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D.v. Derle - One of the best experts on this subject based on the ideXlab platform.
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Effect of Polacrilin Potassium as Disintegrant on Bioavailability of Diclofenac Potassium in Tablets : a Technical Note
AAPS PharmSciTech, 2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Polacrilin potassium is an ion exchange resin used in oral pharmaceutical formulations as a tablet disintegrant. It is a weakly acidic cation exchange resin. Chemically, it is a partial potassium salt of a copolymer of methacrylic acid with divinyl benzene. It ionizes to an anionic polymer chain and potassium cations. It was hypothesized that Polacrilin potassium may be able to improve the permeability of anionic drugs according to the Donnan membrane phenomenon. The effect of Polacrilin potassium on the permeability of diclofenac potassium, used as a model anionic drug, was tested in vitro using diffusion cells and in vivo by monitoring serum levels in rats. The amount of drug permeated across a dialysis membrane in vitro was significantly more in the presence of Polacrilin potassium. Significant improvement was found in the extent of drug absorption in vivo . It could be concluded that Polacrilin potassium may be used as a high-functionality excipient for improving the bioavailability of anionic drugs having poor gastrointestinal permeability.
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Effect of Sorbed Water on Disintegrant Performance of Four Brands of Polacrilin Potassium NF
AAPS PharmSciTech, 2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Polacrilin Potassium NF is a commonly used weak cation exchange resin disintegrant in pharmaceutical tablets. The objective of this research was to evaluate the effects of sorbed moisture on physical characteristics and disintegrant performance of four brands of Polacrilin Potassium NF. The disintegrants were stored in five different relative humidity chambers and their dynamic vapor adsorption–desorption analysis, effect of moisture on their compressibility, compactability, particle size, morphology, water uptake rate, and disintegration ability were studied. Moisture seemed to plasticize the disintegrants, reducing their yield pressures. However, certain optimum amount of moisture was found to be useful in increasing the compactablity of the tablets containing disintegrants. The tablets, however, lost their tensile strengths beyond this optimum moisture content. Moisture caused two brands of the disintegrants to swell; however, two other brands aggregated upon exposure to moisture. Swelling without aggregation increased the water uptake, and in turn the disintegrant performance. However, aggregation probably reduced the porosities of the disintegrants, reducing their water uptake rate and disintegrant performance. Different brands of Polacrilin Potassium NF differed in the abilities to withstand the effects of moisture on their functionality. Effect of moisture on disintegrant performance of Polacrilin Potassium NF needs to be considered before its use in tablets made by wet granulation.
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Brief/Technical Note Effect of Polacrilin Potassium as Disintegrant on Bioavailability of Diclofenac Potassium in Tablets: a Technical Note
2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Abstract. Polacrilin potassium is an ion exchange resin used in oral pharmaceutical formulations as a tablet disintegrant. It is a weakly acidic cation exchange resin. Chemically, it is a partial potassium salt of a copolymer of methacrylic acid with divinyl benzene. It ionizes to an anionic polymer chain and potassium cations. It was hypothesized that Polacrilin potassium may be able to improve the permeability of anionic drugs according to the Donnan membrane phenomenon. The effect of Polacrilin potassium on the permeability of diclofenac potassium, used as a model anionic drug, was tested in vitro using diffusion cells and in vivo by monitoring serum levels in rats. The amount of drug permeated across a dialysis membrane in vitro was significantly more in the presence of Polacrilin potassium. Significant improvement was found in the extent of drug absorption in vivo. It could be concluded that Polacrilin potassium may be used as a high-functionality excipient for improving the bioavailability of anionic drugs having poor gastrointestinal permeability. KEY WORDS: bioavailability improvement; disintegrants; permeability enhancement; Polacrilin potassium
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Mechanism of disintegrant action of Polacrilin potassium: Swelling or wicking?
Acta Pharmaceutica Sinica B, 2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Abstract The effect of particle size, pH of medium, and presence of lubricant on the swelling behaviour, water uptake properties and disintegrant performance of Polacrilin potassium was examined. Particle size did not affect the bulk swelling of disintegrant particles when measured as settling volume, but increased the water uptake and decreased the disintegration time of tablets containing this disintegrant. An increase in the pH of the medium from acidic to neutral increased the bulk swelling of the particles, whereas it decreased water uptake and disintegrant performance. Addition of lubricant had no effect on settling volume, but decreased the water uptake rate and the disintegrant performance significantly. It is concluded that wicking, i.e. capillary action, rather than swelling, is the major factor that contributes to the disintegration behaviour of Polacrilin potassium.
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Brand to brand variation in the disintegrant functionality of Polacrilin Potassium, NF.
Journal of Excipients and Food Chemicals, 2011Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:The current monograph for Polacrilin Potassium NF does not specify tests that could help in distinguishing between different brands of this disintegrant. The objective of this work was to study the physical characteristics of four brands of Polacrilin Potassium NF and relate the observed differences to the differences in their functionality. Significant differences were observed in particle size, true density, porosity, surface area, viscosity and morphology of the samples of the four brands of Polacrilin Potassium NF. Functionality tests such as settling volume, intrinsic swelling, rate and extent of water uptake were performed. The differences in settling volumes were not significant. However, significant differences were observed in intrinsic swelling and initial rate of water uptake rate. The disintegration times of the tablets were found to be a function of the rate of water uptake in the initial few seconds of disintegration. Since the disintegration times were observed to be significantly different in spite of negligible differences in settling volumes, wicking and water uptake appear to be the major mechanism of disintegration performance for Polacrilin Potassium NF. The measurement of water uptake rate may be a useful functionality test for ion exchange resin disintegrants. The settling volume test, however, was unable to distinguish between the samples of different sources of Polacrilin Potassium NF.
Mrudula H. Bele - One of the best experts on this subject based on the ideXlab platform.
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Effect of Polacrilin Potassium as Disintegrant on Bioavailability of Diclofenac Potassium in Tablets : a Technical Note
AAPS PharmSciTech, 2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Polacrilin potassium is an ion exchange resin used in oral pharmaceutical formulations as a tablet disintegrant. It is a weakly acidic cation exchange resin. Chemically, it is a partial potassium salt of a copolymer of methacrylic acid with divinyl benzene. It ionizes to an anionic polymer chain and potassium cations. It was hypothesized that Polacrilin potassium may be able to improve the permeability of anionic drugs according to the Donnan membrane phenomenon. The effect of Polacrilin potassium on the permeability of diclofenac potassium, used as a model anionic drug, was tested in vitro using diffusion cells and in vivo by monitoring serum levels in rats. The amount of drug permeated across a dialysis membrane in vitro was significantly more in the presence of Polacrilin potassium. Significant improvement was found in the extent of drug absorption in vivo . It could be concluded that Polacrilin potassium may be used as a high-functionality excipient for improving the bioavailability of anionic drugs having poor gastrointestinal permeability.
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Effect of Sorbed Water on Disintegrant Performance of Four Brands of Polacrilin Potassium NF
AAPS PharmSciTech, 2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Polacrilin Potassium NF is a commonly used weak cation exchange resin disintegrant in pharmaceutical tablets. The objective of this research was to evaluate the effects of sorbed moisture on physical characteristics and disintegrant performance of four brands of Polacrilin Potassium NF. The disintegrants were stored in five different relative humidity chambers and their dynamic vapor adsorption–desorption analysis, effect of moisture on their compressibility, compactability, particle size, morphology, water uptake rate, and disintegration ability were studied. Moisture seemed to plasticize the disintegrants, reducing their yield pressures. However, certain optimum amount of moisture was found to be useful in increasing the compactablity of the tablets containing disintegrants. The tablets, however, lost their tensile strengths beyond this optimum moisture content. Moisture caused two brands of the disintegrants to swell; however, two other brands aggregated upon exposure to moisture. Swelling without aggregation increased the water uptake, and in turn the disintegrant performance. However, aggregation probably reduced the porosities of the disintegrants, reducing their water uptake rate and disintegrant performance. Different brands of Polacrilin Potassium NF differed in the abilities to withstand the effects of moisture on their functionality. Effect of moisture on disintegrant performance of Polacrilin Potassium NF needs to be considered before its use in tablets made by wet granulation.
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Brief/Technical Note Effect of Polacrilin Potassium as Disintegrant on Bioavailability of Diclofenac Potassium in Tablets: a Technical Note
2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Abstract. Polacrilin potassium is an ion exchange resin used in oral pharmaceutical formulations as a tablet disintegrant. It is a weakly acidic cation exchange resin. Chemically, it is a partial potassium salt of a copolymer of methacrylic acid with divinyl benzene. It ionizes to an anionic polymer chain and potassium cations. It was hypothesized that Polacrilin potassium may be able to improve the permeability of anionic drugs according to the Donnan membrane phenomenon. The effect of Polacrilin potassium on the permeability of diclofenac potassium, used as a model anionic drug, was tested in vitro using diffusion cells and in vivo by monitoring serum levels in rats. The amount of drug permeated across a dialysis membrane in vitro was significantly more in the presence of Polacrilin potassium. Significant improvement was found in the extent of drug absorption in vivo. It could be concluded that Polacrilin potassium may be used as a high-functionality excipient for improving the bioavailability of anionic drugs having poor gastrointestinal permeability. KEY WORDS: bioavailability improvement; disintegrants; permeability enhancement; Polacrilin potassium
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Mechanism of disintegrant action of Polacrilin potassium: Swelling or wicking?
Acta Pharmaceutica Sinica B, 2012Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:Abstract The effect of particle size, pH of medium, and presence of lubricant on the swelling behaviour, water uptake properties and disintegrant performance of Polacrilin potassium was examined. Particle size did not affect the bulk swelling of disintegrant particles when measured as settling volume, but increased the water uptake and decreased the disintegration time of tablets containing this disintegrant. An increase in the pH of the medium from acidic to neutral increased the bulk swelling of the particles, whereas it decreased water uptake and disintegrant performance. Addition of lubricant had no effect on settling volume, but decreased the water uptake rate and the disintegrant performance significantly. It is concluded that wicking, i.e. capillary action, rather than swelling, is the major factor that contributes to the disintegration behaviour of Polacrilin potassium.
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Brand to brand variation in the disintegrant functionality of Polacrilin Potassium, NF.
Journal of Excipients and Food Chemicals, 2011Co-Authors: Mrudula H. Bele, D.v. DerleAbstract:The current monograph for Polacrilin Potassium NF does not specify tests that could help in distinguishing between different brands of this disintegrant. The objective of this work was to study the physical characteristics of four brands of Polacrilin Potassium NF and relate the observed differences to the differences in their functionality. Significant differences were observed in particle size, true density, porosity, surface area, viscosity and morphology of the samples of the four brands of Polacrilin Potassium NF. Functionality tests such as settling volume, intrinsic swelling, rate and extent of water uptake were performed. The differences in settling volumes were not significant. However, significant differences were observed in intrinsic swelling and initial rate of water uptake rate. The disintegration times of the tablets were found to be a function of the rate of water uptake in the initial few seconds of disintegration. Since the disintegration times were observed to be significantly different in spite of negligible differences in settling volumes, wicking and water uptake appear to be the major mechanism of disintegration performance for Polacrilin Potassium NF. The measurement of water uptake rate may be a useful functionality test for ion exchange resin disintegrants. The settling volume test, however, was unable to distinguish between the samples of different sources of Polacrilin Potassium NF.
Chamanlal Shishoo - One of the best experts on this subject based on the ideXlab platform.
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Exploring the potential of Polacrilin potassium as a novel superdisintegrant in microcrystalline cellulose based pellets prepared by extrusion-spheronization
Chronicles of Young Scientists, 2011Co-Authors: Amita Joshi, Swati Pund, Manish Nivsarkar, Kamala K. Vasu, Chamanlal ShishooAbstract:Polacrilin potassium (PP), an ion exchange resin, was used as a superdisintegrant to improve the dissolution of rifampicin, from microcrystalline cellulose (MCC) based pellets prepared by extrusion-spheronization. Production of fast release pellets by extrusion-spheronization using MCC is a complicated process. In the present study, pellets were prepared containing 50% w/w rifampicin (BCS class II drug) and 40% w/w MCC as extrusion-spheronization aid. Different levels of PP and lactose ratio investigated were 0:10, 2:8, 4:6, 6:4, 8:2, and 10:0. Pellets were evaluated for yield, size, size distribution, shape, porosity, friability, residual moisture, and dissolution efficiency (DE) at 30 minutes. Incorporation of this novel superdisintegrant had no adverse effect on the mechanical and micromeritic characteristics of pellets. All the batches of pellets showed high yields', ~90%; narrow particle size distribution; aspect ratio, 1.0-1.1; friability, 2 . Addition of Polacrilin results in significant improvement in the DE of rifampicin. The dissolution profiles were significantly different from the dissolution profile of pellets formulated without PP. This preliminary study indicates that PP can serve as an effective superdisintegrant in MCC pellets prepared by extrusion-spheronization.
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Exploring the potential of Polacrilin potassium as a novel superdisintegrant in microcrystalline cellulose based pellets prepared by extrusion-spheronization
Wolters Kluwer Medknow Publications, 2011Co-Authors: Amita K Joshi, Swati Pund, Manish Nivsarkar, Kamala K. Vasu, Chamanlal ShishooAbstract:Polacrilin potassium (PP), an ion exchange resin, was used as a superdisintegrant to improve the dissolution of rifampicin, from microcrystalline cellulose (MCC) based pellets prepared by extrusion-spheronization. Production of fast release pellets by extrusion-spheronization using MCC is a complicated process. In the present study, pellets were prepared containing 50% w/w rifampicin (BCS class II drug) and 40% w/w MCC as extrusion-spheronization aid. Different levels of PP and lactose ratio investigated were 0:10, 2:8, 4:6, 6:4, 8:2, and 10:0. Pellets were evaluated for yield, size, size distribution, shape, porosity, friability, residual moisture, and dissolution efficiency (DE) at 30 minutes. Incorporation of this novel superdisintegrant had no adverse effect on the mechanical and micromeritic characteristics of pellets. All the batches of pellets showed high yields′, ~90%; narrow particle size distribution; aspect ratio, 1.0-1.1; friability,
Satish K Mandlik - One of the best experts on this subject based on the ideXlab platform.
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Formulation and Optimization of Mouth dissolving tablets of Olanzapine by using 32 Factorial Design.
Research Journal of Pharmacy and Technology, 2011Co-Authors: Dinesh S. Nandare, Satish K Mandlik, Sachin K. Khiste, Yogesh D. MohiteAbstract:The objective of study deals with the Formulation and Optimization of Mouth dissolving tablets of Olanzapine with the application of Factorial Design. Olanzapine is well absorbed following an oral dose undergoes extensive first pass metabolism, resulting in systemic bioavailability of 50–60% only following oral administration. Prolonged release of the drug and increased bioavailability leads to significant reduction in dose and hence dose related side effects. For the formulation development Camphor and Polacrilin Potassium were selected as variable to formulate MDT of drug. A 32 factorial design was used to optimize the effect of the amounts of Polacrilin Potassium (superdisintegrant), X1 and Camphor(subliming agent), X2 which were independent variables. Direct compression method is used for the tablet Preparation. From the experimental design, drug release rate and profile is obtained. Relation between the dependent and independent variables are drawn out from the Mathematical equations and response surface plots. The result shows that the dissolution rate found to be increased. The results of a 32 full factorial design revealed that the amount of Polacrilin potassium and camphor significantly affect the dependent variables, disintegration time, and percentage friability. So conclusively successful development of Olanzapine MDT which improve the bioavailability of drug by providing an alternative to parenteral and other drug delivery of Olanzapine.
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Effect of Superdisintegrants on Olanzapine Oro-Dispersible Tablets
Research Journal of Pharmaceutical Dosage Forms and Technology, 2009Co-Authors: Satish K Mandlik, Dinesh S. Nandare, Mehul M Joshi, Pramod S Jagtap, Kishor S JainAbstract:This study investigated to compare the disintegration efficiency for the 5 classes of superdisintegrants represented by Cros-carmellose Sodium (CCS), Cros-povidone (CP), Polacrilin K (PK), Sodium Starch Glycolate (SSG), and L-Hydroxy Propyl Cellulose (L-HPC). Tablets were prepared by direct compression method. Effect of 5 superdisintegrants on disintegration time, dissolution parameters, and friability has been studied. Among all the superdisintegrants, a PK containing tablets has shown faster disintegration followed by SSG. Tablets containing L-HPC disintegrated after PK and SSG containing tablets.
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Statistical Optimization of Orodispersible Tablets Containing Telmisartan Using Factorial Design and Response Surface Methodology
Research Journal of Pharmacy and Technology, 2009Co-Authors: Satish K Mandlik, Dinesh S. Nandare, Mm Joshi, Pd Chudiwal, Ks JainAbstract:This study investigated utility of a 32 factorial design and Response Surface Methodology for orodispersible tablets containing Telmisartan. In an attempt to construct a statistical model for the prediction of disintegration time and percentage friability, a 32 factorial design was used to optimize the influence of the amounts of superdisintegrant (Polacrilin Potassium), X1 and subliming agent (Camphor), X2 which were independent variables. Tablets were prepared by direct compression with camphor sublimation method. Based on the experimental design, different drug release rates and profiles were obtained. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The obtained results showed that dispersion of the drug in the polymer considerably enhanced the dissolution rate. Concerning the optimization study, the multiple regression analysis revealed that an optimum concentration of camphor and higher concentration of Polacrilin potassium are required for obtaining rapidly disintegrating tablets. Hence, this investigation demonstrated the potential of the experimental design in understanding the effect of the formulation variables on the quality of orodispersible tablets containing Telmisartan.
Dinesh S. Nandare - One of the best experts on this subject based on the ideXlab platform.
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Formulation and Optimization of Mouth dissolving tablets of Olanzapine by using 32 Factorial Design.
Research Journal of Pharmacy and Technology, 2011Co-Authors: Dinesh S. Nandare, Satish K Mandlik, Sachin K. Khiste, Yogesh D. MohiteAbstract:The objective of study deals with the Formulation and Optimization of Mouth dissolving tablets of Olanzapine with the application of Factorial Design. Olanzapine is well absorbed following an oral dose undergoes extensive first pass metabolism, resulting in systemic bioavailability of 50–60% only following oral administration. Prolonged release of the drug and increased bioavailability leads to significant reduction in dose and hence dose related side effects. For the formulation development Camphor and Polacrilin Potassium were selected as variable to formulate MDT of drug. A 32 factorial design was used to optimize the effect of the amounts of Polacrilin Potassium (superdisintegrant), X1 and Camphor(subliming agent), X2 which were independent variables. Direct compression method is used for the tablet Preparation. From the experimental design, drug release rate and profile is obtained. Relation between the dependent and independent variables are drawn out from the Mathematical equations and response surface plots. The result shows that the dissolution rate found to be increased. The results of a 32 full factorial design revealed that the amount of Polacrilin potassium and camphor significantly affect the dependent variables, disintegration time, and percentage friability. So conclusively successful development of Olanzapine MDT which improve the bioavailability of drug by providing an alternative to parenteral and other drug delivery of Olanzapine.
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Effect of Superdisintegrants on Olanzapine Oro-Dispersible Tablets
Research Journal of Pharmaceutical Dosage Forms and Technology, 2009Co-Authors: Satish K Mandlik, Dinesh S. Nandare, Mehul M Joshi, Pramod S Jagtap, Kishor S JainAbstract:This study investigated to compare the disintegration efficiency for the 5 classes of superdisintegrants represented by Cros-carmellose Sodium (CCS), Cros-povidone (CP), Polacrilin K (PK), Sodium Starch Glycolate (SSG), and L-Hydroxy Propyl Cellulose (L-HPC). Tablets were prepared by direct compression method. Effect of 5 superdisintegrants on disintegration time, dissolution parameters, and friability has been studied. Among all the superdisintegrants, a PK containing tablets has shown faster disintegration followed by SSG. Tablets containing L-HPC disintegrated after PK and SSG containing tablets.
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Statistical Optimization of Orodispersible Tablets Containing Telmisartan Using Factorial Design and Response Surface Methodology
Research Journal of Pharmacy and Technology, 2009Co-Authors: Satish K Mandlik, Dinesh S. Nandare, Mm Joshi, Pd Chudiwal, Ks JainAbstract:This study investigated utility of a 32 factorial design and Response Surface Methodology for orodispersible tablets containing Telmisartan. In an attempt to construct a statistical model for the prediction of disintegration time and percentage friability, a 32 factorial design was used to optimize the influence of the amounts of superdisintegrant (Polacrilin Potassium), X1 and subliming agent (Camphor), X2 which were independent variables. Tablets were prepared by direct compression with camphor sublimation method. Based on the experimental design, different drug release rates and profiles were obtained. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The obtained results showed that dispersion of the drug in the polymer considerably enhanced the dissolution rate. Concerning the optimization study, the multiple regression analysis revealed that an optimum concentration of camphor and higher concentration of Polacrilin potassium are required for obtaining rapidly disintegrating tablets. Hence, this investigation demonstrated the potential of the experimental design in understanding the effect of the formulation variables on the quality of orodispersible tablets containing Telmisartan.