Synthesis of diastereomeric anhydrides of (RS)-ketorolac and (RS)-etodolac, semi-preparative HPLC enantioseparation, establishment of molecular asymmetry and recovery of pure enantiomers
New J. Chem., 2017, Advance Article DOI: 10.1039/C7NJ02898A, PaperPoonam Malik, Ravi Bhushan Herein, enantioseparation of two anti-inflammatory drugs, namely, (RS)-ketorolac and (RS)-etodolac, commonly marketed and administered as racemates, was achieved by RP-HPLC. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - New J. Chem. latest articles)
Source: RSC - New J. Chem. latest articles - October 23, 2017 Category: Chemistry Authors: Poonam Malik Source Type: research
Synthesis of diastereomeric anhydrides of (RS)-ketorolac and (RS)-etodolac, semipreparative HPLC enantioseparation, establishment of molecular asymmetry and recovery of pure enantiomers
New J. Chem., 2017, Accepted Manuscript DOI: 10.1039/C7NJ02898A, PaperPoonam Malik, Ravi Bhushan Enantioseparation of two anti-inflammatory drugs, namely, (RS)-ketorolac and (RS)- etodolac, marketed and administered commonly as racemates has been achieved by RPHPLC. The method provided very low limits of detection values... The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - New J. Chem. latest articles)
Source: RSC - New J. Chem. latest articles - October 6, 2017 Category: Chemistry Authors: Poonam Malik Source Type: research
Preparation, Characterization and In Vitro / In Vivo Evaluation of Oral Time-Controlled Release Etodolac Pellets.
The objective of this study was to prepare time-controlled release etodolac pellets to facilitate drug administration according to the body's biological rhythm, optimize the drug's desired effects, and minimize adverse effects. The preparation consisted of three laminal layers from center to outside: the core, the swelling layer, and the insoluble polymer membrane. Factors influenced the core and the coating films were investigated in this study. The core pellets formulated with etodolac, lactose, and sodium carboxymethyl starch (CMS-Na) were prepared by extrusion-spheronization and then coated by a fluidized bed coater. C...
Source: AAPS PharmSciTech - September 15, 2017 Category: Drugs & Pharmacology Authors: Zhang X, Li Q, Ye M, Zhao Z, Sun J, Yang X, Pan W Tags: AAPS PharmSciTech Source Type: research
Development of an Enantioselective and Biomarker-Informed Translational Population Pharmacokinetic/Pharmacodynamic Model for Etodolac
This study aimed to characterize the relationship between NSAID concentrations,in vitro COX-2 inhibition, and acute pain decrease in humans over time by a translational approach using clinical pharmacokinetic and literature reportedin vitro and clinical pharmacodynamic data. In a two-way cross-over study, eight healthy volunteers received 300 and 400 mg racemic etodolac, a preferential COX-2 inhibitor.R- andS-etodolac were determined by LC-MS/MS and simultaneously modeled. Literaturein vitro IC50 data for COX-2 inhibition byS-etodolac were used to fit adjusted pain score profiles from dental patients receiving etodolac. ...
Source: The AAPS Journal - September 5, 2017 Category: Drugs & Pharmacology Source Type: research
Acute Liver Failure Due to Etodolac, a Selective Cycloxygenase- 2 (COX -2) Inhibitor Non-Steroidal Anti-Inflammatory Drug Established by RUCAM-Based Causality Assessment.
Authors: Taneja S, Kumar P, Rathi S, Duseja A, Singh V, Dhiman RK, Chawla YK
Abstract
Drug induced liver injury is a common cause of acute liver failure (ALF). While most of these cases are due to dose dependent hepatotoxicity with acetaminophen, idiosyncratic drug-induced liver injury (DILI) is responsible for about 15% cases of ALF. Antibiotics are the most common cause of idiosyncratic DILI as well as DILI induced ALF. Etodolac is a selective cycloxygenase- 2 (COX -2) inhibitor non-steroidal anti-inflammatory drug used as an analgesic and anti-inflammatory in musculoskeletal diseases. Severe liver impai...
Source: Annals of Hepatology - August 18, 2017 Category: Gastroenterology Tags: Ann Hepatol Source Type: research
Chiral separation and modeling of baclofen, bupropion, and etodolac profens on amylose reversed phase chiral column.
Abstract
Chiral resolution of baclofen, bupropion, and etodolac profens was obtained with amylose derivatized chiral reversed stationary phase (carbamate groups). The eluent used for bupropion and etodolac was MeOH-water (20:80, v/v) and for baclofen was water-methanol (95:5, v/v). The eluent run rates, finding wavelength and temperature, were 1.0 mL/min, 220 nm and 27 ± 1 °C for all the eluents. The magnitude of the retardation factors for S- and R-enantiomers of baclofen, bupropion, and etodolac were 1.37, 2.62, 2.25, 3.25, 1.8, and 3.0. The magnitudes of separation and resolution factors were 1.9...
Source: Chirality - June 15, 2017 Category: Molecular Biology Authors: Ali I, Suhail M, Alothman ZA, Alwarthan A Tags: Chirality Source Type: research
Etodolac transdermal cubosomes for the treatment of rheumatoid arthritis: ex vivo permeation and in vivo pharmacokinetic studies.
In this study, transdermal etodolac-loaded cubosomes were developed in order to relieve patient pain and joints stiffness by providing stable etodolac concentration at the targeting sites through controlled drug delivery via the noninvasive skin route with more sustaining and less frequent dosing. Different ratios and percentages of poloxamer 407 and monoolein were used to formulate the cubosomes using emulsification and homogenization processes. The etodolac-loaded cubosomes showed particle size values ranging from 135.95 to 288.35 nm and zeta potential values ranging from -18.40 to -36.10 mV. All the cubosomes offere...
Source: Drug Delivery - May 27, 2017 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research
Perioperative COX-2 and & beta;-adrenergic blockade improves metastatic biomarkers in breast cancer patients in a phase-II randomized trial.
Conclusions:<br /> <p>Perioperative inhibition of COX-2 and b-adrenergic signaling provides a safe and effective strategy for inhibiting multiple cellular and molecular pathways related to metastasis and disease recurrence in early-stage breast cancer. .
PMID: 28490464 [PubMed - as supplied by publisher] (Source: Clinical Cancer Research)
Source: Clinical Cancer Research - May 10, 2017 Category: Cancer & Oncology Authors: Shaashua L, Shabat-Simon M, Haldar R, Matzner P, Zmora O, Shabtai M, Sharon E, Allweis T, Barshack I, Hayman L, Arevalo JMG, Ma J, Horowitz M, Cole SW, Ben-Eliyahu S Tags: Clin Cancer Res Source Type: research
Treatment of chemical synthesis-based pharmaceutical wastewater in an ozonation-anaerobic membrane bioreactor (AnMBR) system
In this study, treatability of etodolac chemical synthesis wastewater from the pharmaceutical industry was investigated in a hybrid ozonation-Anaerobic Membrane Bioreactor (AnMBR) system. The AnMBR was successfully operated up to 7500mg/L of chemical oxygen demand (COD), but sulfite inhibition occurred at this loading. A pre-ozonation process was applied to overcome the problem of sulfite inhibition resulted from raw wastewater by decreasing the sulfite concentration through oxidation to sulphate. Furthermore, it was shown that this process was also effective obtaining high etodolac removal efficiencies up to 99%. Approxim...
Source: Chemical Engineering Journal - April 14, 2017 Category: Chemistry Source Type: research
Fast dissolving drug-drug eutectics with improved compressibility and synergistic effects.
Abstract
Combinational therapy has become increasingly popular in recent times due to various advantages like greater therapeutic effect, reduced number of prescriptions, lower administrative costs, and an increase in patient compliance. Drug-drug multicomponent adducts could help in combination of drugs at supramolecular level. Two drug-drug eutectics of etodolac with paracetamol (EP) and etodolac with propranolol hydrochloride (EPHC) were successfully designed and synthesized for the first time. These eutectics significantly improved dissolution and material properties. A 6 to 9 fold enhancement in % dis...
Source: European Journal of Pharmaceutical Sciences - March 30, 2017 Category: Drugs & Pharmacology Authors: Thipparaboina R, Thumuri D, Chavan R, Naidu VG, Shastri NR Tags: Eur J Pharm Sci Source Type: research
Coxibs Refocus Attention on the Cardiovascular Risks of Non-Aspirin NSAIDs
This article explains how coxibs refocused attention on the cardiovascular safety of NSAIDs and the general implications of that. COX-2 activity/specificity is one factor associated with increased cardiovascular risks; however, these risks cannot be attributed to coxibs alone. The traditional NSAIDs (i.e., meloxicam, etodolac, and nabumetone) have significant COX-2 specificity, but naproxen and ibuprofen have less specificity. All NSAIDs, whether traditional or a coxib, pose some cardiovascular risks. It is possible that clinicians continue to focus more on decreasing the immediate gastric risks than preventing the later c...
Source: American Journal of Cardiovascular Drugs - March 28, 2017 Category: Cardiology Source Type: research
Quantification of Etodolac in Human Plasma for Pharmacokinetics and Bioequivalence Studies in 27 Korean Subjects
Conclusion: Thus, the new testified method was successfully applied for the pharmacokinetic and bioequivalence studies for two etodolac formulations. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Inclusion Complexation of Etodolac with Hydroxypropyl-beta-cyclodextrin
and Auxiliary Agents: Formulation Characterization and Molecular Modeling
Studies
Molecular PharmaceuticsDOI: 10.1021/acs.molpharmaceut.6b01115 (Source: Molecular Pharmaceutics)
Source: Molecular Pharmaceutics - March 1, 2017 Category: Drugs & Pharmacology Authors: Atul P. Sherje, Vaidehi Kulkarni, Manikanta Murahari, Usha Y. Nayak, Pritesh Bhat, Vasanti Suvarna and Bhushan Dravyakar Source Type: research
Taste-Masking Effect of Chlorogenic Acid (CGA) on Bitter Drugs Evaluated by Taste Sensor and Surface Plasmon Resonance on the Basis of CGA-Drug Interactions.
Abstract
The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste sensor outputs were significantly inhibited by the addition of CGA to all drugs. The inhibition ratio of the taste sensor output decreased in the following order DPH>DNP>AMD≈DCF≈RB...
Source: Chemical and Pharmaceutical Bulletin - February 7, 2017 Category: Drugs & Pharmacology Authors: Shiraishi S, Haraguchi T, Nakamura S, Li D, Kojima H, Yoshida M, Uchida T Tags: Chem Pharm Bull (Tokyo) Source Type: research
The Role of Epithelial to Mesenchymal Transition in Human Amniotic Membrane Rupture.
CONCLUSION: This work demonstrated that amniotic cell EMT was associated with labor, and that EMT decreased the tensile strength of the amnion. These findings suggest a role for EMT in the pathophysiology of PPROM and may provide a basis for development of therapies to prevent preterm labor.
PMID: 27992249 [PubMed - as supplied by publisher] (Source: The Journal of Clinical Endocrinology and Metabolism)
Source: The Journal of Clinical Endocrinology and Metabolism - December 18, 2016 Category: Endocrinology Authors: Janzen C, Sen S, Lei MY, Gagliardi de Assumpcao M, Challis J, Chaudhuri G Tags: J Clin Endocrinol Metab Source Type: research
