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Journal of Molecular Recognition : JMR Aug 2020To get an idea about the pharmacokinetics and pharmacodynamics, it is important to study the drug-protein interaction. Therefore, herein, we studied the interaction of...
To get an idea about the pharmacokinetics and pharmacodynamics, it is important to study the drug-protein interaction. Therefore, herein, we studied the interaction of diclofenac sodium (DIC) with human hemoglobin. The binding study of nonsteroidal antiinflammatory drug, DIC with human hemoglobin (HHB) was done by utilizing fluorescence, UV-visible, time-resolved fluorescence and far-UV circular dichroism spectroscopy (CD). Various thermodynamic parameters such as enthalpy change (ΔH), entropy change (ΔS), and Gibbs free energy change (ΔG) were also calculated. CD results showed that DIC induces secondary structure change in HHB. Fluorescence resonance energy transfer was also performed. Additionally, it was also observed that DIC inhibits the esterase-like enzymatic activity of HHB via competitive inhibition.
Topics: Circular Dichroism; Diclofenac; Esterases; Fluorescence Resonance Energy Transfer; Hemoglobins; Humans; Molecular Docking Simulation; Protein Binding; Protein Structure, Secondary; Thermodynamics
PubMed: 32150309
DOI: 10.1002/jmr.2841 -
Knee Surgery, Sports Traumatology,... Feb 2014The present study was designed to evaluate the penetration of diclofenac sodium 4 % spray gel in synovial tissue, synovial fluid and blood plasma after topical... (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
The present study was designed to evaluate the penetration of diclofenac sodium 4 % spray gel in synovial tissue, synovial fluid and blood plasma after topical application in subjects with joint effusions and planned total knee arthroplasty (TKA) due to osteoarthritis.
METHODS
A total of 39 patients were randomised to two- or three-times daily application of diclofenac sodium 4 % spray gel to knees requiring surgery over a treatment period of 3 days. Within 8 h after the last application, TKA was conducted, and the diclofenac concentrations in synovial tissue, synovial fluid and blood plasma were measured by liquid chromatography.
RESULTS
The median diclofenac concentration was approximately 10-20-fold higher in synovial tissue (36.2 and 42.8 ng/g) than in synovial fluid (2.6 and 2.8 ng/mL) or plasma (3.9 and 4.1 ng/mL) in both treatment groups. Dose proportionality for any compartment or treatment groups could not be detected. Treatment-related adverse events were noted in two cases and limited to skin reactions.
CONCLUSION
Diclofenac sodium 4 % spray gel was found to penetrate the skin locally in substantial amounts and thus reach the desired target tissue. Concentrations were not dose-dependent, and application was well tolerated by 97.4 % of patients. Topical application of diclofenac should be considered a valuable alternative to systemic NSAID therapy in the initial treatment of osteoarthritis.
Topics: Administration, Cutaneous; Adult; Aged; Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Chromatography, Liquid; Diclofenac; Female; Gels; Humans; Knee Joint; Male; Middle Aged; Osteoarthritis, Knee; Synovial Fluid; Synovial Membrane
PubMed: 23338668
DOI: 10.1007/s00167-013-2408-0 -
Journal of Pharmaceutical and... Jul 2002Diclofenac sodium is one of the potent Non Steroidal Anti-Inflammatory Drugs (NSAID) used in the treatment of inflammatory conditions. The present work deals with the...
Diclofenac sodium is one of the potent Non Steroidal Anti-Inflammatory Drugs (NSAID) used in the treatment of inflammatory conditions. The present work deals with the estimation of diclofenac sodium from serum by a novel High Performance Thin Layer Chromatographic (HPTLC) method developed in our laboratory. Standard diclofenac sodium was spotted on Silica Gel 60 F(254) precoated plates, which were developed using the mobile phase toluene:acetone:glacial acetic acid (80:30:1,v/v/v). Densitometric analysis of diclofenac sodium was carried out at 280 nm with diclofenac being detected at an R(f) of 0.58. The method was subsequently developed to estimate diclofenac sodium from serum. Diclofenac sodium was extracted with ethyl acetate from serum samples, spotted on Silica Gel 60 F(254) plates and the plates were developed using the above mentioned mobile phase. The method was validated for selectivity, extraction efficiency, sensitivity, accuracy, and intra and inter-day reproducibility studies. The extraction efficiency was found to range from 76 to 80%. The Limit of Detection (LOD) and Limit of Quantification (LOQ) of diclofenac sodium in serum were found to be 90 and 120 ng, respectively. The calibration curve of diclofenac sodium in serum was found to be linear in the range of 200-800 ng. The mean values (+/-S.D.) of correlation coefficient, slope and intercept were found to be 0.9876 (+/-0.0105), 0.0228 (+/-0.0036) and 6.15 (+/-1.4), respectively. The mean percentage coefficient of variation for accuracy, intra-day and inter-day analysis at 200-800 ng of diclofenac sodium were found to be 3.2, 6.35 and 8.025, respectively. The proposed method is a simple and sensitive method with good precision and reproducibility for the estimation of diclofenac sodium form serum samples.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Chromatography, Thin Layer; Diclofenac; Sensitivity and Specificity
PubMed: 12062654
DOI: 10.1016/s0731-7085(02)00131-0 -
British Journal of Community Nursing Nov 2006Osteoarthritis (OA) is a common complaint that affects millions of people worldwide. As there is no cure for OA, drug treatment is the main form of management. This can... (Review)
Review
Osteoarthritis (OA) is a common complaint that affects millions of people worldwide. As there is no cure for OA, drug treatment is the main form of management. This can be achieved through the use of analgesics and anti-inflammatory drugs such as the NSAID diclofenac sodium. The chronic use of diclofenac sodium can lead to adverse gastrointestinal problems. The use of a topical formulation of diclofenac sodium aims to reduce this problem. Evidence from four randomized controlled trails of the efficacy and safety of topical diclofenac sodium as a method of pain relief for the treatment of OA of the knee is presented and discussed. Findings imply that topical diclofenac sodium is an efficacious and safe method of pain control in patients with OA of the knee.
Topics: Administration, Cutaneous; Administration, Oral; Anti-Inflammatory Agents, Non-Steroidal; Chemistry, Pharmaceutical; Diclofenac; Evidence-Based Medicine; Humans; Osteoarthritis, Knee; Pain; Pain Measurement; Randomized Controlled Trials as Topic; Research Design; Safety; Treatment Outcome
PubMed: 17170650
DOI: 10.12968/bjcn.2006.11.11.22278 -
International Journal of Pharmaceutical... 2024Diclofenac Sodium is a nonsteroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory, and antipyretic properties, and has been found to be effective...
Diclofenac Sodium is a nonsteroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory, and antipyretic properties, and has been found to be effective in treating a variety of acute and chronic pain and inflammatory conditions. A stability study was designed to assess the physical, chemical, and antimicrobial stability of three extemporaneously compounded bracketed Diclofenac Sodium formulations over time using a validated, stability indicating HPLC method. Diclofenac Sodium 1% and 15% were compounded in Medisca VersaPro™ Cream Base, VersaPro™ Gel Base and PLO Gel Mediflo™30 Compound Kit and stored at room temperature, in tightly closed, light resistant, plastic containers for 180 days. The organoleptic properties, pH, viscosity, and Diclofenac Sodium concentration of each formulation were evaluated at predetermined time points. Antimicrobial effectiveness testing of the compounded formulation according to USP <51> was also evaluated at the initial time point and after 180 days. The results demonstrated that all formulations remained within the specified stability criteria for the duration of the study. Therefore, an extended beyond-use-date of 180 days may be assigned to these compounded formulations under the studied conditions.
Topics: Diclofenac; Drug Stability; Anti-Inflammatory Agents, Non-Steroidal; Analgesics; Anti-Infective Agents; Drug Compounding
PubMed: 38604143
DOI: No ID Found -
Ophthalmology Apr 1996Anti-inflammatory medications are traditionally administered to the eye only postoperatively for control of inflammation. Because the presumed mechanism of action of... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
PURPOSE
Anti-inflammatory medications are traditionally administered to the eye only postoperatively for control of inflammation. Because the presumed mechanism of action of nonsteroidal anti-inflammatory drugs (NSAIDs) is to inhibit the formation of prostaglandin mediators of inflammation, the author studied the effect that pretreatment with an NSAID had on postoperative inflammation.
METHODS
In a prospective study, 60 patients scheduled for phacoemulsification with silicone lens implantation were randomly assigned to receive either (1) pretreatment with one drop of diclofenac sodium 0.1% four times per day for the 3 days before surgery plus one drop of diclofenac sodium 0.1% every 15 minutes for four doses, beginning 1 hour before surgery along with the dilating drops; (2) no pretreatment, but one drop of diclofenac sodium 0.1% every 15 minutes for four doses beginning 1 hour before surgery along with the dilating drops; or (3) no diclofenac sodium drops at all before surgery. No anti-inflammatory medications were given either during or immediately after surgery, and all patients were begun on a regimen of one drop of diclofenac sodium 0.1% to the operated eye four times per day after being examined on the first postoperative day. Postoperative inflammation was measured on the first postoperative day and at 1 week with a laser cell and flare meter.
RESULTS
On the first postoperative day, the mean flare score for group A was 25.59 photons/millisecond; for group B, 29.69 photons/millisecond; and for group C, 33.07 photons/millisecond. The difference between groups A and C was statistically significant. The differences between groups A and B and between groups B and C were not statistically significant. There was no statistically significant difference for cell scores at 1 day or for cell or flare scores at 1 week.
CONCLUSIONS
The pretreatment with an NSAID before cataract surgery can reduce the amount of initial postoperative inflammation.
Topics: Administration, Topical; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac; Endophthalmitis; Humans; Lenses, Intraocular; Phacoemulsification; Postoperative Complications; Premedication; Prospective Studies; Single-Blind Method
PubMed: 8618764
DOI: 10.1016/s0161-6420(96)30641-6 -
Journal of Pharmaceutical Sciences May 2001A known impurity is formed in the production of a parenteral dosage form of diclofenac sodium if terminally sterilized by autoclave. This impurity has been detected as...
A known impurity is formed in the production of a parenteral dosage form of diclofenac sodium if terminally sterilized by autoclave. This impurity has been detected as 1-(2,6-dichlorophenyl) indolin-2qone, which is also an intermediate from which diclofenac sodium is generally synthesized. It is only the condition of the autoclave method (i.e., 123 +/- 2 degrees C) that enforces the intramolecular cyclic reaction of diclofenac sodium forming the indolinone derivative and sodium hydroxide. The formation of this impurity has been found to depend on the initial pH of the formulation. The reaction follows first-order kinetics, and the energy of activation is 5.34 kcal/mol. The other excipients in the formulation do not have a role in this reaction. The concentration of the impurity in the resultant product in the ampule goes beyond the limit of the raw materials in the pharmacopoeias. It is thus preferable to use an alternative sterilization method; that is, an aseptic filtration method in which the formation of this impurity can be avoided.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Chromatography, High Pressure Liquid; Diclofenac; Filtration; Hydrogen-Ion Concentration; Sterilization
PubMed: 11288099
DOI: 10.1002/1520-6017(200105)90:5<541::aid-jps1011>3.0.co;2-o -
Acta Neurologica Scandinavica May 1986
Topics: Adult; Diclofenac; Epilepsy; Humans; Male
PubMed: 3727929
DOI: 10.1111/j.1600-0404.1986.tb04595.x -
Ultrasonics Sonochemistry May 2014Diclofenac sodium, a widely detected pharmaceutical drug in wastewater samples, has been selected as a model pollutant for degradation using novel combined approach of...
Diclofenac sodium, a widely detected pharmaceutical drug in wastewater samples, has been selected as a model pollutant for degradation using novel combined approach of hydrodynamic cavitation and heterogeneous photocatalysis. A slit venturi has been used as cavitating device in the hydrodynamic cavitation reactor. The effect of various operating parameters such as inlet fluid pressure (2-4 bar) and initial pH of the solution (4-7.5) on the extent of degradation have been studied. The maximum extent of degradation of diclofenac sodium was obtained at inlet fluid pressure of 3 bar and initial pH as 4 using hydrodynamic cavitation alone. The loadings of TiO2 and H2O2 have been optimised to maximise the extent of degradation of diclofenac sodium. Kinetic study revealed that the degradation of diclofenac sodium fitted first order kinetics over the selected range of operating protocols. It has been observed that combination of hydrodynamic cavitation with UV, UV/TiO2 and UV/TiO2/H2O2 results in enhanced extents of degradation as compared to the individual schemes. The maximum extent of degradation as 95% with 76% reduction in TOC has been observed using hydrodynamic cavitation in conjunction with UV/TiO2/H2O2 under the optimised operating conditions. The diclofenac sodium degradation byproducts have been identified using LC/MS analysis.
Topics: Catalysis; Diclofenac; Hydrodynamics; Hydrogen Peroxide; Hydrogen-Ion Concentration; Kinetics; Photochemical Processes; Pressure; Sonication; Titanium
PubMed: 24262760
DOI: 10.1016/j.ultsonch.2013.10.020 -
Cellular and Molecular Biology... Jan 2019Diclofenac sodium (DS) was the third generation non-steroidal drugs with analgesic and antipyretic properties. Owing to taking action faster, long lasting potency, good...
Diclofenac sodium (DS) was the third generation non-steroidal drugs with analgesic and antipyretic properties. Owing to taking action faster, long lasting potency, good efficacy and low side effects, DS was widely used in the pharmaceutical industry. To further ensure animal food safety and consumer health, the rational usages regulations of DS and DS withdrawal time should be provided. In the present study, a new high performance liquid chromatography tandem mass spectrometry (HPLC/MS) method was first established for extracting and validating diclofenac sodium levels in edible porcine tissues. Meanwhile, the pharmacokinetics characteristics and residue elimination of intramuscular DS administration in pigs were also studied. We found DS eliminated quickly and the distribution was poor in vivo. After a single dose of 2.5 mg/kg body weight per day for continuous 3 days, the withdrawal time in the tissues of liver, kidney, sebum, muscle and administration site were 9.892 days, 5.116 days, 14.205 days, 5.444 days and 8.818 days, respectively. According to the double-sided 95% confidence interval, DS withdrawal period should be 15 days. These experiment evidences lay a good foundation on the rational usages regulations of DS and DS withdrawal time, which will be helpful for the animal food safety and consumer health.
Topics: Animals; Chromatography, High Pressure Liquid; Diclofenac; Injections, Intramuscular; Mass Spectrometry; Reference Standards; Swine
PubMed: 30782291
DOI: No ID Found