pH responsive alginate polymeric rafts for controlled drug release by using box behnken response surface design

Abstract

Aim of the present work was to develop alginate raft forming tablets for controlled release pantoprazole sodium sesquihydrate (PSS). Box behnken design was used to optimize 15 formulations with three independent and three dependent variables. Physical tests of all formulations were within pharmacopoeial limits. Raft was characterized by their strength, thickness, resilience, acid neutralizing capacity, floating lag time and total floating time. Raft strength, thickness and resilience of optimized formulation AR9 were 7.43 ± 0.019 g, 5.8 ± 0.245 cm and greater than 480 min, respectively. Buffering and neutralizing capacity were 11.2 ± 1.01 and 6.5 ± 0.56 meq, respectively. Dissolution studies were performed by using simulated gastric fluid pH 1.2 and cumulative percentage release of optimized formulation AR9 was found 98%. First order release kinetics were followed and non-fickian diffusion was observed as value of n was greater than 0.45 in korsmeyer-peppas model. PSS, polymers, tablets and rafts were further characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). FTIR spectra of PSS, polymers and raft of optimized formulation AR9 showed peaks at 3223.09, 1688.17, 1586.67, 1302.64 and 1027.74 cm−1 due to –OH stretching, ester carbonyl group (C=O) stretching, existence of water and carboxylic group in raft, C–N stretching and –OH bending vibration showed no interaction between them. XRD showed diffraction lines indicates crystalline nature of PSS. DSC thermogram showed endothermic peaks at 250 °C for PSS. The developed raft was suitable for controlled release delivery of PSS.

<p>Enhancement of Oral Bioavailability of Ibandronate Through Gastroretentive Raft Forming Drug Delivery System: In Vitro and In Vivo Evaluation</p>

“…The TFT of all prepared formulations ranged from 5-6 hours. Abbas et al 10 observed a similar pattern of FLT and TFT of alginate raft forming formulations.…”

“…Antacids are also trapped in the polymeric gel to extend the neutralization time. 10 The antacids in the formulation immediately neutralize the acid in the stomach and reduce the burning sensation. A raft was effectively formed on the surface of the SGF when adding tablets of formulations PPR1 to PPR5, but a raft did not develop when adding formulations PPR6 to PPR9.…”

“…The tablet was placed in 50 mL of four different acidic mediums, ie, SGF, 0.1, 0.5, and 1.0 N HCl solution in 250 mL capacity beaker. The temperature was maintained at 37ºC and 2 mL of sample was collected at5,10,15,20,25, 30, 45, and 60 minutes. The same volume of fresh dissolution medium was added into the beaker containing tablets for dissolution study to maintain the sink condition.…”

Gum Karaya-G-Poly (Acrylamide): Microwave Assisted Synthesis, Optimisation and Characterisation

“…Where Y is the measured response of the dependent variables, β0 is the intercept, β1-β9 are the regression coefficients computed from the observed experimental values of Y. X1, X2 and X3 are the coded value of the independent variables. X1 X2X3 (a, b = 1, 2, 3) and X 2 i (i = 1, 2, 3) represent the interaction and quadratic terms, respectively [16,17]. The graft copolymer of karaya with acrylamide was characterized by FTIR, DSC, XRD and SEM and % grafting (%G) and % grafting efficiency (%GE) were calculated by using following equations [18]:…”

Sodium alginate and pectin estimation in raft forming pharmaceuticals by high performance liquid chromatography method

“…The physicochemical properties of sodium alginate, the sodium salt of alginic acid, indicate that this natural macromolecule is biodegradable, nontoxic and pH sensitive in nature; in addition, the pH sensitivity of the polymer makes it stable only in an acidic environment, while in alkaline media, rapid dissolution occurs, which leads to instability and limits its applications. Sodium alginate swells in water but typically produces an acid pH gel due to its protonation and can be crosslinked by the application of physical and chemical methods [1]. The chemical structure of alginate, as mentioned in Fig.…”