Optimization and characterization of gastroretentive floating drug delivery system using Box-Behnken design

Rapolu, Kishore; Sanka, Krishna; Vemula, Praveen Kumar; Aatipamula, Vinaydas; Mohd, Abdul Bari; Diwan, Prakash V.

doi:10.3109/03639045.2012.699068

Cited by 33 publications

(18 citation statements)

References 39 publications

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“…The interaction of X 2 and X 3 was significant and has a positive effect on Y 2 , Y 4 , and Y 8 . The optimized formulation PR9 was selected on the basis of a better drug‐release pattern at 2, 4, and 8 h. Rapolu et al . studied the effect of different polymer concentrations on the release profile of GERD of metronidazole by using BBD.…”

Section: Resultsmentioning

confidence: 99%

“…Box–Behnken designs (BBD) are response surface designs, especially made to require only three levels, coded as −1, 0, and +1. A BBD was used to make a polynomial model for optimization of bilayer tablets, keeping three independent variables and three dependent variables using Design‐Expert (version 7.1, Stat‐Ease Inc., Minneapolis, MN). The independent variables were percentages of pectin ( X 1 ), HPMC K100M ( X 2 ), and sodium bicarbonate (X 3 ), and the dependent variables were % drug release at 2 h ( Y 2 ), 4 h ( Y 4 ), and 8 h ( Y 8 ), as shown in Table .…”

Section: Methodsmentioning

confidence: 99%

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pH‐Sensitive pectin polymeric rafts for controlled‐release delivery of pantoprazole sodium sesquihydrate

Abbas

Hanif

2016

J of Applied Polymer Sci

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The aim of the present work was to develop pectin raft-forming tablets for controlled-release delivery of pantoprazole sodium sesquihydrate (PSS). A Box-Behnken design was used to optimize 15 formulations with three independent and three dependent variables. The physical tests of all compressed formulations were within pharmacopoeial limits. The rafts were characterized by their strength, thickness, resilience, reflux resistance, acid-neutralizing capacity, floating lag time, and total floating time. The raft strength, thickness, resilience, and reflux resistance through a 10-mm orifice of optimized formulation PR9 were 7.43 6 0.019 g, 5.8 6 0.245 cm, greater than 480 min, and 2490 6 0.004 g, respectively. The buffering and neutralizing capacity was 11.2 6 1.01 meq and 6.5 6 0.56 meq, respectively. Dissolution studies were performed by using simulated gastric fluid at pH 1.2, and the cumulative percentage release of PR9 was found to be 97%. First-order release kinetics were followed, and non-Fickian diffusion was observed as the value of n was greater than 0.45 in the Korsmeyer-Peppas model. The Fourier transform infrared spectra of the PSS, polymers, and optimized raft formulation PR9 showed peaks at 3223.09 cm 21 , 1688.17 cm 21 , 1586.67 cm 21 , 1302.64 cm 21 , and 1027.74 cm 21 that are due to AOH stretching, ester carbonyl group (C@O) stretching, the existence of water and carboxylic groups in the raft, CAN stretching, and AOH bending vibrations and showed no interaction between them. The developed raft was suitable for sustained-release delivery of PSS.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

pH‐Sensitive pectin polymeric rafts for controlled‐release delivery of pantoprazole sodium sesquihydrate

Abbas

Hanif

2016

J of Applied Polymer Sci

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“…After preliminary screening, formulation and optimization of fast dissolving films was carried out using Box-Behnken experimental design. [15] and sweetener (alitame) were obtained from Xylopia Research Center, Ahmedabad, India. All other chemicals used were of analytical grade.…”

Section: Original Articlementioning

confidence: 99%

Application of Box-Behnken design to formulate and optimize multipolymeric fast dissolving film of rizatriptan benzoate

Mehta¹,

Dave²,

Dadhaniya³

et al. 2014

Asian J Pharm

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T he present investigation aims at formulation and optimization of multipolymeric fast dissolving film of rizatriptan benzoate.Three film forming polymers namely hydroxypropyl methylcellulose (HPMC), maltodextrin and polyvinylalcohol were explored using Box-Behnken experimental design to derive optimized fast dissolving film formulation using desirability function. Analysis of variance (ANOVA) was performed for five dependent variables tensile strength, folding endurance, load at yield, percentage elongation and percentage drug release in 30 s (Q 30 ). Mathematical regression equations were derived by applying ANOVA and validated using checkpoint batches. Results of the experimental design exposed that the effect of independent factors HPMC and maltodextrin significantly influenced the mechanical properties and percentage drug release from the film. Optimized batch was derived based on set criteria using desirability function. Reponses of the optimized formulation were tensile strength (500 N/m 2 ), folding endurance (203), load at yield (15.06 N/m 2 ), percentage elongation (4.56%) and Q 30 (60.03%) falling under acceptable limits. High percentage drug release from the film in simulated saliva and simulated gastric fluid reveal fast dissolving characteristics. Fast dissolving dosage form can help patients with diseases like migraine.

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“…Moreover, the release of the drug is often disturbed by the floatation mechanism adopted. For example, frequently described floating drug delivery systems are swellable matrices, in which the floatation is determined by the bubbles, produced by a gas-generating agent, entrapped in the gel layer 12,13 . Since the bubbles develop in the gel layer, their presence interferes with the release of drug due to the fact that the gel layer controls the drug release.…”

Section: Introductionmentioning

confidence: 99%

Floating modular drug delivery systems with buoyancy independent of release mechanisms to sustain amoxicillin and clarithromycin intra-gastric concentrations

Rossi

Conti

Colombo

et al. 2015

Drug Development and Industrial Pharmacy

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Release modules of amoxicillin and clarithromycin combined in a single dosage form designed to float in the gastric content and to sustain the intra-gastric concentrations of these two antibiotics used for the eradication of Helicobacter pylori have been studied. The modules having a disc shape with curved bases were formulated as hydrophilic matrices. Two modules of clarithromycin were assembled by sticking the concave base of one module to the concave base of the other, creating an internal void chamber. The final dosage form was a floating assembly of three modules of clarithromycin and two of amoxicillin in which the drug release mechanism did not interfere with the floatation mechanism. The assembled system showed immediate in vitro floatation at pH 1.2, lasting 5 h. The in vitro antibiotics release profiles from individual modules and assembled systems exhibited linear release rate during buoyancy for at least 8 h. The predicted antibiotic concentrations in the stomach maintained for long time levels significantly higher than the respective minimum inhibitory concentrations (MIC). In addition, an in vivo absorption study performed on beagle dogs confirmed the slow release of clarithromycin and amoxicillin from the assembled system during the assembly's permanence in the stomach for at least 4 h.

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Optimization and characterization of gastroretentive floating drug delivery system using Box-Behnken design

Abstract: It can be concluded that a combination of hydroxypropyl methylcellulose K 15M, sodium carboxy methylcellulose and NaHCO3 can be used to increase the gastric residence time of the dosage form to improve local effect of metronidazole.

Cited by 33 publications

References 39 publications

pH‐Sensitive pectin polymeric rafts for controlled‐release delivery of pantoprazole sodium sesquihydrate

pH‐Sensitive pectin polymeric rafts for controlled‐release delivery of pantoprazole sodium sesquihydrate

Application of Box-Behnken design to formulate and optimize multipolymeric fast dissolving film of rizatriptan benzoate

Floating modular drug delivery systems with buoyancy independent of release mechanisms to sustain amoxicillin and clarithromycin intra-gastric concentrations

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