Evaluation of the fluid uptake kinetics and drug release from gellan gum tablets containing metronidazole

Emeje, Martins; Franklin-Ude, P.I.; Ofoefule, S. I.

doi:10.1016/j.ijbiomac.2010.05.005

Cited by 35 publications

(8 citation statements)

References 23 publications

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“…These characteristics make GG an interesting material for pharmaceutical applications 22,29 . Several drug delivery systems based on GG, such as in situ momethasone furoate nasal gel 30 , in situ gelling terbinafine hydrochloride ophtalmic nanoemulsion 31 , and GG tablets with metronidazole 32 were developed. The development of hydrogel microspheres based on GG crosslinked with mono and divalent cations, mainly Ca 2+ , has been exploited to obtain different drug delivery systems 22,24 .…”

Section: Introductionmentioning

confidence: 99%

Gellan gum microspheres crosslinked with trivalent ion: effect of polymer and crosslinker concentrations on drug release and mucoadhesive properties

Boni

Prezotti

Cury

2016

Drug Development and Industrial Pharmacy

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Gellan gum microspheres were obtained by ionotropic gelation technique, using the trivalent ion Al(3+). The percentage of entrapment efficiency ranged from 48.76 to 87.52% and 2(2) randomized full factorial design demonstrated that both the increase of polymer concentration and the decrease of crosslinker concentration presented a positive effect in the amount of encapsulated drug. Microspheres size and circularity ranged from 700.17 to 938.32 μm and from 0.641 to 0.796 μm, respectively. The increase of polymer concentration (1-2%) and crosslinker concentration (3-5%) led to the enlargement of particle size and circularity. However, the association of increased crosslinker concentration and reduced polymer content made the particles more irregular. In vitro and ex vivo tests evidenced the high mucoadhesiveness of microspheres. The high liquid uptake ability of the microspheres was demonstrated and the pH variation did not affect this parameter. Drug release was pH dependent, with low release rates in acid pH (42.40% and 44.93%) and a burst effect in phosphate buffer pH (7.4). The Weibull model had the best correlation with the drug release data, demonstrating that the release process was driven by a complex mechanism involving the erosion and swelling of the matrix or by non-Fickian diffusion.

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Section: Introductionmentioning

confidence: 99%

Gellan gum microspheres crosslinked with trivalent ion: effect of polymer and crosslinker concentrations on drug release and mucoadhesive properties

Boni

Prezotti

Cury

2016

Drug Development and Industrial Pharmacy

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“…Flow rate rather than CI is a direct measurement of powder flowability. 24) Generally, values of the angle of repose for all the formulations show that, the powders have fair flow potentials. Blending was also found to improve flow as indicated by the angle of repose of AEG/C71 at 1 : 2 and 3 : 1.…”

Section: Resultsmentioning

confidence: 86%

“…16,[24][25][26][27][28][29][30][31][32][33][34][35] The drug release from polymer matrix can be due to disentanglement or diffusion, depending on the polymer molecular weight and the thickness of the diffusion boundary layer. 35) Several kinetic models have been proposed to describe the release characteristics of a drug from controlled release polymer matrix.…”

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confidence: 99%

Oral Sustained Release Tablets of Zidovudine Using Binary Blends of Natural and Synthetic Polymers

Emeje

Olaleye

Isimi

et al. 2010

Biological & Pharmaceutical Bulletin

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Oral sustained release matrix tablets of zidovudine (ZDV) were prepared using different types, proportions and blends of carbopol 71G (C71) and a plant gum obtained from Abelmoschus esculentus (AEG). The effect of various formulation factors like polymer proportion, polymer type and pH of the dissolution medium on the in vitro release of the drug was studied, using the half change technique, in 900 ml of dissolution medium, at 100 rpm. Release kinetics were analyzed using Zero-order, Higuchi's square-root and Ritger-Peppas' empirical equations. In vitro release performance as revealed by the time taken for 70% of the drug to be released (t 70% ), showed that the release rate decreased with increase in polymer proportion. Matrix tablets containing 10 and 20% AEG were found to exhibit immediate-release characteristics. Matrix tablets containing 30% AEG showed t 70% value of 204 min and extended the release up to 5 h, while matrix tablets containing 30% carbopol showed t 70% value of 234 min and extended the release up to 6 h. Three blends of AEG and C71 at the ratio of 1 : 2, 2 : 1 and 1 : 3 showed t 70% values of 132, 312 and 102 min respectively and extended the release up to 8 h. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets followed Fickian and anomalous release. Drug release from matrix tablets of zidovudine containing blends of AEG and C71 demonstrates the advantage of blending a natural and synthetic polymer over single polymer use.

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“…appearance, weight variation, thickness, hardness, drug content which was evaluated via in vitro release studies. 31,32 Experimental animal model: One hundred and twenty (120) male Sprague Dawley ® rats weighing 350-400g at the start of the experiment were allowed to acclimatize in their new environment for seven days prior to commencing the experiment. They were housed, each rat in an individual polypropylene and metal cages equipped to provide food and water.…”

Section: Dissolution Rate Of Metronidazole and Metronidazole/activatementioning

confidence: 99%

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2017

IJPSR

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Background: Due to Escherichia coli O157:H7 bacteria's peculiar biochemical characteristics it is considered an emerging pathogen. The aim of this study is to design, develop and evaluate the efficacy of a single formulation combining adsorptive and anti infective properties in the treatment of diarrhoea caused by Escherichia coli O157:H7 in an animal model. Method: A bilayered tablet of metronidazole and activated charcoal (AC) formulated via direct compression was developed using hydrophilic mucoadhesive polymer xanthan gum in varying concentrations to ensure modified release of metronidazole in the first layer and activated charcoal with microcrystalline cellulose for instant disintegration in the second layer. Escherichia coli infected Sprague Dawley ® rats was utilized to evaluate the efficacy of the formulation. Results: Swelling studies reflected an affinity for the polymer to swell in pH 6.8 where drug release and swelling was influenced by ionic strength of the medium owing to the conformational changes in the xanthan gum in this media with an increase in the zeta charge from-28.5 mV to-40.2 mV, drug release being predominantly by zero order. Treatment with activated charcoal and metronidazole reflected a negative result for identification of Escherichia coli O157:H7 by the third day of treatment in stool with symptoms cessation occurring by the second day of treatment. Conclusion: The synergistic potential of a nitro-imidazole and an adsorbent has been evaluated and established with treated groups showing cessation of symptoms within twenty four hours thus effective in the treatment of Escherichia coli O157:H7 associated diarrhea. INTRODUCTION: Metronidazole a nitro imidazole derivative is a commonly used antibiotic in the treatment of anaerobic infections associated with diarrheal disease as well as clostridium difficile infections. 1

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Evaluation of the fluid uptake kinetics and drug release from gellan gum tablets containing metronidazole

Cited by 35 publications

References 23 publications

Gellan gum microspheres crosslinked with trivalent ion: effect of polymer and crosslinker concentrations on drug release and mucoadhesive properties

Gellan gum microspheres crosslinked with trivalent ion: effect of polymer and crosslinker concentrations on drug release and mucoadhesive properties

Oral Sustained Release Tablets of Zidovudine Using Binary Blends of Natural and Synthetic Polymers

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