In-vitro Kinetic Hydrolysis Study of Metronidazole Derivatives with Carvacrol and Eugenol Using Validated RP-HPLC Method

2020 ◽  
Vol 16 ◽  
Author(s):  
M. Alarjah
Keyword(s):  
Half Life ◽  
Hplc Method ◽  
Hydrolysis Rate ◽  
First Order ◽  
First Order Kinetics ◽  
Rp Hplc ◽  
Pharmacokinetic Properties ◽  
Pseudo First Order ◽  
Kinetic Hydrolysis

Background: Prodrugs principle is widely used to improve the pharmacological and pharmacokinetic properties of some active drugs. Much effort was made to develop metronidazole prodrugs to enhance antibacterial activity and or to improve pharmacokinetic properties of the molecule or to lower the adverse effects of metronidazole. Objective: In this work, the pharmacokinetic properties of some of monoterpenes and eugenol pro metronidazole molecules that were developed earlier were evaluated in-vitro. The kinetic hydrolysis rate constants and half-life time estimation of the new metronidazole derivatives were calculated using the validated RP-HPLC method. Method: Chromatographic analysis was done using Zorbbax Eclipse eXtra Dense Bonding (XDB)-C18 column of dimensions (250 mm, 4.6 mm, 5 μm), at ambient column temperature. The mobile phase was a mixture of sodium dihydrogen phosphate buffer of pH 4.5 and methanol in gradient elution, at 1ml/min flow rate. The method was fully validated according to the International Council for Harmonization (ICH) guidelines. The hydrolysis process carried out in an acidic buffer pH 1.2 and in an alkaline buffer pH 7.4 in a thermostatic bath at 37ºC. Results: The results followed pseudo-first-order kinetics. All metronidazole prodrugs were stable in the acidic pH, while they were hydrolysed in the alkaline buffer within a few hours (6-8 hr). The rate constant and half-life values were calculated, and their values were found to be 0.082- 0.117 hr-1 and 5.9- 8.5 hr., respectively. Conclusion: The developed method was accurate, sensitive, and selective for the prodrugs. For most of the prodrugs, the hydrolysis followed pseudo-first-order kinetics; the method might be utilised to conduct an in-vivo study for the metronidazole derivatives with monoterpenes and eugenol.

scholarly journals CATION EXCHANGE BETWEEN CELLS AND PLASMA OF MAMMALIAN BLOOD

1950 ◽  
Vol 33 (6) ◽  
pp. 703-722 ◽  
Author(s):  
C. W. Sheppard ◽  
W. R. Martin
Keyword(s):  
Exchange Rate ◽  
Radioactive Isotope ◽  
Specific Activity ◽  
Compartment System ◽  
First Order ◽  
First Order Kinetics ◽  
Mammalian Blood ◽  
The Mean ◽  
Pseudo First Order

The exchange of potassium between cells and plasma of heparinized human blood has been studied in vitro using the radioactive isotope K42. The changes in cell and plasma specific activity are characteristic of a simple two-compartment system. The mean of seven determinations of the exchange rate at 38°C. is 1.8 per cent of the cellular potassium per hour. The results indicate that at 38°C. the rate is relatively insensitive to oxygenation or reduction of the hemoglobin, and to 1200 r of gamma radiation. With varying temperature the rate follows pseudo first order kinetics with a Q10 of 2.35. Below 15°C. the rate of loss of potassium exceeds the rate of uptake.

The In Vitro Degradation Kinetics of Polyurethane Prodrug Materials

2011 ◽  
Vol 399-401 ◽  
pp. 1067-1070
Author(s):  
Chun Yan Li ◽  
Cong Cong Hu ◽  
Zhi Guo Wen ◽  
Sheng Xiong Dong
Keyword(s):  
Drug Release ◽  
High Performance ◽  
Degradation Kinetics ◽  
Hplc Method ◽  
In Vitro Degradation ◽  
Erosion Mechanism ◽  
First Order ◽  
First Order Kinetics ◽  
Kinetics Of

The method of high performance liquid chromatography (HPLC) is established to determine the content of antibacterial agent — ciprofloxacin (CF) in the degradation solution of ciprofloxacin-polyurethane (CFPU) and investigate the in vitro degradation kinetics by plotting and fitting the cumulative release curves to inspect the effects of different medium and different concentrations on drug release. The results showed that the HPLC method is accurate, reliable and simple. The drug-release of CFPU was bioresponsive and could be accorded with first order kinetics. It was observed that CF was released from CFPU by a combination of diffusion and erosion mechanism, mainly in the manner of diffusion in the absence of infection while erosion mechanism in the presence of infection.

Role of pH on Metribuzin Dissipation in Field Soils

Weed Science ◽  
1976 ◽  
Vol 24 (5) ◽  
pp. 508-511 ◽  
Author(s):  
James S. Ladlie ◽  
William F. Meggitt ◽  
Donald Penner
Keyword(s):  
Soil Ph ◽  
Half Life ◽  
Residue Analysis ◽  
Soil Samples ◽  
First Order ◽  
First Order Kinetics ◽  
Field Soils ◽  
Pseudo First Order

Metribuzin [4-amino-6-tert-butyl-3-(methylthio)-as-triazine-5(4H)one] residue analysis of soil samples showed greater amounts of residue extractable at soil pH 6.7 than 4.6. Metribuzin leaching increased with increasing soil pH. Metribuzin disappearance from soil followed pseudo first-order kinetics. The half-life of metribuzin decreased as soil pH increased and increased at all soil pH levels as depth of sampling increased. The decreased activity and decreased rate of metribuzin dissipation at lower soil pH is apparently due to protonation and increased adsorption.

scholarly journals Study of the Oxidative Forced Degradation of Glutathione in Its Nutraceutical Formulations Using Zone Fluidics and Green Liquid Chromatography

Separations ◽  
2020 ◽  
Vol 7 (1) ◽  
pp. 16
Author(s):  
Apostolia Tsiasioti ◽  
Constantinos K. Zacharis ◽  
Anastasia-Stella Zotou ◽  
Paraskevas D. Tzanavaras
Keyword(s):  
Reversed Phase ◽  
Hplc Method ◽  
Forced Degradation ◽  
Oxidized Glutathione ◽  
Reversed Phase Hplc ◽  
First Order ◽  
Direct Uv Detection ◽  
First Order Kinetics ◽  
Time Period ◽  
Pseudo First Order

In the present study, we report the results of our investigation of the oxidative forced degradation of glutathione in its nutraceutical formulations by two validated analytical methods. The first is based on the reaction of glutathione with o-phthalaldehyde through an automated zone fluidics flow platform and fluorimetric detection (λex/λem = 340/425 nm). The second is based on the separation of glutathione and its oxidation product by a green reversed-phase HPLC method coupled to direct UV detection, at 210 nm. A solution of 3% w/v H2O2 provided fast oxidation of more than 95% of glutathione to yield oxidized glutathione in a time period of 180 min. The mechanism of the oxidation was proved to follow pseudo-first order kinetics. The k, t90 and t1/2 values were calculated.

scholarly journals Active-site-directed irreversible inhibition of rat brain 4-aminobutyrate aminotransferase by ethanolamine O-sulphate in vitro and in vivo

1972 ◽  
Vol 130 (2) ◽  
pp. 569-573 ◽  
Author(s):  
L. J. Fowler ◽  
R. A. John
Keyword(s):  
Rat Brain ◽  
Dependent Manner ◽  
Aminobutyrate Aminotransferase ◽  
First Order ◽  
Irreversible Inhibition ◽  
First Order Kinetics ◽  
Intracisternal Injection ◽  
Pseudo First Order

1. Partially purified preparations of rat brain 4-aminobutyrate aminotransferase were inhibited in a time-dependent manner by ethanolamine O-sulphate. The inhibition was not reversed by dialysis. 2. The inhibitor formed an initial reversible complex with the enzyme (Ki=4.4×10−4m) and the rate of inactivation followed pseudo-first-order kinetics (k=7.15×10−4s−1). The inclusion of 4-aminobutyrate markedly slowed the rate of inactivation. 3. Ethanolamine O-sulphate did not inhibit glutamate decarboxylase, alanine aminotransferase or aspartate aminotransferase. 4. Intracisternal injection of ethanolamine O-sulphate into rats led to rapid inactivation of 4-aminobutyrate aminotransferase in vivo.

scholarly journals Kinetic Study on Removal of Sulphur Mustard on Granular Activated Carbon from Aqueous Solution

2016 ◽  
Vol 1 (2) ◽  
pp. 167 ◽  
Author(s):  
Anuradha Baghel ◽  
Beer Singh
Keyword(s):  
Aqueous Solution ◽  
Activated Carbon ◽  
Rate Constant ◽  
Half Life ◽  
Chemical Warfare Agent ◽  
Sulphur Mustard ◽  
Adsorptive Removal ◽  
First Order ◽  
First Order Kinetics ◽  
Pseudo First Order

Sulphur mustard is a powerful blister agent and has been worked as a chemical warfare agent. No specific antidote is available for its wound. Therefore, adsorptive removal is an effective way of removal. Here, adsorptive removal of sulphur mustard from aqueous solution was studied on activated carbon and screened out MeOH : H2O (1 : 1) solution as a good solvent than others used solvent. Adsorption isotherm of sulphur mustard was compared with its hydrolysis in the same solution. Kinetics of sulphur mustard removal on carbon from aqueous solution was found to be slower than hydrolysis and follow pseudo first order kinetics with the rate constant 5.04 X 10–3 min-1 and half life 137.5 min. The hydrolysis of sulphur mustard in MeOH : H2O (1 : 1) solution was found to be following the pseudo first order kinetics with the rate constant 8.68 x10-3 min-1 and half life 79.8 min.

scholarly journals Bleaching of chlorophylls by UV irradiation in vitro: The effects on chlorophyll organization in acetone and n-hexane

2008 ◽  
Vol 73 (3) ◽  
pp. 271-282 ◽  
Author(s):  
Jelena Zvezdanovic ◽  
Dejan Markovic
Keyword(s):  
Uv Irradiation ◽  
Photosynthetic Pigments ◽  
Energy Input ◽  
First Order ◽  
First Order Kinetics ◽  
Uv Photons ◽  
The Stability ◽  
Major Factors

The stability of chlorophylls toward UV irradiation was studied by Vis spectrophotometry in extracts containing mixtures of photosynthetic pigments in acetone and n-hexane. The chlorophylls underwent destruction (bleaching) obeying first-order kinetics. The bleaching was governed by three major factors: the energy input of the UV photons, the concentration of the chlorophylls and the polarity of the solvent, implying different molecular organizations of the chlorophylls in the two solvents.

New insights on the UV/TiO2 photocatalytic treatment of thiomersal and its 2-sulfobenzoic acid product

2021 ◽  
Vol 02 ◽  
Author(s):  
Emmanuel M. de la Fournière ◽  
Jorge M. Meichtry ◽  
Graciela S. Custo ◽  
Eduardo A. Gautier ◽  
Marta I. Litter
Keyword(s):  
Degradation Products ◽  
Acidic Ph ◽  
Cosmetic Products ◽  
Acid Product ◽  
First Order ◽  
First Order Kinetics ◽  
Photocatalytic Destruction ◽  
Pseudo First Order ◽  
Mineralization Degree ◽  
Suitable Technique

Background: Thiomersal (TM), a complex between 2-mercaptobenzoic acid (2-MBA) and ethylmercury (C2H5Hg+), is an antimicrobial preservative used in immunological, ophthalmic, cosmetic products, and vaccines. Objective: TM has been treated by UV/TiO2 photocatalysis in the presence or absence of oxygen at acidic pH. C2H5Hg+, 2-MBA, and 2-sulfobenzoic acid (2-SBA) were found as products. A 2-SBA photocatalytic treatment was undertaken to study sulfur evolution. Methods: Photocatalytic runs were performed using a UVA lamp (λmax = 352 nm), open to the air or under N2. A suspension of the corresponding TM or 2-SBA salt and TiO2 was prepared, and pH was adjusted. Suspensions were stirred in the dark for 30 min and then irradiated. TM, 2-MBA, 2-SBA, and C2H5Hg+ were quantified by HPLC, sulfur by TXRF, and the deposits on the photocatalyst were analyzed by chemical reactions. The mineralization degree was followed by TOC. Sulfate was determined using BaCl2 at 580 nm. Results: Photocatalytic destruction of TM and total C2H5Hg+ was complete under N2 and air, but TM degradation was much faster in air. The evolution of TM and the products followed a pseudo-first-order kinetics. Conclusion: TiO2-photocatalytic degradation is a suitable technique for the treatment of TM and its degradation products. In contrast to other organomercurial compounds, TM degradation is faster in the presence of O2, indicating that the oxidative mechanism is the preferred pathway. A significant TM mineralization (> 60%, NPOC and total S) was obtained. TM was more easily degraded than 2-SBA. Sulfate was the final product.

Chemical effects induced by gas–liquid jet flow

2022 ◽  
Author(s):  
Zhiliang Zhang ◽  
Jiaqi Lu ◽  
Bingqian Lv ◽  
Wei Liu ◽  
Shuyuan Shen ◽  
...  
Keyword(s):  
Methylene Blue ◽  
Jet Flow ◽  
Reaction Process ◽  
Liquid Jet ◽  
First Order ◽  
First Order Kinetics ◽  
Chemical Effects ◽  
Pseudo First Order

The gas-liquid jet flow was proved to be capable of inducing chemical consequences which can lead to the decomposition of methylene blue (MB). The reaction process follows a pseudo-first-order kinetics....

Use of purified lyophilized human lactate dehydrogenase isoenzyme 5 in a study of measuring lactate dehydrogenase activity.

1989 ◽  
Vol 35 (8) ◽  
pp. 1774-1776 ◽  
Author(s):  
D A Smith ◽  
G C Moses ◽  
A R Henderson
Keyword(s):  
Lactate Dehydrogenase ◽  
Half Life ◽  
Specific Activity ◽  
Lactate Dehydrogenase Activity ◽  
Bovine Albumin ◽  
First Order ◽  
First Order Kinetics ◽  
The Stability ◽  
Lactate Dehydrogenase Isoenzymes ◽  
Excellent Stability

Abstract We examined the stability of human lactate dehydrogenase (EC 1.1.1.27) isoenzyme 5--purified to a specific activity of about 400 kU/g--when lyophilized in a buffered, stabilized matrix of bovine albumin. This isoenzyme was prepared with a final activity of about 500 U/L and stored at -20, 4, 20, 37, and 56 degrees C for as long as six months. This isoenzyme decayed with approximate first-order kinetics, with an estimated half-life at -20 degrees C of about 475 years. Stability of reconstituted samples stored at 20 or 4 degrees C was poor, suggesting that the reconstituted material should be used without delay; material stored at -20 degrees C showed excellent stability for 15 days. We propose that such preparations might be further investigated as standards for use in electrophoresis of lactate dehydrogenase isoenzymes.

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