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Sample records for polyox wsr-fra polyox

  1. Design and Evaluation of Polyox and Pluronic Controlled Gastroretentive Delivery of Troxipide

    PubMed Central

    Jagdale, Swati C.; Kamble, Shraddha B.; Kuchekar, Bhanudas S.; Chabukswar, Aniruddha R.

    2014-01-01

    Objective. Objective of the present work was to develop site-specific gastroretentive drug delivery of Troxipide using polymers Pluronic F127 and Polyox 205?WSR. Troxipide is a novel gastroprotective agent with antiulcer, anti-inflammatory, and mucus secreting properties with elimination half-life of 7.4?hrs. Troxipide inhibits H. pylori-derived urease. It is mainly absorbed from stomach. Methods. 32 factorial design was applied to study the effect of independent variable. Effects of concentration of polymer on dependant variables as swelling index, hardness, and % drug release were studied. Pluronic F127 and Polyox 205?WSR were used as rate controlled polymer. Sodium bicarbonate and citric acid were used as effervescent-generating agent. Results. From the factorial batches, it was observed that formulation F5 (19% Pluronic F127 and 80% Polyox 205?WSR) showed optimum controlled drug release (98.60%?±?1.82) for 10?hrs with ability to float >12?hrs. Optimized formulation characterized by FTIR and DSC studies confirmed no chemical interactions between drug and polymer. Gastroretention for 6?hrs for optimized formulations was confirmed by in vivo X-ray placebo study. Conclusion. Results demonstrated feasibility of Troxipide in the development of gastroretentive site-specific drug delivery. PMID:25505995

  2. An Investigation on the Effect of Polyethylene Oxide Concentration and Particle Size in Modulating Theophylline Release from Tablet Matrices.

    PubMed

    Shojaee, Saeed; Emami, Parastou; Mahmood, Ahmad; Rowaiye, Yemisi; Dukulay, Alusine; Kaialy, Waseem; Cumming, Iain; Nokhodchi, Ali

    2015-12-01

    Polyethylene oxide has been researched extensively as an alternative polymer to hydroxypropyl methylcellulose (HPMC) in controlled drug delivery due to its desirable swelling properties and its availability in a number of different viscosity grades. Previous studies on HPMC have pointed out the importance of particle size on drug release, but as of yet, no studies have investigated the effect of particle size of polyethylene oxide (polyox) on drug release. The present study explored the relationship between polymer level and particle size to sustain the drug release. Tablets produced contained theophylline as their active ingredient and consisted of different polyethylene oxide particle size fractions (20-45, 45-90, 90-180 and 180-425 ?m). It was shown that matrices containing smaller particle sizes of polyox produced harder tablets than when larger polyox particles were used. The release studies showed that matrices consisting of large polyox particles showed a faster release rate than matrices made from smaller particles. Molecular weight (MW) of the polymer was a key determining step in attaining sustained release, with the high MW of polyox resulting in a delayed release profile. The results showed that the effect of particle size on drug release was more detrimental when a low concentration of polyox was used. This indicates that care must be taken when low levels of polyox with different particle size fractions are used. More robust formulations could be obtained when the concentration of polyox is high. Differential scanning calorimetry (DSC) traces showed that particle size had no major effect on the thermal behaviour of polyox particles. PMID:25771738

  3. Optimization Studies on Compression Coated Floating-Pulsatile Drug Delivery of Bisoprolol

    PubMed Central

    Jagdale, Swati C.; Bari, Nilesh A.; Kuchekar, Bhanudas S.; Chabukswar, Aniruddha R.

    2013-01-01

    The purpose of the present work was to design and optimize compression coated floating pulsatile drug delivery systems of bisoprolol. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The rapid release core tablet (RRCT) was prepared by using superdisintegrants with active ingredient. Press coating of optimized RRCT was done by polymer. A 32 full factorial design was used for optimization. The amount of Polyox WSR205 and Polyox WSR N12K was selected as independent variables. Lag period, drug release, and swelling index were selected as dependent variables. Floating pulsatile release formulation (FPRT) F13 at level 0 (55?mg) for Polyox WSR205 and level +1 (65?mg) for Polyox WSR N12K showed lag time of 4?h with >90% drug release. The data were statistically analyzed using ANOVA, and P < 0.05 was statistically significant. Release kinetics of the optimized formulation best fitted the zero order model. In vivo study confirms burst effect at 4?h in indicating the optimization of the dosage form. PMID:24367788

  4. Blood flow velocity measurements in rat mesentery arterioles in health and under hypertensive conditions

    NASA Astrophysics Data System (ADS)

    Polyakova, Marina S.; Sokolova, Irina A.; Priezzhev, Alexander V.; Proskurin, Sergei G.; Savchenko, Natalia B.; Shakhnazarov, Alexander A.

    1994-07-01

    Laser Doppler measurements of blood flow velocities in the vessels of rat mesentery have been performed to study the effect of the drag-reducing agent polyethylene oxide Polyox WSR-301 on microcirculation. These agents are capable of increasing the cardiac output and decreasing the arterial pressure. Measurements performed on spontaneously hypertensive rats anesthetized by Nembutal showed that the mean blood velocities in all groups of studied vessels are higher (by nearly two to three times) as compared to those in controls. Most likely these results reflect the effects of hypertensive raising pressure drop and the `rarefaction' phenomenon.

  5. Investigating the cubosomal ability for transnasal brain targeting: In vitro optimization, ex vivo permeation and in vivo biodistribution.

    PubMed

    Abdelrahman, Fatma Elzahraa; Elsayed, Ibrahim; Gad, Mary Kamal; Badr, Ahmed; Mohamed, Magdi Ibrahim

    2015-07-25

    The aim of this study was to enhance the risperidone delivery to the brain through the transnasal route via optimization of cubosomal gel. Cubosomes were prepared using glycerol mono-oleate (GMO), Pluronic F127 (PF127) and Tween 80 (T80). The prepared formulae were characterized by testing their particle size, polydispersity index, zeta potential, entrapment efficiency, in vitro drug release and transmission electron microscopy. Central composite design was planned for the formulae optimization and the selected formula (containing PF127 with concentration 15 mg/g GMO and T80 with concentration of 20mg/L) was re-prepared in presence of gelling polymer (gellan gum or polyox). The optimal cubosomal gel (containing 0.4% w/v polyox) had been subjected to ex-vivo permeation, histopathological evaluation and in vivo biodistribution studies. It showed significantly higher transnasal permeation and better distribution to the brain, when compared to the used control (drug solution and/or suspension). Finally, the cubosomal gel could be considered as a promising carrier for brain targeting of CNS acting drugs through the transnasal route. PMID:26026251

  6. Formulation Optimization of Hot Melt Extruded Abuse Deterrent Pellet Dosage Form Utilizing Design of Experiments (DOE)

    PubMed Central

    Maddineni, Sindhuri; Battu, Sunil Kumar; Morott, Joe; Majumdar, Soumyajit; Repka, Michael A.

    2014-01-01

    The objective of the present study was to develop techniques for an abuse-deterrent (AD) platform utilizing hot melt extrusion (HME) process. Formulation optimization was accomplished by utilizing Box-Behnken design of experiments to determine the effect of the three formulation factors: PolyOx™ WSR301, Benecel™ K15M, and Carbopol 71G; each of which was studied at three levels on TR attributes of the produced melt extruded pellets. A response surface methodology was utilized to identify the optimized formulation. Lidocaine Hydrochloride was used as a model drug, and suitable formulation ingredients were employed as carrier matrices and processing aids. All of the formulations were evaluated for the TR attributes such as particle size post-milling, gelling, percentage of drug extraction in water and alcohol. All of the DOE formulations demonstrated sufficient hardness and elasticity, and could not be reduced into fine particles (<150µm), which is a desirable feature to prevent snorting. In addition, all of the formulations exhibited good gelling tendency in water with minimal extraction of drug in the aqueous medium. Moreover, Benecel™ K15M in combination with PolyOx™ WSR301 could be utilized to produce pellets with TR potential. HME has been demonstrated to be a viable technique with a potential to develop novel abuse-deterrent formulations. PMID:24433429

  7. Particle-laden tubeless siphon

    NASA Astrophysics Data System (ADS)

    Joseph, Daniel; Wang, Jing

    2003-11-01

    A tubeless siphon was created by sucking a 1% aqueous Polyox(Polyox is a registered trademark of Union Carbide.) solution laden with particles from a beaker into a cylinder by a moving piston. The piston speed and particle concentration were varied. At very high rates of withdrawal, all the fluid could be removed before the siphon broke. In this case, the beaker was completely cleaned without a trace of liquid. The addition of small concentrations of small, nearly neutrally buoyant particles greatly enhanced the pulling power of the liquid, reducing the threshold speed of withdrawal at which the beaker was completely cleaned. At speeds of withdrawal smaller than the threshold not all of the fluid-particle mixture is pulled out of the beaker. The amount pulled out first increases, then decreases as the particle concentration is increased. We present an argument, based on viscoelastic potential flow, that the enhancement of the effective extensional stress is due to the reversal of the sign of the normal stresses at stagnation points on the particles.

  8. Polymer drag reduction in large diameter coal log pipeline

    SciTech Connect

    Wu, G.; Xu, J. Miles, J.

    1998-07-01

    A hydraulic capsule pipeline (HCP) drag reduction study is being conducted using a 210 mm inner diameter, 131 m long steel pipe loop located at the Research Park of the University of Missouri-Columbia (UMC). Polyox (trade name for polyethylene oxide) was tested alone and in combination with fiber for the first time for drag reduction investigations in such a large diameter HCP flow. A novel design of vacuum-aided Polyox dissolution and injection system was also tested for the first time in this pipeline. The injected polymer concentration present was determined on the basis of average concentration over the entire pipeline loop. Subsequently, more detailed data reduction will be presented based upon local polymer concentration in the test section determined by a dispersion model, which is being developed and will be calibrated to the experimental system using a fluorescent dye additive for experimental measurement. In addition, abrasion-resistant resin logs with cement additives for density control were employed to simulate coal logs. Results of this study not only answered some basic questions about drag reduction in HCP flow, it is also beneficial and important to HCP commercial applications.

  9. Polymer drag reduction in large diameter coal log pipeline

    SciTech Connect

    Wu, Gangwei; Miles, J.; Xu, Jihuai

    1998-04-01

    A hydraulic capsule pipeline (HCP) drag reduction study is being conducted using a 210 mm inner diameter, 131 m long steel pipe loop located at the Research Park of the University of Missouri-Columbia (UMC). Polyox (trade name for polyethylene oxide) was tested alone and in combination with fiber for the first time for drag reduction investigations in such a large diameter HCP flow. A novel design of vacuum-aided Polyox dissolution and injection system was also tested for the first time in this pipeline. The injected polymer concentration present was determined on the basis of average concentration over the entire pipeline loop. Subsequently, more detailed data reduction will be presented based upon local polymer concentration in the test section determined by a dispersion model, which is being developed and will be calibrated to the experimental system using a fluorescent dye additive for experimental measurement. In addition, abrasion-resistant resin logs with cement additives for density control were employed to simulate coal logs. Results of this study not only answered some basic questions about drag reduction in HCP flow, it is also beneficial and important to HCP commercial applications.

  10. D-optimal mixture design: optimization of ternary matrix blends for controlled zero-order drug release from oral dosage forms.

    PubMed

    El-Malah, Yasser; Nazzal, Sami; Khanfar, Nile M

    2006-01-01

    The objective of the present study was to develop a tablet formulation with a zero-order drug release profile based on a balanced blend of three matrix ingredients. To accomplish this goal, a 17-run, three-factor, two-level D-Optimal mixture design was employed to evaluate the effect of Polyox (X1), Carbopol (X2), and lactose (X3) concentrations on the release rate of theophylline from the matrices. Tablets were prepared by direct compression and were subjected to an in vitro dissolution study in phosphate buffer at pH 7.2. Polynomial models were generated for the responses Y4 (percent released in 8 h) and Y6 (similarity factor or f2). Fitted models were used to predict the composition of a formulation that would have a similar dissolution profile to an ideal zero-order release at a rate of 8.33% per hour. When tested, dissolution profile of the optimized formulation was comparable to the reference profile (f2 was 74.2, and n [release exponent] was 0.9). This study demonstrated that a balanced blend of matrix ingredients could be used to attain a zero-order release profile. Optimization was feasible by the application of response surface methodology, which proved efficient in designing controlled-release dosage forms. PMID:17090443

  11. Two different approaches for the prediction of in vivo plasma concentration-time profile from in vitro release data of once daily formulations of diltiazem hydrochloride.

    PubMed

    Bendas, Ehab R

    2009-09-01

    The aim of this study was to employ two different mathematical approaches: first, a convolution approach using computer software; second, a mathematical calculation exploiting Wagner-Nelson calculation to predict in vivo plasma concentration-time profile from the in vitro release study for the once daily formulations of a model drug diltiazem hydrochloride. The once daily extended release tablets (120 mg) were prepared by the wet granulation technique. Ethanol or ethanolic solutions of ethylcellulose (N22), were used as granulating agents along with hydrophilic matrix polymers like hydroxypropyl methylcellulose (HPMC) (K 15M). The granules showed satisfactory flow properties, compressibility, moisture content and drug content. All the tablet formulations showed acceptable properties and complied with pharmacopeial limits. The in vitro drug release study revealed that formula F7-T which contains drug: HPMC ratio 1:1 and 20 mg of ethylcellulose was able to sustain the drug release for 24 h and satisfied the USP dissolution limits. Fitting the in vitro drug release data to Korsmeyer-Peppas equation indicated that the mechanism of drug release could be zero-order. The capsule formulation F14-C which consists of drug: HPMC ratio 1:2, 12 mg of ethylcellulose and 20 mg of polyox 100 showed in vitro drug release similar to the tablet F7-T using the similarity factor (f 2). The mechanism of drug release could be coupled diffusion, and polymer matrix relaxation. The percent dissolved data from the two formulations were used as input function to predict the in vivo plasma data by the two approaches (Convolution by Kinetica software and Wagner-Nelson calculation). The two methods were validated by prediction of plasma data from in vitro release data of FDA approved 300 mg extended release capsule. Prediction errors were estimated for Cmax and area under the curve (AUC) to determine the validity of the methods. The percent prediction error for each parameter is not exceeding 15%. PMID:19784589

  12. Influence of Plasticizers on the Stability and Release of a Prodrug of ?9-Tetrahydrocannabinol Incorporated in Poly (Ethylene Oxide) Matrices

    PubMed Central

    Thumma, Sridhar; ElSohly, Mahmoud A.; Zhang, Shuang-Qing; Gul, Waseem; Repka, Michael A.

    2008-01-01

    The objective of the present research was to stabilize a heat-labile novel prodrug of ?9-tetrahydrocannabinol (THC), THC-hemiglutarate (THC-HG), in polyethylene oxide (PEO) [PolyOx® WSR N-80 (PEO N-80), MW 200,000 Daltons] polymeric matrix systems produced by hot-melt fabrication for systemic delivery of THC through the oral transmucosal route. For this purpose, the effects of processing conditions (processing temperature and heating duration), plasticizer type and concentration and storage conditions on the stability of the prodrug were investigated. The selected plasticizers studied included vitamin E succinate (VES), acetyltributyl citrate (ATBC), triethyl citrate (TEC), triacetin and polyethylene glycol 8000 (PEG 8000). Furthermore, the influence of plasticizer concentration on drug release was also studied. The stability of THC-HG in PEO matrices was influenced by all of the aforementioned variables. Films processed at 110 °C for 7 min were found to be favorable for hot-melt processing with a post- processing drug content of 95%, while significant degradation of THC-HG (~42%) was observed in those processed at 200 °C for 15 min. The degradation of the prodrug during hot-melt fabrication and also upon storage was considerably reduced in the presence of the plasticizers investigated, VES being the most effective. Modulation of the microenvironmental pH to an acidic range via incorporation of citric acid in PEO-plasticizer matrices significantly improved the stability of the prodrug, with almost 90% of the theoretical drug remaining as opposed to only 15% remaining in PEO-only matrices when stored at 40 °C for up to 3 months. The release of drug from PEO matrices was influenced both by the plasticizer type and concentration. A faster release resulted from water-soluble plasticizers, PEG 8000 and triacetin, and with increasing concentration. However, a slower release was observed with an increase in concentration of water-insoluble plasticizers, VES and ATBC. PMID:18602993