drug release of prepared tablets at 5, 10, 15 and 30 min were 60.6, 80.75, 87.47 and 92.85 %, respectively. It showed Higuchi mechanism of release kinetics by diffusion. In vivo pharmacokinetics of the prepared tablets was studied in rabbits (IAEC/NRML/2022-2023/09) with and without permeation enhancer to find the rate of absorption. when compared to Marketed product-Allegra 24 (F21) with (t1/2 absorption) 0.192711±0.00278 h and MRT 19.10608±0.257571 h and formulation without poloxamer 407 (F22) (t1/2 absorption) 0.165013±0.024164 h and MRT 19.32228±0.764531 h, maximum absorption was observed for the Formulation F23 with poloxamer 407 (15 %) with (t1/2 absorption) of 0.144662±0.006787 h and Mean residence time (MRT) of 24.10796±1.01232 h. Microsponge technique improved the aqueous solubility of the fexofenadine Hydrochloride and Eudragit EPO extended the mean residence time up to 24 h along with improved permeability in presence of Poloxamer 407 to full fill the needs of BCS class-III drug.
2018
The objective of the present work was to formulate and to characterize controlled release matrix tablets of Fexofenadine in order to improve bioavailability and to minimize the frequency of administration and increase the patient compliance. A matrix tablets was developed that releases Fexofenadine over a 12-hour period and the influence of the polymer type and concentration on the release rate of the drug was evaluated. Fexofenadine tablets were prepared by direct compression technique by the use of different natural, synthetic polymers such as gum acacia, hydroxypropyl methyl cellulose K15, xanthum gum and guar gum individually and also in combination. Studies were carried out to study the influence of type of polymer on drug release rate, and in vitro release kinetics were examined. All the formulations were subjected to physicochemical characterization such as weight variation, hardness, thickness, friability, drug content. In vitro dissolution studies were carried out simulated...
Formulation and In vitro Evaluation of Eudragit RL 100 Loaded Fexofenadine HCl Microspheres
The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.
2011
The objective of present work is to investigate the enhancement of dissolution profile for oral delivery of Fexofenadine Hydrochloride (FH) through solid dispersion (SD) technique by the method of solvent evaporation. The SD was prepared by using ethanol as a solvent. Tablets were formulated containing solid dispersion of FH and compared with tablets of same formula without solid dispersion of FH. The using of ethanol to prepare solid dispersion found a significant effect on the dissolution of FH. Dissolution studies using the USP-33 paddle method were performed for tablets formulated with and without solid dispersions of FH. Dissolution of FH improved significantly in tablets formulated with SD (85% in 10 minutes) exhibited better dissolution profile than tablets formulated without SD. Infrared (IR) spectroscopy was also performed to identify the physicochemical interaction between drug and solvent, hence its effect on dissolution.