scholarly journals Improvement of fluconazole flowability and its effect on dissolution from tablets and capsules

2010 ◽  
Vol 46 (1) ◽  
pp. 115-120
Author(s):  
Vladi Olga Consiglieri ◽  
Samanta Mourão ◽  
Mauricio Sampaio ◽  
Patricia Granizo ◽  
Pedro Garcia ◽  
...  
Keyword(s):  
High Speed ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Wet Granulation ◽  
Flow Properties ◽  
Granulation Process ◽  
Index Data ◽  
Compressibility Index ◽  
Dissolution Efficiency

The aim of this work was to improve fluconazole flowability by wet granulation and to study the effect of granulation on drug dissolution from tablets and capsules. Fluconazole was submitted to a process of wet granulation in a high-speed granulator using Plasdone® K29/32 or K90. Flow properties of granules and dissolution profiles for tablets and capsules produced with them were determined. Fluconazole granules demonstrated better flowability, calculated by angle of repose and compressibility index data, compared with powder. Additionally, it was observed that the granulation process improved the dissolution efficiency (ED) of fluconazole from tablets and capsules, which could also suggest an increase in bioavailability. Higher dissolution efficiencies were achieved with Plasdone® K29/32.

FORMULASI GRANUL EFFERVESCENT EKSTRAK ETANOL 90% BUAH LABU AIR (Lagenaria siceraria) SEBAGAI ANTIOKSIDAN DENGAN VARIASI GAS GENERATING AGENT

2020 ◽  
Vol 5 (2) ◽  
pp. 220-229
Author(s):  
Dyera Forestryana ◽  
◽  
Yunitha Hestiarini ◽  
Aristha Novyra Putri
Keyword(s):  
Citric Acid ◽  
Moisture Content ◽  
Sodium Bicarbonate ◽  
Physical Properties ◽  
Tartaric Acid ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Lagenaria Siceraria ◽  
Flow Properties ◽  
Compressibility Index

Water pumpkin (Lagenaria siceraria) is a vegetable that contains secondary metabolites that are beneficial to health. Its use as a vegetable is less attractive to the people so that to increase its utilization, dosage forms are made that can attract public interest, one of which is effervescent granules. Effervescent granules are the most popular dosage form because they can serve in fresh drinks. This study aims to determine the effect of variations in the concentration of acids (citric acid-tartaric acid) and base (sodium bicarbonate) on the physical properties of the formula. The water pumpkin effervescent granules made with various ratios of citric acid, tartaric acid, and sodium bicarbonate consisting of FI (2: 1: 2.5); F II (1: 2: 2,5); F III (2: 1: 3,52); F IV (1: 2: 3,44). The granule made by the wet granulation method. The physical properties of the formula included organoleptic, moisture content, flow properties, compressibility index, pH, solubility time, and acceptability test. Based on the results of the evaluation of physical properties, the granule formula of the water pumpkin effervescent meets the standard requirements with a moisture content of 1.26% -2.26%, flow properties from 6.33 to 7.0 seconds, angle of repose 31.14˚-33.69 ˚, compressibility index 13.61% -17.08%, pH 6.1-7.1 and dissolving time 191-223.33 seconds. Variations of citric acid-tartaric acid and sodium bicarbonate affect the physical properties and taste of the effervescent granules. Based on the acceptability test showed that the panelists liked the water pumpkin effervescent granules in FII.

The Effect of the Wet Granulation Process on Drug Dissolution

1988 ◽  
Vol 14 (10) ◽  
pp. 1327-1349 ◽  
Author(s):  
Hoshang M. Unvala ◽  
Joseph B. Schwartz ◽  
Roger L. Schnaare
Keyword(s):  
Drug Dissolution ◽  
Wet Granulation ◽  
Granulation Process

Formulation and Evaluation of Immediate Release Tablets of Etizolam

2021 ◽  
pp. 281-284
Author(s):  
Abhishek Kumar Singh ◽  
Kasif Shakeel
Keyword(s):  
Immediate Release ◽  
Magnesium Stearate ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Compressibility Index ◽  
Tablet Hardness ◽  
In Vitro Disintegration

In the present investigation, immediate release tablet formulation of etizolam was developed for management of insomnia and anxiety using different Superdisintegrants (Sodium Starch Glycolate, Croscarmellose, Crospovidone), Povidone K-30 and Magnesium stearate by wet granulation method. The drug-excipients interaction was investigated by UV spectrophotometer. The granules and tablets of Etizolam were evaluated for various pre and post compression parameters like angle of repose, compressibility index, hausners ratio, tablet hardness, friability and in vitro disintegration and dissolution studies and their results were found to be satisfactory. These results suggest that maximum in vitro dissolution profile of formulation F6 were found to have equivalent percentage of drug release and concluded that F6 is better and similar to innovator product.

scholarly journals FORMULATION OF EFFERVESCENT GRANULES FROM RED GINGER (ZINGIBERIS OFFICINALE ROSCOE VAR. RUBRUM) EXTRACT AND ITS ANTIOXIDANT ACTIVITY

2022 ◽  
pp. 112-115
Author(s):  
DIAH LIA AULIFA ◽  
DIKI PRAYUGO WIBOWO ◽  
NENI SAFITRI ◽  
ARIF BUDIMAN
Keyword(s):  
Antioxidant Activity ◽  
Free Radicals ◽  
Physical Stability ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Flow Properties ◽  
Organoleptic Evaluation ◽  
Hausner Ratio ◽  
High Antioxidant Activity ◽  
Red Ginger

Objective: Ginger is one of the Indonesian plants that has been used as traditional medicine. The flavonoids and phenols compounds contained high antioxidant activity. This study aimed to formulate effervescent granules (EG) from red ginger (RG) extract and evaluate its antioxidant activity. Methods: The formulation of EG from RG extract was prepared by the wet granulation method using different concentrations of polyvinylpyrrolidone (PVP). Furthermore, the flowability of granules was evaluated, including flow rate, angle of repose, bulk density, tapped density, Carr's index, Hausner ratio, and effervescent time. The physical stability of granules such as organoleptic evaluation, effervescent time, and pH measurement was also evaluated after 28 d of storage, and the antioxidant activity of EG from RG extract was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Results: The result showed that the EG of RG extract was successfully prepared by wet granulation with a concentration of 15%. In addition, the flowability study showed that all formulas of EG from RG extract have good flow properties, and the granules showed excellent flow properties based on Carr′s index results. The effervescent time of granules remained within the acceptable range according to USP, and the physical stability did not change even after 28 d of storage. The IC50 of EG from RG extract was 283.28±3.6 ppm and has moderate in free radicals scavenging activity. Conclusion: EG from RG extract can be used as food supplements to protect the human body from free radicals and inhibit oxidases.

scholarly journals Physicochemical Characterization and Evaluation of the Binding Effect of Acacia etbaica Schweinf Gum in Granule and Tablet Formulations

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Kidan Haily Desta ◽  
Ebisa Tadese ◽  
Fantahun Molla
Keyword(s):  
Water Solubility ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hot Water ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Flow Properties ◽  
Disintegration Time ◽  
Binding Effect ◽  
Tablet Formulations

This study is aimed at evaluating the binding effect of Acacia etbaica gum in granule and tablet formulations using paracetamol as a model drug. Some physicochemical properties of the purified gum such as pH, the presence of tannin and dextrin, solubility, viscosity, loss on drying, total ash value, water solubility index, swelling power, moisture sorption, and powder flow properties were investigated. Paracetamol granules were prepared using wet granulation method at 2%, 4%, 6%, and 8% w / w of the Acacia etbaica gum and compared with granules prepared with reference binders (PVP K-30 and Acacia BP) in similar concentrations. The granules were characterized for bulk and tapped densities, compressibility index and Hausner ratio, angle of repose, flow rate, and friability. Finally, the prepared granules were compressed into tablets and evaluated for different tablet characteristics: weight uniformity, thickness, diameter, crushing strength, tensile strength, friability, disintegration time, and in vitro release profile. The physicochemical characterization revealed that tannins and dextrin are absent in the gum, and the gum has acidic pH. Both the moisture content and total ash values were within the official limits. Furthermore, the gum was found to be soluble in cold and hot water but insoluble in organic solvent and exhibited a shear thickening viscosity profile and excellent flow properties with excellent compressibility. The granules prepared with the gum of Acacia etbaica and reference binders showed good particle size distribution and excellent flow and compressibility properties. All the prepared tablets passed pharmacopeial specifications with respect to their uniformity of weight, thickness, and disintegration time. Tablets formulated with Acacia etbaica gum and acacia BP meet the compendial specification for friability at binder concentrations more than 2%. Drug release properties of all the batches formulated with Acacia etbaica, PVP, and acacia BP complied with the pharmacopeial specification. It can be concluded that the gum of Acacia etbaica could be explored as an alternative excipient for its binder effect in granule and tablet formulations.

scholarly journals Formulation and Evaluation of Ciprofloxacin Solid Dispersion Controlled Release Floating Capsules for Solubility Improvement

2017 ◽  
Vol 5 (03) ◽  
pp. 07-16
Author(s):  
Gaurav Subhash Katore ◽  
S. J. Bidkar ◽  
G. Y. Dama
Keyword(s):  
Controlled Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Evaluation Studies ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Wet Granulation ◽  
Weight Variation

Solid dispersions in water soluble carriers have attracted considerable interests as a mean of improving the dissolution rate and hence possibly bioavailability range of hydrophobic drugs. The poor solubility of ciprofloxacin leads to poor dissolution and hence variation in bioavailability. The purpose of present investigation was formulation and evaluation of controlled release floating capsule of ciprofloxacin with improved solubility and dissolution rate. In present study solid dispersion using various carriers like mannitol and lactose in different ratios were prepared by solvent evaporation method. The prepared solid dispersions were characterized for drug content, solubility and dissolution rate. The dissolution rate substantially improved for ciprofloxacin from its solid dispersions compared with pure drug. Dissolution rate increased with increase in carrier content. The dissolution rate was increased 3 folds with solid dispersions containing 1:4 of drug: lactose. The granules of ciprofloxacin solid dispersion containing 1:4 of drug: lactose ratio was prepared by wet granulation method using polymer such as ethyl cellulose and HPMC. The prepared granules were evaluated to preformulation studies such as angle of repose (18.41-24.22), bulk density, tapped density, compressibility index (11.31-12.75) and hausner’s ratio. All the parameters shows that the granules having good flow properties. These granules had converted into the capsule forms. Then the formulated capsules were taken to the evaluation studies such as weight variation, release study, buoyancy and floating duration (more than 6 hrs.). We can conclude that all the parameters were within the acceptable limits.

scholarly journals Formulation and evaluation of chewable tablets of Desloratadine prepared by aqueous and non-aqueous techniques

2020 ◽  
Vol 10 (1) ◽  
pp. 5-10
Author(s):  
Muhammad Abbas ◽  
Musharraf Abbas ◽  
Fatima Tariq ◽  
Rabiya Yasin ◽  
Muhammad Nabeel
Keyword(s):  
Magnesium Stearate ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Blue Color ◽  
Organoleptic Evaluation ◽  
Drug Content ◽  
Weight Variation ◽  
Compressibility Index ◽  
Tap Density ◽  
Chewable Tablets

In the modern era, chewable tablets are preferred over conventional dosage forms by pediatric, geriatric and bedridden patients due to difficulty in swallowing, lesser amount of water for swallowing medications as well as unable to tolerate the bitter taste of certain drugs. Chewable tablets of Desloratadine (DS) were formulated by aqueous and non-aqueous granulation method using water paste and Isopropyl alcohol (IPA) as a wetting agents respectively. Desloratadine is used to treat the symptoms of allergy such as sneezing, watery eyes. In the recent research, we have formulated eight trials by various concentrations of excipients. For instance; lactose, talcum, magnesium stearate, blue color, flavor, aspartame, mannitol, avicel 101 and polyvenylpyrollidine (PVP). Pre-compression and post compression parameters (thickness, hardness, friability weight variation and drug content) of the formulations were evaluated. B3 was our optimum dosage form because its Hausner’s ratio, compressibility index, bulk density, tap density, angle of repose have optimum values i.e. 1.01, 5.1%, 0.66(g/cc), 0.69(g/cc), 26.1º respectively and post-compression i.e. thickness, hardness, friability weight variation and drug content have values, 2.9mm, 3.9(kg/cm²), 0.6%, 99.5% respectively. Tablets prepared by wet granulation technique showed reasonable release profile i.e. 100% within the required time i.e. 2 hours.  Moreover, organoleptic evaluation of all formulations were performed. Keywords: Desloratadine, chewable, magnesium stearate, aspartame, compressibility, granulation.

scholarly journals Drug Technology in Hunting Practice

2021 ◽  
Vol 68 (1) ◽  
pp. 63-65
Author(s):  
S. Laca Megyesi ◽  
A. Königová ◽  
L. Molnár ◽  
M. Várady ◽  
M. Fedorová ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Particle Shape ◽  
Sem Analysis ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Hausner Ratio ◽  
Compressibility Index ◽  
Drug Technology ◽  
The Right ◽  
Shape And Size

Abstract Antiparasitic therapy in living ratites is based on the right dose and efficacy is only when the drug is pharmaceutically stable and safe. Ivermectin is considered to be the most widely used drug in the treatment of parasitosis in ruminants worlwide. For these reasons, in our study, we focused on the pharmaceutical investigation of ivermectin by SEM analysis of its powder particle shape and size, flow properties of solids (angle of repose, compressibility index, Hausner ratio) and zeta potential.

scholarly journals The effect of magnesium stearate and sodium starch glycolate on powder flowability

2019 ◽  
pp. 304-310
Author(s):  
Gordana Svonja-Parezanovic ◽  
Mladena Lalic-Popovic ◽  
Svetlana Golocorbin-Kon ◽  
Nemanja Todorovic ◽  
Nebojsa Pavlovic ◽  
...  
Keyword(s):  
Microcrystalline Cellulose ◽  
Magnesium Stearate ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Sodium Starch Glycolate ◽  
Compressibility Index ◽  
Powder Flowability ◽  
The Individual ◽  
Full Factorial ◽  
Spray Dried

The powder flow plays an important role in the manufacture of dosage form such as direct compression tablets. The objective of this research was to investigate the individual and interaction effects of magnesium stearate (MgSt) (Merck Ltd., Germany) as lubricant and sodium starch glycolate (SSG) (Primojel?) as superdesintegrator on powder flowability. Powder formulations were prepared by mixing different concentration of MgSt (0.25% and 5%) and SSG (0.5% and 4%) with microcrystalline cellulose (MCC) (Vivapur?101) or spray-dried lactose (LAC) (Super Tab 21AN) as diluents. Eight powder formulations were prepared using as filler LAC and MCC, as superdesintegrator SSG and as lubricant MgSt in ratios as follows: P1 (LAC : 0.5% SSG : 0.25% MgSt); P2 (LAC : 4% SSG : 5% MgSt); P3 (LAC : 0.5% SSG : 5% MgSt); P4 (LAC : 4% SSG : 5% MgSt); P5 (MCC : 0.5% SSG : 0.25% MgSt); P6 (MCC : 4% SSG : 5% MgSt); P7 (MCC : 0.5% SSG : 5% MgSt); P8 (MCC : 4% SSG : 0.25% MgSt). The powder formulations were evaluated using indirect methods of flowability evaluation according to 9th European Pharmacopoeia: measurement of tapped and bulk density (Ph.Eur.9, 2.9.34) and angle of repose (Ph.Eur. 2.9.36). Also, compressibility index, Hausner?s ratio were calculated. A full factorial design with three factors at two levels and response surface methodology were applied to evaluate the influence of various concentrations of MgSt and SSG on powder flowability. The results indicate that flow properties improved with decrease of SSG content and with increase of MgSt content. Magnesium stearate in powder formulations with microcrystalline cellulose has a greater influence on the improvement of the flow properties than powder formulations with spray-dried lactose.

scholarly journals Particle-Scale Modeling to Understand Liquid Distribution in Twin-Screw Wet Granulation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 928
Author(s):  
Ashish Kumar ◽  
Stefan Radl ◽  
Krist V. Gernaey ◽  
Thomas De Beer ◽  
Ingmar Nopens
Keyword(s):  
High Speed ◽  
Particle Surface ◽  
Multiphase System ◽  
Wet Granulation ◽  
Liquid Distribution ◽  
Granulation Process ◽  
Twin Screw ◽  
Dimensional Simulation ◽  
High Shear Wet Granulation ◽  
Solid Liquid

Experimental characterization of solid-liquid mixing for a high shear wet granulation process in a twin-screw granulator (TSG) is very challenging. This is due to the opacity of the multiphase system and high-speed processing. In this study, discrete element method (DEM) based simulations are performed for a short quasi-two-dimensional simulation domain, incorporating models for liquid bridge formation, rupture, and the effect of the bridges on inter-particular forces. Based on the knowledge gained from these simulations, the kneading section of a twin-screw wet granulation process was simulated. The time evolution of particle flow and liquid distribution between particles, leading to the formation of agglomerates, was analyzed. The study showed that agglomeration is a rather delayed process that takes place once the free liquid on the particle surface is well distributed.

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