Tablets compressed with gastric floating pellets coated with acrylic resin for gastro retention and sustained release of famotidine: in-vitro and in-vivo study

Qi, Xiaole; Jiang, Yunfeng; Zhang, Huiting; Wu, Zhenghong

doi:10.1111/jphp.12339

Cited by 8 publications

(6 citation statements)

References 25 publications

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“…Our experimental results also showed that PH 301 could prevent the pellets from being damaged. This is consistent with the experimental results by Xiaole Qi et al [ 26 ]. The best formulation of pulseⅠwas finally determined to be amoxicillin 69%, Avicel PH 301 25%, HPMC E5 4% and PVPP 2%.…”

Section: Resultssupporting

confidence: 94%

“…Based on the single factor experiment, four factors and three levels Box–Behnken design was carried through to get an optimal composition of the tablets by investigating the effect of the coating weight of Eudragit L30 D-55, the coating weight of AQOAT AS-HF, the extrusion screen aperture and the compression forces. The dependent variables and independent variables were related by mathematical relationships [ 26 ]. The polynomial equations obtained were:…”

Section: Resultsmentioning

confidence: 99%

“…The coefficients before (X 1 ~ X 4 ) indicated the independent variables were dependent on each other. The coefficients with more than one factor term and those with higher order terms represented interaction terms and quadratic relationships [ 26 ]. A plus sign expresses a synergistic effect and a subtraction sign indicates an antagonistic effect [ 26 ].…”

Section: Resultsmentioning

confidence: 99%

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A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling

Chai

Yang

et al. 2016

PLoS ONE

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BackgroundAmoxicillin is a commonly used antibiotic which has a short half-life in human. The frequent administration of amoxicillin is often required to keep the plasma drug level in an effective range. The short dosing interval of amoxicillin could also cause some side effects and drug resistance, and impair its therapeutic efficacy and patients’ compliance. Therefore, a three-pulse release tablet of amoxicillin is desired to generate sustained release in vivo, and thus to avoid the above mentioned disadvantages.MethodsThe pulsatile release tablet consists of three pulsatile components: one immediate-release granule and two delayed release pellets, all containing amoxicillin. The preparation of a pulsatile release tablet of amoxicillin mainly includes wet granulation craft, extrusion/spheronization craft, pellet coating craft, mixing craft, tablet compression craft and film coating craft. Box–Behnken design, Scanning Electron Microscope and in vitro drug release test were used to help the optimization of formulations. A crossover pharmacokinetic study was performed to compare the pharmacokinetic profile of our in-house pulsatile tablet with that of commercial immediate release tablet. The pharmacokinetic profile of this pulse formulation was simulated by physiologically based pharmacokinetic (PBPK) model with the help of Simcyp®.Results and DiscussionSingle factor experiments identify four important factors of the formulation, namely, coating weight of Eudragit L30 D-55 (X1), coating weight of AQOAT AS-HF (X2), the extrusion screen aperture (X3) and compression forces (X4). The interrelations of the four factors were uncovered by a Box–Behnken design to help to determine the optimal formulation. The immediate-release granule, two delayed release pellets, together with other excipients, namely, Avicel PH 102, colloidal silicon dioxide, polyplasdone and magnesium stearate were mixed, and compressed into tablets, which was subsequently coated with Opadry® film to produce pulsatile tablet of amoxicillin. In vitro release study firstly indicated a three-pulse release profile of the tablet. Later the pulse tablet was found to generate the sustained release of amoxicillin in beagle dogs. Furthermore, the Simcyp® software was used to simulate the in vivo concentration time curve model of the three-pulse release tablet for amoxicillin in both human and beagle dog. The prediction by PBPK model nicely fitted the observation in human and beagle dog.ConclusionsThis study has demonstrated the interrelation of factors affecting the pulsatile formulation of amoxicillin using a Box–Behnken design. The three-pulse release tablets of amoxicillin were proven to generate pulsatile release in vitro and sustained release in vivo. This formulation was also found to extend the effective plasma concentration in human compared to the tablet of immediate release based on the simulation data by PBPK modeling. This study provides an example of using PBPK to guide the development of pulsatile dosage forms.

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Section: Resultssupporting

confidence: 94%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling

Chai

Yang

et al. 2016

PLoS ONE

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“…Gastro-retentive systems (floating tablets, pellets or beads) were successfully developed and evaluated for several category of drugs like antihistamines (cetrizeine, famotidine, ranitidine), NSAIDS (ketorolac, celecoxib), antibiotics (metronidazole, ofloxacin, amoxicillin), antidiabetics (metformin, repaglinide) and many more [8][9][10][11][12][13][14][15][16][17] .…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of floating tablets of pregabalin

Kanwar

Kumar

Sarwal

et al. 2015

Drug Development and Industrial Pharmacy

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Floating tablets of pregabalin were prepared using different concentrations of the gums (xanthan gum and guar gum), Carbopol 974P NF and HPMC K100. Optimized formulations were studied for physical tests, floating time, swelling behavior, in vitro release studies and stability studies. In vitro drug release was higher for tablet batches containing guar and xanthan gum as compared to the batches containing Carbopol 974P NF. Tablet batches were subjected to stability studies and evaluated by different parameters (drug release, drug content, FTIR and DSC studies). The optimized tablet batch was selected for in vivo pharmacodynamic studies (PTZ induced seizures). The results obtained showed that the onset of jerks and clonus were delayed and extensor phase was abolished with time in treated groups. A significant difference (p > 0.05) was observed in control and treated group behavior indicating an excellent activity of the formulation for a longer period (>12 h).

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“…Obtention of immediate-release systems, with a focus on masking drug flavor (Hamedelniel, Bajdik, Pintye-Hódi, 2010;Issa et al, 2012b;Patel, Patel, Patel, 2010);  Controlled-release (Abbaspour, Sadeghi, Garekani, 2008;Bialleck, Rein, 2011;Cantor, Hoag, Augsburger, 2009a;Cantor, Hoag, Augsburger, 2009b;Franc et al, 2015;Ghanam, Kleinebudde, 2011;Ghosh, Chakraborty, 2013;Han et al, 2013;Heckötter et al, 2011;Hung et al, 2015;Ríos, Ghaly, 2015;Roblegg et al, 2011;Szkutnik-Fiedler et al, 2014;Wang et al, 2015;Xu, Liew, Heng, 2015;You et al, 2014);  Improvement in dissolution of poorly soluble drugs (Abdalla, Mader, 2007;Abdalla, Klein, Mader, 2008;Chopra, Venkatesan, Betageri, 2013;Ibrahim, El-Badry, 2014;Lu et al, 2009;Patel et al, 2016);  Gastro-retentive systems/ floating systems (Amrutkar, Chaudhari, Patil, 2012;Li et al, 2014;Pagariya, Patil, 2013;Qi et al, 2015;Zhang et al, 2012);  Enteric release/gastro-resistant systems (Andreo-Filho et al, 2009;Ghanam, Kleinebudde, 2011;Pund et al, 2010);  Improvement of plant extract or active ingredient stability (Araújo-Junior et al, 2013;Beringhs et al, 2012;Bu...…”

Section: Multiparticulate Dosage Forms and Drug Delivery Systemsmentioning

confidence: 99%

Physical characterization of multiparticulate systems

Issa

Souza

Duque

et al. 2018

Braz. J. Pharm. Sci.

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The search for new pharmaceutical dosage forms and different drug delivery systems already used in therapeutics is a global trend, serving as an opportunity to expand the portfolio for the pharmaceutical industry. In this context, multiparticulate systems, such as pellets, granules, and minitablets, represent an attractive alternative, given the range of possibilities they provide. Among the methods used in the production of these systems, we highlight the process of extrusion-spheronization for pellet manufacture, wet granulation and hot-melt extrusion for the obtention of granules, and direct compression for minitablets. Although highly versatile, depending on the technology chosen, many processes and formulation variables can influence the ensuing stages of manufacture, as well as the final product. Therefore, the characterization of these small units is of fundamental importance for achieving batch homogeneity and optimal product performance. Analyses, including particle size distribution, morphology, density, porosity, mechanical strength and disintegration, are example tests used in this characterization. The objective of this review was to address the most widely used tests for the physical evaluation of multiparticulate systems.

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Tablets compressed with gastric floating pellets coated with acrylic resin for gastro retention and sustained release of famotidine: in-vitro and in-vivo study

Abstract: The experimental results indicated that the optimized formulation did offer a new gastro retention and sustained release approach to enhance the oral absorption of famotidine.

Cited by 8 publications

References 25 publications

A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling

A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling

Preparation and evaluation of floating tablets of pregabalin

Physical characterization of multiparticulate systems

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