Enhancement of Solubility and Dissoultion Rate of Domperidone Using Cogrinding and Kneading Technique

Tyagi, Reena; Dhillon, Vandana

doi:10.22270/jddt.v2i4.251

Cited by 4 publications

(2 citation statements)

References 10 publications

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“…This indicates a stable reaction product. The Gibbs free energy of the reaction (∆G) was also calculated using the following equation (Tyagi and Dhillon, 2012) :…”

Section: The Stability Constantmentioning

confidence: 99%

The development of analytical methods to determine metoclopramide-hydrochloric acid in the standard raw and it compared with pharmaceuticals

Abd-Alrassol

Qasim

AL-Rikabi

et al. 2019

ijrps

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The three novel easy, to the prepare and sensitive spectral methods, were used to estimate metoclopramide in both standard and pharmaceuticals. The effective double–electron, was present in the metoclopramide compound helps to interact in an acidic medium with a reagent such as diazetide resorcinol and 8-hydroxyquinoline reagents. The present article was extended to find out three analytical methods with UV-V is the detector. In both A and B methods, two azo-dyes are formed, they are orange-red and red stable and have high water solubility, giving highest absorption values at 415 nm and 485 nm but the C method will depend on a complex colour configuration with the p-benzoquinone reagent, which has a maximum absorption at a wavelength of 285 nm. Beer's law was applied in a range of concentrations between 1 and 10 μg / ml, 2-20 μg / ml and 1-30 μg / ml. The values of the molar absorption factors were (4.1224 × 104, 3.0229 × 104 and 1.7373 × 104) L mol-1cm-1 with a sensitivity of Sandell’s equal to 0.2606 × 10-4, 0.9834 × 10-4 and 0.2568 × 10 - 4 μg cm-2 to methods A, B respectively and LLOD values were 0.255, 0.553 and 0.158 μg / ml to methods A, B and C. LLOQ 0.512, 0.898 and 0.455 μg / ml to methods A, B, C respectively. The constant fixed Kf configuration was also calculated for the colored outputs of the reaction where it was found to be equal to 43.6435 × 108, 54.6261 × 10-8 and 17.29099 × 106 L2 mol-2 to all methods A, B, C respectively. The values of G were calculated based on -43.9293 KJ / mol, -44.3735 and -51.2019. G values, molar absorption factor, Sandell sensitivity, detection limit.

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“…This indicates a stable reaction product. The Gibbs free energy of the reaction (∆G) was also calculated using the following equation (Tyagi and Dhillon, 2012) :…”

Section: The Stability Constantmentioning

confidence: 99%

The development of analytical methods to determine metoclopramide-hydrochloric acid in the standard raw and it compared with pharmaceuticals

Abd-Alrassol

Qasim

AL-Rikabi

et al. 2019

ijrps

View full text Add to dashboard Cite

show abstract

“…Its low water solubility is the reason of the low bioavailability. [ 13 14 ] To increase the dissolution rate of this drug, some techniques have been used such as melt granulation technique,[ 15 ] orodispersible tablet,[ 16 ] solid lipid nanoparticles,[ 17 ] self-microemulsifying systems,[ 18 ] inclusion complex with cyclodextrins,[ 19 ] and solid dispersion[ 14 ] technique.…”

Section: Introductionmentioning

confidence: 99%

Solubility Enhancement of Domperidone by Solvent Change In situ Micronization Technique

Enteshari

Varshosaz

2018

Adv Biomed Res

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Background:Domperidone (DOM), a dopamine receptor antagonist, is used as antiemetic for the treatment of gastroparesis, vomiting, and nausea. The low water solubility of DOM leads to a low dissolution rate and variable bioavailability. The aim of this study was to enhance the solubility of DOM by the preparation of micron-sized particles.Materials and Methods:The in situ micronization process was carried out using solvent change method in the presence of Soluplus® or PEG6000 as stabilizing agents. DOM was dissolved in appropriate solvent (acetone and methanol 1:1 v/v), and the stabilizing agent was dissolved in water (as nonsolvent). The nonsolvent was poured rapidly into the drug solution under stirring by a homogenizer, and the resultant was freeze dried. The crystalline shape and particle size of DOM and interaction of DOM with stabilizers were investigated by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC), and then, dissolution test was carried out.Results:Optimum formulation was composed of DOM (0.5%) and PEG6000 (0.1%) with the lowest particle size (3 μm) and the highest DE60% (95.95%) as compared to pure DOM (particle size of 13.4 μm and DE60% 52.18%).Conclusion:SEM micrographs showed uniform and spherical shape of microcrystals. FTIR, XRD, and DSC studies indicated the micron size of the microcrystals and no interference between the drug and the stabilizer.

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Domperidone Solubility in Aqueous Cosolvent Mixtures of N,N-Dimethylformamide, Isopropanol, Dimethyl Sulfoxide, and Ethanol: Thermodynamic Modeling and Preferential Solvation Analysis

Zheng

Zhao

2019

J. Chem. Eng. Data

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The determination of solubility of domperidone in aqueous cosolvent mixtures of isopropanol, N,N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), and ethanol was carried out by a shake-flask method over the temperatures from 293.15 to 333.15 K under local atmospheric pressure p = 101.1 kPa. It may be observed that the domperidone solubility increased and then decreased as the mass fractions of DMF (DMSO, isopropanol, or ethanol) increased. The maximum solubility data was found with the cosolvent composition of 0.8 in mass fraction. The determined solubility values were correlated using the Jouyban–Acree, van’t Hoff–Jouyban–Acree, and Apelblat–Jouyban–Acree models. The attained average relative deviations were smaller than 7.56%. Preferential solvation analysis of domperidone was performed by the inverse Kirkwood–Buff integral method. The preferential solvation parameters (δx 1,3) by the cosolvent showed positive values in the composition regions of 0.20 < x 1 < 0.50 for DMF, 0.24 < x 1 < 0.55 for isopropanol, 0.20 < x 1 < 0.45 for DMSO, and 0.24 < x 1 < 0.61 for ethanol. Domperidone was solvated preferentially by the cosolvents in these regions. We may conjecture that the drug acts as a Lewis acid in the presence of isopropanol (DMF, DMSO, and ethanol) molecules.

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Enhancement of Solubility and Dissoultion Rate of Domperidone Using Cogrinding and Kneading Technique

Cited by 4 publications

References 10 publications

The development of analytical methods to determine metoclopramide-hydrochloric acid in the standard raw and it compared with pharmaceuticals

The development of analytical methods to determine metoclopramide-hydrochloric acid in the standard raw and it compared with pharmaceuticals

Solubility Enhancement of Domperidone by Solvent Change In situ Micronization Technique

Domperidone Solubility in Aqueous Cosolvent Mixtures of N,N-Dimethylformamide, Isopropanol, Dimethyl Sulfoxide, and Ethanol: Thermodynamic Modeling and Preferential Solvation Analysis

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