Lidocaine self-sacrificially improves the skin permeation of the acidic and poorly water-soluble drug etodolac via its transformation into an ionic liquid.
Abstract
Poor transdermal penetration of active pharmaceutical ingredients (APIs) impairs both bioavailability and therapeutic benefits and is a major challenge in the development of transdermal drug delivery systems. Here, we transformed a poorly water-soluble drug, etodolac, into an ionic liquid in order to improve its hydrophobicity, hydrophilicity and skin permeability. The ionic liquid was prepared by mixing etodolac with lidocaine (1:1, mol/mol). Both the free drug and the transformed ionic liquid were characterized by differential scanning colorimetry (DSC), infrared spectroscopy (IR), and saturatio...
Source: European Journal of Pharmaceutics and Biopharmaceutics - March 2, 2016 Category: Drugs & Pharmacology Authors: Miwa Y, Hamamoto H, Ishida T Tags: Eur J Pharm Biopharm Source Type: research
Stress impairs the efficacy of immune stimulation by CpG-C: Potential neuroendocrine mediating mechanisms and significance to tumor metastasis and the perioperative period.
Abstract
We recently reported that immune stimulation can be compromised if animals are simultaneously subjected to stressful conditions. To test the generalizability of these findings, and to elucidate neuroendocrine mediating mechanisms, we herein employed CpG-C, a novel TLR-9 immune-stimulating agent. Animals were subjected to ongoing stress (20-hrs of wet cage exposure) during CpG-C treatment, and antagonists to glucocorticoids, β-adrenoceptor, COX2, or opioids were employed (RU486, nadolol, etodolac, naltrexone). In F344 rats, marginating-pulmonary NK cell numbers and cytotoxicity were studied, and t...
Source: Brain, Behavior, and Immunity - March 1, 2016 Category: Neurology Authors: Levi B, Matzner P, Goldfarb Y, Sorski L, Shaashua L, Melamed R, Rosenne E, Page GG, Ben-Eliyahu S Tags: Brain Behav Immun Source Type: research
Selective COX-2 Inhibitors Significantly Reduce the Occurrence of Heterotopic Ossification After Hip Arthroscopic Surgery
Conclusion:
HO after hip arthroscopic surgery is a relatively common complication, with a rate of 19% for Brooker grade ≥2 in the patients who did not receive NSAID prophylaxis. No HO was found in the patients who received short-term COX-2 inhibitor prophylaxis. The short-term administration of 600 mg etodolac once daily for 2 weeks was found to be safe and effective in preventing HO in patients undergoing hip arthroscopic surgery. HO prophylaxis protocols based on short-term etodolac treatment may be considered after hip arthroscopic surgery. (Source: The American Journal of Sports Medicine)
Source: The American Journal of Sports Medicine - February 29, 2016 Category: Sports Medicine Authors: Rath, E., Warschawski, Y., Maman, E., Dolkart, O., Sharfman, Z. T., Salai, M., Amar, E. Tags: Hip/Pelvis/Thigh, Hip, femoroactabular impingement, Hip arthroscopy, NSAIDS Hip and Thigh Source Type: research
Improving the performance of an aerobic membrane bioreactor (MBR) treating pharmaceutical wastewater with powdered activated carbon (PAC) addition.
In this study, the effects of organic loading rate (OLR) and the addition of powdered activated carbon (PAC) on the performance and membrane fouling of MBR were conducted to treat real pharmaceutical process wastewater. Over 145 days of operation, the MBR system was operated at OLRs ranging from 1 to 2 kg COD m(-3) day(-1) without sludge wasting. The addition of PAC provided an improvement in the flux, despite an increase in the OLR:PAC ratio. The results demonstrated that the hybrid PAC-MBR system maintained a reduced amount of membrane fouling and steadily increased the removal performance of etodolac. PAC addition r...
Source: Bioprocess and Biosystems Engineering - February 5, 2016 Category: Biomedical Engineering Authors: Kaya Y, Bacaksiz AM, Golebatmaz U, Vergili I, Gönder ZB, Yilmaz G Tags: Bioprocess Biosyst Eng Source Type: research
Enantioselective analysis of etodolac in human plasma by LC–MS/MS: Application to clinical pharmacokinetics
Publication date: 20 February 2016 Source:Journal of Pharmaceutical and Biomedical Analysis, Volume 120 Author(s): Carolina de Miranda Silva, Adriana Rocha, Eduardo Tozatto, Lucienir Maria da Silva, Eduardo Antônio Donadi, Vera Lucia Lanchote Etodolac is a non-steroidal anti-inflammatory drug with preferential inhibition of cyclooxigenase-2 and is widely used in the management of pain in patients with inflammatory arthritis. Etodolac is available as a racemic mixture of (−)-(R)-Etodolac and (+)-(S)-Etodolac; cyclooxigenases inhibition is attributed to (+)-(S)-Etodolac. According to our knowledge, this is...
Source: Journal of Pharmaceutical and Biomedical Analysis - December 24, 2015 Category: Drugs & Pharmacology Source Type: research
Ultrasound-assisted chiral derivatization of etodolac with (1R)-(−)-menthyl chloroformate for the determination of etodolac enantiomers
This study presents the first report of an ultrasound-assisted derivatization reaction between a carboxylic acid of etodolac (ETO) and a chiral derivatization reagent, (1R)-(−)-menthyl chloroformate (R-MCF). FiftyμL of deproteinated mouse serum containing ETO enantiomers was derivatized with 125μL of 200mM R-MCF and 17μL of pyridine (a catalyst), with the reaction facilitated by ultrasonic radiation for 13min, which were the optimal conditions as determined by response surface methodology. After quenching the reaction by adding an aqueous L-proline solution, the mixture was subjected to salting-out assisted liquid–l...
Source: Arabian Journal of Chemistry - November 30, 2015 Category: Chemistry Source Type: research
Ultrasound-assisted chiral derivatization of etodolac with (1R)-(-)-menthyl chloroformate for the determination of etodolac enantiomers
This study presents the first report of an ultrasound-assisted derivatization reaction between a carboxylic acid of etodolac (ETO) and a chiral derivatization reagent, (1R)-(-)-menthyl chloroformate (R-MCF). Fifty μL of deproteinated mouse serum containing ETO enantiomers was derivatized with 125 μL of 200 mM R-MCF and 17 μL of pyridine (a catalyst), with the reaction facilitated by ultrasonic radiation for 13 min, which were the optimal conditions as determined by response surface methodology. After quenching the reaction by adding an aqueous L-proline solution, the mixture was subjected to salting-out assisted liquid-...
Source: Arabian Journal of Chemistry - November 13, 2015 Category: Chemistry Source Type: research
An ionic liquid-in-water microemulsion as a potential carrier for topical delivery of poorly water soluble drug: Development, ex-vivo and in-vivo evaluation
Publication date: 30 November 2015 Source:International Journal of Pharmaceutics, Volume 495, Issue 2 Author(s): Shishu Goindi, Ramanpreet Kaur, Randeep Kaur In this paper, we report an ionic liquid-in-water (IL/w) microemulsion (ME) formulation which is able to solubilize etodolac (ETO), a poorly water soluble drug for topical delivery using BMIMPF6 (1-butyl-3-methylimidazolium hexafluorophosphate) as IL, Tween 80 as surfactant and ethanol as co-surfactant. The prepared ME was characterized for physicochemical parameters, subjected to ex-vivo permeation studies as well as in-vivo pharmacodynamic evaluation. The ...
Source: International Journal of Pharmaceutics - October 21, 2015 Category: Drugs & Pharmacology Source Type: research
Network Meta-Analysis Comparing Relatively Selective COX-2 Inhibitors Versus Coxibs for the Prevention of NSAID-Induced Gastrointestinal Injury
This study included 36 trials with a total of 112,351 participants. Network meta-analyses indicated no significant difference between relatively selective COX-2 inhibitors and coxibs regarding ulcer complications (RR, 1.38; 95% CI, 0.47–3.27), symptomatic ulcer (RR, 1.02; 95% CI, 0.09–3.92), and endoscopic ulcer (RR, 1.18; 95% CI, 0.37–2.96). Network meta-analyses adjusting potential influential factors (age, sex, previous ulcer disease, and follow-up time), and sensitivity analyses did not reveal any major change to the main results. Network meta-analyses suggested that relatively selective COX-2 inhibitors and coxi...
Source: Medicine - October 1, 2015 Category: Internal Medicine Tags: Research Article: Systematic Review and Meta-Analysis (PRISMA Compliant) Source Type: research
Anodic oxidation of etodolac and its linear sweep, square wave and differential pulse voltammetric determination in pharmaceuticals
In this study, simple, fast and reliable cyclic voltammetry, linear sweep voltammetry, square wave voltammetry and differential pulse voltammetry methods were developed and validated for determination of etodolac in pharmaceutical preparations. The proposed methods were based on electrochemical oxidation of etodolac at platinum electrode in acetonitrile solution containing 0.1 M lithium perchlorate.
The well-defined oxidation peak was observed at 1.03 V. The calibration curves were linear for etodolac at the concentration range of 2.5-50 µg/ml for linear sweep, square wave and differential pulse voltammetry met...
Source: Indian Journal of Pharmaceutical Sciences - September 8, 2015 Category: Drugs & Pharmacology Authors: B YilmazS KabanBK Akcay Source Type: research
A window‐of‐opportunity biomarker study of etodolac in resectable breast cancer
Abstract
Observational data show that nonsteroidal anti‐inflammatory drug (NSAID) use is associated with a lower rate of breast cancer. We evaluated the effect of etodolac, an FDA‐approved NSAID reported to inhibit cyclooxygenase (COX) enzymes and the retinoid X receptor alpha (RXR), on rationally identified potential biomarkers in breast cancer. Patients with resectable breast cancer planned for initial management with surgical resection were enrolled and took 400 mg of etodolac twice daily prior to surgery. Protein and gene expression levels for genes related to COX‐2 and RXRα were evaluated in tumor samples from...
Source: Cancer Medicine - August 15, 2015 Category: Cancer & Oncology Authors: Richard B. Schwab, Shumei Kato, Brian Crain, Minya Pu, Karen Messer, Noel Weidner, Sarah L. Blair, Anne M. Wallace, Dennis A. Carson, Barbara A. Parker Tags: Original Research Source Type: research
Effect of etodolac hydrazone, a new compound synthesised from etodolac, on spermatozoon quality, testicular lipid peroxidation, apoptosis and spermatozoon DNA integrity
In conclusion, two different doses of EH, in particular its high dose, damage to testicular spermatogenic cells and spermatozoon DNA and, it decreases spermatozoon motility, count and testosterone level in healthy rats. (Source: Andrologia)
Source: Andrologia - May 1, 2015 Category: Urology & Nephrology Authors: S. Sarıözkan, G. Türk, P. Çıkla‐Süzgün, M. Güvenç, A. Yüce, A. H. Yay, F. Cantürk, Ş. G. Küçükgüzel Tags: Original Article Source Type: research
A method for rapid screening of interactions of pharmacologically active compounds with albumin.
Abstract
We determine the association constants for ligand-protein complex formation using the flow injection method. We carry out the measurements at high flow rates (F=1mLmin(-1)) of a carrier phase. Therefore, determination of the association constant takes only a few minutes. Injection of 1nM of the ligand (10μL of 1μM concentration of the ligand solution) is sufficient for a single measurement. This method is tested and verified for a number of complexes of selected drugs (cefaclor, etodolac, sulindac) with albumin (BSA). We obtain K=4.45×10(3)M(-1) for cefaclor, K=1.00×10(5)M(-1) for etodolac and...
Source: Analytica Chimica Acta - January 2, 2015 Category: Chemistry Authors: Majcher A, Lewandrowska A, Herold F, Stefanowicz J, Słowiński T, Mazurek AP, Wieczorek SA, Hołyst R Tags: Anal Chim Acta Source Type: research
Bitterness evaluation of acidic pharmaceutical substances (NSAIDs) using a taste sensor.
The objective of this study was to evaluate an improved bitterness sensor which has been developed to allow the precise and sensitive prediction of the bitterness of acidic bitter pharmaceutical active ingredients, using as examples nine non-steroidal anti-inflammatory drugs (NSAIDs). The bitterness of the nine NSAIDs was measured using a multichannel taste-sensing system incorporating a bitterness sensor, C00, which has a membrane surface with high hydrophobicity, and was developed to allow an enhanced hydrophobic interaction with acidic bitter substances. The sourness intensities of the nine NSAIDs were also determined i...
Source: Chemical and Pharmaceutical Bulletin - December 7, 2014 Category: Drugs & Pharmacology Authors: Yoshida M, Haraguchi T, Uchida T Tags: Chem Pharm Bull (Tokyo) Source Type: research
Comparison of the effect of Naproxen, Etodolac and Diclofenac on postoperative sequelsfollowing third molar surgery: a randomised, double-blind, crossover study.
CONCLUSION: NSAIDs (Diclofenac, Naproxen and Etodolac) are somehow similarly effective for controlling pain and trismus following extraction of mandibular third molars but Diclofenac potassium surpasses others in reduction of swelling.
PMID: 24316711 [PubMed - in process] (Source: Medicina Oral, Patologia Oral y Cirugia Bucal)
Source: Medicina Oral, Patologia Oral y Cirugia Bucal - December 2, 2014 Category: ENT & OMF Tags: Med Oral Patol Oral Cir Bucal Source Type: research
