scholarly journals Preparation and Hydro-Lipophilic Properties of Methoxylated and Methylated 1-Hydroxynaphthalene-2-Carboxanilides

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 43 ◽  
Author(s):  
Iva Kapustikova ◽  
Tomas Gonec ◽  
Jiri Kos ◽  
Ewelina Spaczynska ◽  
Michal Oravec ◽  
...  
Keyword(s):  
Mobile Phase ◽  
High Performance ◽  
Chemical Structure ◽  
Reversed Phase ◽  
Log P ◽  
Organic Modifier ◽  
Chromatography Method ◽  
P Values ◽  
Liquid Chromatography Method ◽  
Substituted 1

A series of variously methoxylated and methylated N-aryl-1-hydroxynaphthalene-2-carboxanilides was prepared and characterized as potential anti-invasive agents. As it is known that lipophilicity significantly influences the biological activity of compounds, the hydro-lipophilic properties of these mono-, di- and tri-substituted 1-hydroxynaphthalene-2-carboxanilides are investigated in the study. All the discussed hydroxynaphthalene derivatives were analyzed using the reversed-phase, high-performance liquid chromatography method, to measure lipophilicity. The procedure was performed under isocratic conditions with methanol as an organic modifier in the mobile phase, using an end-capped, non-polar C18 stationary reversed-phase column. The present study discusses the correlations between the logarithm of the capacity factor k and log P/Clog P values, calculated in various ways, as well as the relationships between the lipophilicity and the chemical structure of the studied compounds.

scholarly journals Preparation and Hydro-Lipophilic Properties of Selected Novel Chlorinated and Brominated N-Arylcinnamamides

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 11
Author(s):  
Tomas Strharsky ◽  
Timotej Jankech ◽  
Jiri Kos ◽  
Kristina Maricakova ◽  
Andrea Pramukova ◽  
...  
Keyword(s):  
High Performance ◽  
Chemical Structure ◽  
Antimicrobial Agents ◽  
Reversed Phase ◽  
Log P ◽  
Organic Modifier ◽  
Chromatography Method ◽  
P Values ◽  
Liquid Chromatography Method ◽  
Derivatives Of

A series of six di- and tri-halogenated N-arylcinnamanilides designed as anti-inflammatory and antimicrobial agents was prepared and characterized. Since it is known that lipophilicity significantly influences the biological activity of compounds, the hydro-lipophilic properties of these di- and tri-substituted N-arylcinnamanilides were investigated in the study. All the discussed derivatives of cinnamic acid were analyzed using the reversed-phase high performance liquid chromatography method to measure lipophilicity. The procedure was performed under isocratic conditions with methanol as an organic modifier in the mobile phase using an end-capped non-polar C18 stationary reversed-phase column. In the present study, the correlations between the logarithm of the capacity factor k and log P/Clog P values calculated in various ways as well as the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed.

DEVELOPMENT AND VALIDATION OF THE REVERSED-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR THE ESTIMATION OF GUAIFENESIN IN METHOCARBAMOL API AND ITS PHARMACEUTICAL DOSAGE FORMS

2018 ◽  
Vol 11 (5) ◽  
pp. 401
Author(s):  
Mannem Durga Babu ◽  
Kesana Surendrababu
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Mobile Phase ◽  
High Performance ◽  
Reversed Phase ◽  
Dosage Forms ◽  
Solution Stability ◽  
Chromatography Method ◽  
Pharmaceutical Dosage Forms ◽  
Liquid Chromatography Method

Objective: The objective of the study was to develop and validate a novel, specific, precise, and simple reversed-phase high-performance liquid chromatography method for the estimation of guaifenesin present in methocarbamol API and its pharmaceutical dosage forms. Methods: The baseline separation for methocarbamol and guaifenesin was achieved by utilizing a Inertsil ODS C18 (250 mm × 4.6 mm) 5 μm column particle size and an isocratic elution method. The mobile phase contains a mixture of water and acetonitrile in the ratio of 70:30 v/v, respectively. The flow rate of the mobile phase was 1.0 mL/min with a column temperature of 25°C and detection wavelength at 272 nm. The method was validated for a limit of detection (LOD), limit of quantification (LOQ), linearity, accuracy, and reproducibility with the help of the exhibit and simulated samples. Results: The LOD for guaifenesin was 0.62 μg/mL. The LOQ for guaifenesin was 1.87 μg/mL. The correlation coefficient obtained for impurity was >0.99. The recovery was obtained for impurity was 106.56% at 50%, 95.20% at 100%, and 100.45% at 150%. In tablet analysis, we can found 0.26% (<0.5%). Conclusion: The developed method was validated as per the ICH guidelines with respect to specificity, precision, linearity, accuracy, LOD and quantification, ruggedness, robustness, and solution stability.

scholarly journals Determination of lipophilicity for antitumor acridinone derivatives supported by gradient high-performance liquid chromatography method

2012 ◽  
Vol 10 (1) ◽  
pp. 216-223 ◽  
Author(s):  
Marcin Koba ◽  
Mariusz Belka ◽  
Tomasz Ciesielski ◽  
Tomasz Bączek
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
High Performance ◽  
Retention Factor ◽  
Reversed Phase ◽  
Log P ◽  
Chromatography Method ◽  
Factor Log ◽  
Liquid Chromatography Method

AbstractThe lipophilicity values of selected acridinone (imidazoacridinone and triazoloacridinone) derivatives were measured by gradient reversed-phase high-performance liquid chromatography (RP-HPLC) using a C18 stationary phase with a water/acetonitrile mixture as a mobile phase. The retention times obtained served as input data and appropriate log kw values (i.e., the retention factor log kw extrapolated to 0% organic modifier) as an alternative to log P were calculated using the DryLab program. The relationships between the lipophilicity (log kw) and the chemical structure of the studied compounds, as well as correlation between experimentally determined lipophilicities (log kw) and log P data calculated using some commonly available software, are discussed.

scholarly journals Method Development and Validation for Simultaneous Estimation of Ketorolac and Sparfloxacin by RP-HPLC

2013 ◽  
Vol 1 (04) ◽  
pp. 95-101 ◽  
Author(s):  
Rahul Singh ◽  
Ashish Pathak ◽  
Pooja Chawla
Keyword(s):  
Mobile Phase ◽  
High Performance ◽  
Method Development ◽  
Sample Volume ◽  
Reversed Phase ◽  
Simultaneous Estimation ◽  
Chromatography Method ◽  
Mobile Phase Flow Rate ◽  
Pharmaceutical Dosage Forms ◽  
Liquid Chromatography Method

A modified simple, selective, rapid, precise reversed phase high performance liquid chromatography method has been developed and validated for the simultaneous estimation of ketorolac and sparfloxacin. The separation was made in a Hypersil-Keystone C-18 column using a methanol: water (60:40, v/v) (pH 3.1) as mobile phase at 308 nm. The mobile-phase flow rate and the sample volume injected were 0.9 ml/min and 20 μl, respectively. Retention time of sparfloxacin and ketorolac was found to be 3.181 and 4.473 minutes respectively. The correlation coefficient of both drugs was found to be 0.999. The accuracy of ketorolac was found to be 99.82% - 100.55% whereas for sparfloxacin, it was 99.76% - 99.89%. Over all % RSD was found to be less than 2%. The method was validated according to ICH guidelines with respect to linearity, accuracy, precision, robustness, specificity, etc. The developed method can be used for routine analysis of ketorolac and sparfloxacin in their pharmaceutical dosage forms.

scholarly journals Gradient HPLC in the determination of drug lipophilicity and acidity

2001 ◽  
Vol 73 (9) ◽  
pp. 1465-1475 ◽  
Author(s):  
Roman Kaliszan ◽  
Piotr Haber ◽  
Tomasz Baczek ◽  
Danuta Siluk
Keyword(s):  
Mobile Phase ◽  
High Performance ◽  
Standard Procedure ◽  
Gradient Elution ◽  
Log P ◽  
Retention Data ◽  
Organic Modifier ◽  
Wide Range ◽  
Aqueous Component ◽  
Initial Ph

The linear-solvent strength (LSS) model of gradient elution in high-performance liquid chromatography (HPLC) has been demonstrated to provide parameters of lipophilicity and acidity of analytes. pKa and log kw values are determined in three gradient runs. The first two experiments use an aqueous buffered eluent with a wide-range organic modifier gradient at pH of buffer, providing suppression of ionization of the analyte. That experiment allows an estimate of contents of the organic modifier in the mobile phase (%B), producing requested retention coefficient, k, for the nonionized form of the analyte. The next experiment is carried out with the latter %B and a pH-gradient of the aqueous component of the eluent that is sufficient to overlap possible pKa value of the analyte. The initial pH of the buffer used to make the mobile phase is selected to insure that the analyte is in nonionized form. The resulting retention time allows an estimate of pKa in a solvent of the given %B.The log kw parameter obtained correlated well with the corresponding value obtained by the standard procedure of extrapolation of retention data determined in a series of isocratic measurements. The correlation between log kw and the reference parameter of lipophilicity, log P, was very good for a series of test analytes. The values of pKa were found to correlate with the literature pKa data determined in water for a set of aniline derivatives studied.

Reversed-phase high performance liquid chromatography method for the determination of paraquat in whole blood

2014 ◽  
Vol 6 (16) ◽  
pp. 6560-6564 ◽  
Author(s):  
Wuxiang Zhang ◽  
Yicong Su ◽  
Jiangu Shi ◽  
Maosheng Zhang ◽  
Bide Wu ◽  
...  
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Whole Blood ◽  
High Performance ◽  
Reversed Phase ◽  
Chromatography Method ◽  
Liquid Chromatography Method

In this paper, a high performance liquid chromatography technique is established for quantification of paraquat in blood.

VALIDATED RP-HPLC METHOD FOR DETERMINATION OF ENZALUTAMIDE IN BULK DRUG AND PHARMACEUTICAL DOSAGE FORM

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (11) ◽  
pp. 46-50
Author(s):  
Z. G Khan ◽  
◽  
S. S. Patil ◽  
P. K. Deshmukh ◽  
P. O. Patil
Keyword(s):  
Retention Time ◽  
Mobile Phase ◽  
High Performance ◽  
Reversed Phase ◽  
Hplc Method ◽  
Uv Detector ◽  
Chromatography Method ◽  
Pharmaceutical Dosage Form ◽  
Bulk Drug

Novel, isocratic reversed phase high performance liquid chromatography method was developed and validated for the determination of enzalutamide (EZA) in bulk drug and pharmaceutical formulation. Efficient separation was achieved on PrincetonSPHER C18 100A, 5μ (250×4.6 mm) under the isocratic mode of elution using acetonitrile: water (80:20) % V/V as a mobile phase pumped in to the column at flow rate 1.0 mL/min. The effluent was monitored at 237.0 nm using UV detector. EZA was eluted in the given mobile phase at retention time (tR) of 3.2 minutes. The standard calibration curve was linear over the concentration range 10 - 60 μg/mL with correlation coefficient 0.997. The method was validated for accuracy, precision, sensitivity, robustness, ruggedness and all the resulting data treated statistically. The system suitability parameters like retention time, theoretical plates, tailing factor, capacity factor were found within the limit.

BIO ANALYTICAL METHOD DEVELOPMENT AND VALIDATION FOR SIMULANEOUS ESTIMATION OF NITAZOXANIDE AND OFLOXACIN IN HUMAN PLASMA BY RP-HPLC

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (10) ◽  
pp. 47-57
Keyword(s):  
Human Plasma ◽  
High Performance ◽  
Method Development ◽  
Reversed Phase ◽  
Chromatography Method ◽  
Rp Hplc ◽  
Method Development And Validation ◽  
Liquid Chromatography Method ◽  
Development And Validation ◽  
Lower Limits

An isocratic Reversed-Phase High Performance Liquid Chromatography method has been developed for rapid and simultaneous separation and estimation of two antibiotics, namely, nitazoxanide and ofloxacin, in human plasma. Separation was carried out on Altima C8 (150 x 4.6 mm, 5µ) column using a mobile phase of 0.1% ortho phosphoric acid: acetonitrile (50:50, V/V) at 260 nm. The retention time of nitazoxanide and ofloxacin was noted to be 4.850 and 7.949 min, respectively. The average % recovery for nitazoxanide and ofloxacin were 98.012 % and 94.176 %, respectively and reproducibility was found to be satisfactory. The linearity was investigated in the concentration range of 0.02-2 µg/ml (r2=0.9996) for nitazoxanide and 0.008-0.8 µg/ml (r2=0.9998) for ofloxacin. The lower limits of quantification were 0.0196 µg/ml and 0.0079 µg/ml for nitazoxanide and ofloxacin, respectively, which reach the level of both drugs possibly found in human plasma. The proposed method can be applied for etermination of nitazoxanide and ofloxacin from dosage forms during pharmacokinetic study.

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