Investigation of Formulation and Process Parameters of Wet Media Milling to Develop Etodolac Nanosuspensions
ConclusionsIn conclusion, it is found that the poor solubility issue of ETD can be solved by nanosuspension. DoE approach provided benefits such as reducing number of experiments, saving time and improving final product quality by using wet media milling. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - May 30, 2020 Category: Drugs & Pharmacology Source Type: research
[Vascular Remodeling Induced by Biological Stresses].
Abstract
The thymus is a vital organ for functional immune systems, and is the site of T cell development, which plays a central role in cellular immune defenses. Unlike other major organs, the thymus is highly dynamic in size and structure. It shrinks immediately upon bacterial infection, aging, pregnancy, mental stress, nutritional deficiency, and more. The reduction in size and function of the thymus during such biological events is called thymic involution or thymic atrophy; thymic involution is a particularly important issue because dysfunctional T cell immunity increases the risks of tumorigenesis an...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - April 4, 2020 Category: Drugs & Pharmacology Authors: Hasegawa H Tags: Yakugaku Zasshi Source Type: research
Induced Prostanoid Synthesis Regulates the Balance between Th1- and Th2-Producing Inflammatory Cytokines in the Thymus of Diet-Restricted Mice.
Abstract
Multiple external and internal factors have been reported to induce thymic involution. Involution involves dramatic reduction in size and function of the thymus, leading to various immunodeficiency-related disorders. Therefore, clarifying and manipulating molecular mechanisms governing thymic involution are clinically important, although only a few studies have dealt with this issue. In the present study, we investigated the molecular mechanisms underlying thymic involution using a murine acute diet-restriction model. Gene expression analyses indicated that the expression of T helper 1 (Th1)-produ...
Source: Biological and Pharmaceutical Bulletin - April 4, 2020 Category: Drugs & Pharmacology Authors: Razali N, Hohjoh H, Inazumi T, Maharjan BD, Nakagawa K, Konishi M, Sugimoto Y, Hasegawa H Tags: Biol Pharm Bull Source Type: research
Drugs for Osteoarthritis
Date: April 20, 2020
Issue #:
1596Summary:
Many different drugs are used for treatment of
osteoarthritis pain, but none of them prevent
progression of the disease. Nonpharmacologic
approaches including weight management, exercise,
tai chi, physical therapy, assistive devices, and total
joint arthroplasty can also be used. The American
College of Rheumatology (ACR) has published new
guidelines for the management of osteoarthritis of the
hip, hand, and knee. (Source: The Medical Letter)
Source: The Medical Letter - April 1, 2020 Category: Drugs & Pharmacology Authors: admin Tags: Acetaminophen Advil Aleve Anaprox Aspercreme Aspirin capsaicin Celebrex Celecoxib chondroitin ConZip corticosteroids Cymbalta Cytotec depo-medrol Diclofenac Duloxetine Durela etodolac Fenoprofen Flector Flurbiprof Source Type: research
Mechanistic insights of the controlled release capacity of polar functional group in transdermal drug delivery system: the relationship of hydrogen bonding strength and controlled release capacity
This study concluded that drugs with strong hydrogen bond forming ability and high skin permeation were suitable to use amide pressure sensitive adhesives to regulate their release rate from patch. The conclusion was further confirmed by in vivo pharmacokinetic study. (Source: Acta Pharmaceutica Sinica B)
Source: Acta Pharmaceutica Sinica B - November 30, 2019 Category: Cancer & Oncology Source Type: research
Systemic drugs with impact on osteoarthritis.
Authors: Apostu D, Lucaciu O, Mester A, Oltean-Dan D, Baciut M, Baciut G, Bran S, Onisor F, Piciu A, Pasca RD, Maxim A, Benea H
Abstract
Articular cartilage has a complex structure and metabolism which allow for a proper movement within joints. Nevertheless, several systemically administered pharmacological agents have been proved to improve the anabolic response in the case of cartilage lesions. Alendronate, glucosamine, chondroitin sulfate, hyaluronic acid, collagen hydrolysate, vitamin C, vitamin D, aspirin and strontium ranelate have shown positive results in clinical trials. On the other hand, calcito...
Source: Drug Metabolism Reviews - November 19, 2019 Category: Drugs & Pharmacology Tags: Drug Metab Rev Source Type: research
Molecules, Vol. 24, Pages 3880: Fingerprinting, Antimicrobial, Antioxidant, Anticancer, Cyclooxygenase and Metabolic Enzymes Inhibitory Characteristic Evaluations of Stachys viticina Boiss. Essential Oil
rik
The present study aimed to identify the chemical constituents and to assess the in-vitro, antimicrobial, anticancer, antioxidant, metabolic enzymes and cyclooxygenase (COX) inhibitory properties of essential oil (EO) of Stachys viticina Boiss. leaves. The S. viticina EO was isolated and identified using microwave-ultrasonic and GC-MS techniques, respectively. Fifty-two compounds were identified, of which endo-borneol was the major component, followed by eucalyptol and epizonarene. The EO was evaluated against a panel of in-vitro bioassays. The EO displayed antimicrobial activity against methicillin-resistant Staphy...
Source: Molecules - October 27, 2019 Category: Chemistry Authors: Nidal Jaradat Nawaf Al-Maharik Tags: Article Source Type: research
Synthesis and biological evaluation of new prodrugs of etodolac and tolfenamic acid with reduced ulcerogenic potential.
In this study, the new prodrugs were prepared through Steglich esterification reaction between the carboxylic acid functional group of etodolac or tolfenamic acid and thymol. The structures were confirmed by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analysis. Their chemical stability in addition to a kinetic study of their hydrolysis in 20% liver homogenate and 10% buffered plasma were investigated. In vitro enzymatic hydrolysis showed half-life times 88.84 and 106.61 min for the prodrugs of etodolac and tolfenamic acid, respectively. Their ability to inhibit paw edema and their ulcerogenic potential were assess...
Source: European Journal of Pharmaceutical Sciences - October 18, 2019 Category: Drugs & Pharmacology Authors: Hassib ST, Hassan GS, El-Zaher AA, Fouad MA, El-Ghafar OAA, Taha EA Tags: Eur J Pharm Sci Source Type: research
Microwave assisted amberlite-IRA-402 (OH) ion exchange resin catalyzed synthesis of new benzoxazole scaffolds derived from antiinflammatory drugs aceclofenac and mefenamic acid as potential therapeutic agents for inflammation
Publication date: Available online 20 September 2019Source: Journal of Molecular StructureAuthor(s): Gangadhara Angajala, Radhakrishnan Subashini, Valmiki ArunaAbstractAn efficient microwave assisted synthesis of 2-substituted benzoxazole derivatives from antiinflammatory drugs aceclofenac and mefenamic acid using amberlite-IRA-402 (OH) ion exchange resin as a base catalyst were reported. The synthesized compounds were purified and characterized by 1H NMR, 13C NMR and Mass spectroscopy. In silico molecular docking studies were carried out to predict the binding affinity of the synthesized benzoxazole derivatives with COX-2...
Source: Journal of Molecular Structure - September 21, 2019 Category: Molecular Biology Source Type: research
Switchable-hydrophilicity solvent liquid–liquid microextraction of non-steroidal anti-inflammatory drugs from biological fluids prior to HPLC-DAD determination
Publication date: 10 September 2019Source: Journal of Pharmaceutical and Biomedical Analysis, Volume 174Author(s): Malek Hassan, Usama AlshanaAbstractSwitchable-hydrophilicity solvent liquid–liquid microextraction was used prior to high-performance liquid chromatography with diode-array detector (HPLC-DAD) for the determination of four non-steroidal anti-inflammatory drugs [i.e., ketoprofen, etodolac, flurbiprofen and ibuprofen] in human urine, saliva and milk. Optimum extraction conditions were as follows: 500 μL switched-on N,N-dimethylcyclohexylamine as the extraction solvent, 9.5 mL of the aqueous phase, 500 Î...
Source: Journal of Pharmaceutical and Biomedical Analysis - June 24, 2019 Category: Drugs & Pharmacology Source Type: research
Switchable-hydrophilicity solvent liquid-liquid microextraction of non-steroidal anti-inflammatory drugs from biological fluids prior to HPLC-DAD determination
Publication date: Available online 20 June 2019Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Malek Hassan, Usama AlshanaAbstractSwitchable-hydrophilicity solvent liquid-liquid microextraction was used prior to high-performance liquid chromatography with diode-array detector (HPLC-DAD) for the determination of four non-steroidal anti-inflammatory drugs [i.e., ketoprofen, etodolac, flurbiprofen and ibuprofen] in human urine, saliva and milk. Optimum extraction conditions were as follows: 500 µL switched-on N,N-dimethylcyclohexylamine as the extraction solvent, 9.5 mL of the aqueous phase, 500 Â...
Source: Journal of Pharmaceutical and Biomedical Analysis - June 20, 2019 Category: Drugs & Pharmacology Source Type: research
Spectral, DFT and molecular docking investigations on Etodolac
Publication date: 5 November 2019Source: Journal of Molecular Structure, Volume 1195Author(s): B. Amul, S. Muthu, M. Raja, S. SevvanthiAbstractThe title compound (RS) -2- (1, 8-Diethyl- 4, 9-dihydro-3H- pyrano [3, 4-b] indol-1-yl) acetic acid (Etodolac) was characterized by experimental FTIR, FT-Raman, NMR and UV-Visible spectral analysis. The optimized molecular geometry and vibrational wave numbers were calculated by employing the method of DFT and B3LYP/6-311++G(d, p) basis set. The vibrational assignments were calculated using VEDA program. Carbon and Proton NMR chemical shifts were calculated in different solvents by ...
Source: Journal of Molecular Structure - June 19, 2019 Category: Molecular Biology Source Type: research
Design by optimization and comparative evaluation of vesicular gels of etodolac for transdermal delivery.
Authors: Madhavi N, Sudhakar B, Reddy KVNS, Ratna JV
Abstract
Aim of the present study was to design vesicular gels of etodolac loaded liposomes and ethosomes for effective transdermal delivery. The physicochemical properties of vesicular gels were compared with 45% v/v ethanolic etodolac solution and commercial product (PROXYM®). The liposomes were prepared by film hydration technique whereas ethosomes were prepared by cold method respectively. Both the systems were characterized for various physicochemical properties. The size range of liposomes shows 186 nm-363 nm whereas for ethosomes 170 nm-261...
Source: Drug Development and Industrial Pharmacy - February 5, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research
Multi-faceted therapeutic strategy for treatment of Alzheimer's disease by concurrent administration of etodolac and α-tocopherol.
In conclusion, this study highlights the significance of combination therapy to simultaneously target multiple disease pathways, and suggest the repurposing and combination of etodolac and α-tocopherol as a novel therapeutic strategy against AD.
PMID: 30710675 [PubMed - as supplied by publisher] (Source: Neurobiology of Disease)
Source: Neurobiology of Disease - January 30, 2019 Category: Neurology Authors: Elfakhri KH, Abdallah IM, Brannen AD, Kaddoumi A Tags: Neurobiol Dis Source Type: research
(S)-1-(1-Methylpyridin-2-yl)-3-aminopiperidine as a novel derivatization reagent capable of enantiomeric separation and enhanced ESI-MS/MS detection for chiral carboxylic acids
Publication date: May 2019Source: Microchemical Journal, Volume 146Author(s): Takaaki Matsumoto, Maho Sato, Wataru Yamazaki, Shoujiro Ogawa, Tatsuya HigashiAbstractA novel derivatization reagent, (S)-1-(1-methylpyridin-2-yl)-3-aminopiperidine (MPAPp), was designed and developed for the enantiomeric separation by conventional reversed-phase liquid chromatography (LC) and the sensitive electrospray ionization-tandem mass spectrometry (ESI-MS/MS) detection of chiral carboxylic acids. MPAPp reacted with the carboxylic acids at 60 °C within 5 min in the presence of a condensation agent to produce the positively-charged and...
Source: Microchemical Journal - December 29, 2018 Category: Chemistry Source Type: research
