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  1. Loh JW, Taib NA, Cheong YT, Tin TS
    World J Surg, 2020 08;44(8):2656-2666.
    PMID: 32193622 DOI: 10.1007/s00268-020-05458-6
    BACKGROUND: Pre-incision wound infiltration using NSAID is an alternative method to manage post-operative pain in surgery. It is postulated that NSAID delivered peripherally exerts efficient analgesic and anti-inflammatory effect with minimal systemic complication. This study explored the efficacy of using diclofenac for wound infiltration in open thyroidectomy and parathyroidectomy as compared to conventional agent, bupivacaine.

    METHODOLOGY: The study was designed as a double-blind, randomized controlled trial involving 94 patients who underwent open thyroidectomy or parathyroidectomy in Hospital Pulau Pinang, Malaysia, from November 2015 to November 2016. The study compared the efficacy of pre-incision wound infiltration of diclofenac (n = 47) versus bupivacaine (n = 47) in post-operative pain relief. Wound infiltration is given prior to skin incision. Mean pain score at designated time interval within the 24-h post-operative period, time to first analgesia, total analgesic usage and total analgesic cost were assessed.

    RESULTS: Ninety-four patients were recruited with no dropouts. Mean age was 49.3 (SD = 14.2) with majority being female (74.5%). Ethnic distribution recorded 42.6% Chinese, 38.3% Malay, followed by 19.1% Indian. Mean duration of surgery was 123.8 min (SD = 56.5), and mean length of hospital stay was 4.7 days (SD = 1.8). The characteristics of patient in both groups were generally comparable except that there were more cases of total thyroidectomy in the diclofenac group (n = 31) as compared to the bupivacaine group (n = 16). Mean pain score peaked at immediate post-operative period (post-operative 0.5 h) with a score of 3.5 out of 10 and the level decreased steadily over the next 20 h starting from 4 h post-operatively. Pre-incision wound infiltration using diclofenac had better pain control as compared to bupivacaine at all time interval assessed. In the resting state, the mean post-operative pain score difference was statistically significant at 2 h [2.1 (SD = 1.5) vs. 2.8 (SD = 1.8), p = 0.04]. During neck movement, the dynamic pain score difference was statistically significant at post-operative 1 h [2.7 (SD = 1.9) vs. 3.7 (SD = 2.1), p = 0.02]; 2 h [2.7 (SD = 1.6) vs. 3.7 (SD = 2.0), p = 0.01]; 4 h [2.2 (SD = 1.5) vs. 2.9 (SD = 1.7), p = 0.04], 6 h [1.9 (SD = 1.4) vs. 2.5 (SD = 1.6), p = 0.04] and 12 h [1.5 (SD = 1.5) vs. 2.2 (SD = 1.4), p = 0.03]. Mean dose of tramadol used as rescue analgesia in 24 h duration was lower in the diclofenac group as compared to bupivacaine group [13.8 mg (SD = 24.9) vs. 36.2 mg (SD = 45.1), p = 0.01]. The total cost of analgesia used was significantly cheaper in diclofenac group as compared to bupivacaine group [RM 3.47 (SD = 1.51) vs. RM 13.43 (SD = 1.68), p diclofenac provides better post-operative pain relief compared to bupivacaine for patient who had underwent open thyroidectomy or parathyroidectomy. Diclofenac is cheap and easily available in the limited resource setting. This approach offers a superior alternative for post-operative pain relief as compared to bupivacaine.

    Matched MeSH terms: Diclofenac/administration & dosage*; Diclofenac/economics
  2. Marzida, M.
    JUMMEC, 2009;12(2):63-69.
    MyJurnal
    It is important to provide effective postoperative analgesia following a Caesarean section because mothers wish to be pain-free, mobile and alert while caring for their babies. The role of regular oral diclofenac as postoperative analgesia was evaluated in a randomized controlled study and it was compared to the established method of parenteral pethidine. Forty healthy women scheduled for elective Caesarean section under spinal anaesthesia with 2-2.5 mg of heavy bupivacaine 0.5% were randomized to receive either 75 mg of oral diclofenac twice daily or 1 mg/kg of subcutaneous pethidine every 8 hourly. Efficacy of pain relief (visual analogue score), patients' satisfaction and side effects such as sedation, nausea and vomiting were recorded for three days. The demographic variables were similar in both groups. Pain relief was adequate and comparable in both groups with similar mean visual analogue score during the second and third day of the study period. However, on the first postoperative day, 60% of the diclofenac group population required rescuemedication consisting of subcutaneous pethidine in order to achieve the same pain scores as those in the pethidine group who did not require any rescue medications. Women who received oral diclofenac reported lower sedation and higher overall satisfaction. The incidence of nausea and vomiting was similar in both groups. This concluded that although oral diclofenac 75mg twice daily may not be superior to the traditional method of subcutaneous pethidine for pain relief following caesarean section, it can still be used alone as an alternative, as it has other benefits of a non-opioid analgesia.
    Matched MeSH terms: Diclofenac
  3. Kamaruzaman S, Hauser PC, Sanagi MM, Ibrahim WA, Endud S, See HH
    Anal Chim Acta, 2013 Jun 14;783:24-30.
    PMID: 23726096 DOI: 10.1016/j.aca.2013.04.042
    A simple adsorption/desorption procedure using a mixed matrix membrane (MMM) as extraction medium is demonstrated as a new miniaturized sample pretreatment and preconcentration technique. Reversed-phase particles namely polymeric bonded octadecyl (C18) was incorporated through dispersion in a cellulose triacetate (CTA) polymer matrix to form a C18-MMM. Non-steroidal anti-inflammatory drugs (NSAIDs) namely diclofenac, mefenamic acid and ibuprofen present in the environmental water samples were selected as targeted model analytes. The extraction setup is simple by dipping a small piece of C18-MMM (7 mm × 7 mm) in a stirred 10 mL sample solution for analyte adsorption process. The entrapped analyte within the membrane was then desorbed into 100 μL of methanol by ultrasonication prior to high performance liquid chromatography (HPLC) analysis. Each membrane was discarded after single use to avoid any analyte carry-over effect. Several important parameters, such as effect of sample pH, salting-out effect, sample volume, extraction time, desorption solvent and desorption time were comprehensively optimized. The C18-MMM demonstrated high affinity for NSAIDs spiked in tap and river water with relative recoveries ranging from 92 to 100% and good reproducibility with relative standard deviations between 1.1 and 5.5% (n=9). The overall results obtained were found comparable against conventional solid phase extraction (SPE) using cartridge packed with identical C18 adsorbent.
    Matched MeSH terms: Diclofenac
  4. Rahim H, Sadiq A, Khan S, Khan MA, Shah SMH, Hussain Z, et al.
    Drug Des Devel Ther, 2017;11:2443-2452.
    PMID: 28860715 DOI: 10.2147/DDDT.S140626
    This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precipitation-ultrasonication approach. The nanocrystals were produced using the optimum conditions investigated for AC. The minimum particle size (PS) and polydispersity index was found to be 112±2.01 nm and 0.165, respectively, using hydroxypropyl methylcellulose (1%, w/w), polyvinylpyrrolidone K30 (1%, w/w) and sodium lauryl sulfate (0.12%, w/w). The characterization of AC was performed using zeta sizer, scanning electron microscopy, transmission electron microscopy, powder X-ray diffraction and differential scanning calorimetry. The saturation solubility of the AC nanocrystals was substantially increased 2.6- and 4.5-fold compared to its unprocessed active pharmaceutical ingredient in stabilizer solution and unprocessed drug. Similarly, the dissolution rate of the AC nanocrystals was substantially enhanced compared to its other counterpart. The results showed that >88% of AC nanocrystals were dissolved in first 10 min compared to unprocessed AC (8.38%), microsuspension (66.65%) and its marketed tablets (17.65%). The in vivo studies of the produced stabilized nanosuspension demonstrated that the Cmax were 4.98- and 2.80-fold while area under curve from time of administration to 24 h (AUC0→24 h) were found 3.88- and 2.10-fold greater when compared with unprocessed drug and its marketed formulation, respectively. The improved antinociceptive activity of AC nanocrystals was shown at much lower doses as compared to unprocessed drug, which is purely because of nanonization which may be attributed to improved solubility and dissolution rate of AC, ultimately resulting in its faster rate of absorption.
    Matched MeSH terms: Diclofenac/administration & dosage; Diclofenac/analogs & derivatives*; Diclofenac/pharmacology; Diclofenac/chemistry
  5. Dua K, Pabreja K, Ramana MV
    Acta Pharm, 2010 Dec;60(4):467-78.
    PMID: 21169138 DOI: 10.2478/v1007-010-0036-5
    Aceclofenac is a new generation non-steroidal anti-inflammatory drug showing effective anti-inflammatory and analgesic properties. It is available in the form of tablets of 100 mg. Importance of aceclofenac as a NSAID has inspired development of topical dosage forms. This mode of administration may help avoid typical side effects associated with oral administration of NSAIDs, which have led to its withdrawal. Furthermore, aceclofenac topical dosage forms can be used as a supplement to oral therapy for better treatment of conditions such as arthritis. Ointments, creams, and gels containing 1% (m/m) aceclofenac have been prepared. They were tested for physical appearance, pH, spreadability, extrudability, drug content uniformity, in vitro diffusion and in vitro permeation. Gels prepared using Carbopol 940 (AF2, AF3) and macrogol bases (AF7) were selected after the analysis of the results. They were evaluated for acute skin irritancy, anti-inflammatory and analgesic effects using the carrageenan-induced thermal hyperalgesia and paw edema method. AF2 was shown to be significantly (p < 0.05) more effective in inhibiting hyperalgesia associated with inflammation, compared to AF3 and AF7. Hence, AF2 may be suggested as an alternative to oral preparations.
    Matched MeSH terms: Diclofenac/administration & dosage; Diclofenac/analogs & derivatives*; Diclofenac/toxicity; Diclofenac/chemistry
  6. Mahmod M, Nor IF, Maskon O
    BMJ Case Rep, 2010;2010.
    PMID: 22448190 DOI: 10.1136/bcr.02.2009.1549
    While selective non-steroidal anti-inflammatory drugs, namely cyclo-oxygenase-2 (COX 2) inhibitors, are known to be associated with acute myocardial infarction, little is known about the cardiovascular safety of the non-selective non-steroidal anti-inflammatory drugs. We report the case of a 44-year-old man who developed anaphylactic reaction and acute inferior myocardial infarction following ingestion of a non-selective anti-inflammatory drug, diclofenac sodium. Coronary angiography revealed a large thrombus in the right coronary artery which was partially removed by intracoronary catheter aspiration. Complete resolution of the remaining thrombus was achieved after treatment with an oral anticoagulant.
    Matched MeSH terms: Diclofenac
  7. Hiew BYZ, Lee LY, Lai KC, Gan S, Thangalazhy-Gopakumar S, Pan GT, et al.
    Environ Res, 2019 01;168:241-253.
    PMID: 30321737 DOI: 10.1016/j.envres.2018.09.030
    Pharmaceutical residues are emerging pollutants in the aquatic environment and their removal by conventional wastewater treatment methods has proven to be ineffective. This research aimed to develop a three-dimensional reduced graphene oxide aerogel (rGOA) for the removal of diclofenac in aqueous solution. The preparation of rGOA involved facile self-assembly of graphene oxide under a reductive environment of L-ascorbic acid. Characterisation of rGOA was performed by Fourier transform infrared, scanning electron microscope, transmission electron microscopy, nitrogen adsorption-desorption, Raman spectroscopy and X-ray diffraction. The developed rGOA had a measured density of 20.39 ± 5.28 mg/cm3, specific surface area of 132.19 m2/g, cumulative pore volume of 0.5388 cm3/g and point of zero charge of 6.3. A study on the simultaneous interactions of independent factors by response surface methodology suggested dosage and initial concentration as the dominant parameters influencing the adsorption of diclofenac. The highest diclofenac adsorption capacity (596.71 mg/g) was achieved at the optimum conditions of 0.25 g/L dosage, 325 mg/L initial concentration, 200 rpm shaking speed and 30 °C temperature. The adsorption equilibrium data were best fitted to the Freundlich model with correlation coefficient (R2) varying from 0.9500 to 0.9802. The adsorption kinetic data were best correlated to the pseudo-first-order model with R2 ranging from 0.8467 to 0.9621. Thermodynamic analysis showed that the process was spontaneous (∆G = - 7.19 to - 0.48 kJ/mol) and exothermic (∆H = - 12.82 to - 2.17 kJ/mol). This research concluded that rGOA is a very promising adsorbent for the remediation of water polluted by diclofenac.
    Matched MeSH terms: Diclofenac/chemistry*
  8. Lua GW, Muthukaruppan R, Menon J
    Dig Dis Sci, 2015 Oct;60(10):3118-23.
    PMID: 25757446 DOI: 10.1007/s10620-015-3609-9
    BACKGROUND: Non steroidal anti-inflammatory drugs (NSAIDs) have been shown to reduce the incidence of post endoscopic retrograde cholangiopancreatography pancreatitis (PEP). There were various trials using different routes and dosages of NSAIDs but meta-analysis revealed inconsistent results.

    AIMS: The aims of this study were to determine the efficacy of rectal diclofenac in preventing PEP and to evaluate any adverse events.

    METHODS: This was a randomized, open-label, two-arm, prospective clinical trial. Only patients at high risk of developing PEP were recruited. They received 100 mg rectal diclofenac or no intervention immediately after ERCP. The patients were reviewed 30 days after discharge to evaluate any adverse event.

    RESULTS: Among 144 recruited patients, 69 (47.9%) received diclofenac and 75 (52.1%) had no intervention. Eleven patients (7.6%) developed PEP, in which seven were from the diclofenac group and four were in the control group. Eight cases of PEP (5.5%) were mild and three cases (2.1%) were moderate. The differences in pancreatitis incidence and severity between both groups were not statistically significant. There were 11 adverse events reported. Clinically significant bleeding happened in four patients (2.8%): one from the diclofenac group and three from the control group. Other events included cholangitis: two patients (2.9%) from the diclofenac group and four (5.3%) from the control group. One patient from the diclofenac group (1.4%) had a perforation which was treated conservatively.

    CONCLUSIONS: In summary, prophylactic rectal diclofenac did not significantly decrease the incidence of PEP among patients at high risk for developing PEP. However, the administration of diclofenac was fairly safe with few clinical adverse events.

    Matched MeSH terms: Diclofenac/administration & dosage*
  9. Magosso E, Yuen KH, Choy WP, Ling SSN, Ng BH, Ur-Rahman N, et al.
    Med J Malaysia, 2004 Aug;59(3):352-6.
    PMID: 15727381
    The bioavailability of a generic diclofenac sodium sustained release tablet preparation (Zolterol, SR) was compared with the innovator product, Voltaren, SR. Twelve healthy adult male volunteers participated in the study, which was conducted according to a randomized, two-way crossover design with a wash out period of one week. The bioavailability of diclofenac was compared using the parameters area under the plasma concentration-time curve (AUC(0-infinity)), peak plasma concentration (Cmax) and time to reach peak plasma concentration (Tmax). No statistically significant difference was observed for both logarithmically transformed AUC(0-infinity), Cmax values and Tmax value of the two preparations.
    Matched MeSH terms: Diclofenac/blood; Diclofenac/pharmacokinetics*
  10. Tantowi NACA, Mohamed S, Lau SF, Hussin P
    Daru, 2020 Dec;28(2):443-453.
    PMID: 32388789 DOI: 10.1007/s40199-020-00343-y
    BACKGROUND: Osteoporotic-osteoarthritis is an incapacitating musculoskeletal illness of the aged.

    OBJECTIVES: The anti-inflammatory and anti-catabolic actions of Diclofenac were compared with apigenin-C-glycosides rich Clinacanthus nutans (CN) leaf extract in osteoporotic-osteoarthritis rats.

    METHODS: Female Sprague Dawley rats were randomized into five groups (n = 6). Four groups were bilateral ovariectomised for osteoporosis development, and osteoarthritis were induced by intra-articular injection of monosodium iodoacetate (MIA) into the right knee joints. The Sham group was sham-operated, received saline injection and deionized drinking water. The treatment groups were orally given 200 or 400 mg extract/kg body weight or 5 mg diclofenac /kg body weight daily for 28 days. Articular cartilage and bone changes were monitored by gross and histological structures, micro-CT analysis, serum protein biomarkers, and mRNA expressions for inflammation and catabolic protease genes.

    RESULTS: HPLC analysis confirmed that apigenin-C-glycosides (shaftoside, vitexin, and isovitexin) were the major compounds in the extract. The extract significantly and dose-dependently reduced cartilage erosion, bone loss, cartilage catabolic changes, serum osteoporotic-osteoarthritis biomarkers (procollagen-type-II-N-terminal-propeptide PIINP; procollagen-type-I-N-terminal-propeptide PINP; osteocalcin), inflammation (IL-1β) and mRNA expressions for nuclear-factor-kappa-beta NF-κβ, interleukin-1-beta IL-1β, cyclooxygenase-2; and matrix-metalloproteinase-13 MMP13 activities, in osteoporotic-osteoarthritis rats comparable to Diclofenac.

    CONCLUSION: This study demonstrates that apigenin-C-glycosides at 400 mg CN extract/kg (about 0.2 mg apigenin-equivalent/kg) is comparable to diclofenac in suppressing inflammation and catabolic proteases for osteoporotic-osteoarthritis prevention. Graphical abstract.

    Matched MeSH terms: Diclofenac/administration & dosage*; Diclofenac/pharmacology
  11. Bakrin FS, Makmor-Bakry M, Che Hon WH, Faizal SM, Manan MM, Ming LC
    Pharmacy (Basel), 2020 Dec 08;8(4).
    PMID: 33302438 DOI: 10.3390/pharmacy8040235
    INTRODUCTION: Drug utilization of analgesics in a private healthcare setting is useful to examine their prescribing patterns, especially the newer injectable cyclooxygenase (COX)-2 inhibitors (coxibs).

    OBJECTIVES: To evaluate the utilization of coxibs and traditional nonsteroidal anti-inflammatory drugs (tNSAIDs) indicated for postoperative orthopaedic pain control using defined daily dose (DDD) and ratio of use density to use rate (UD/UR).

    METHOD: A retrospective drug utilization review (DUR) of nonsteroidal anti-inflammatory drugs (NSAIDs) at an inpatient department of a private teaching hospital in Seremban, Malaysia was conducted. Patients' demographic characteristics, medications prescribed, clinical lab results, visual analogue scale (VAS) pain scores and length of hospital stay were documented. Orthopaedic surgeries, namely arthroscopy, reconstructive, and fracture fixation, were included. Stratified random sampling was used to select patients. Data were collected through patients' medical records. The DDD per 100 admissions and the indicator UD/UR were calculated with the World Health Organization's DDD as a benchmark. The inclusion criteria were patients undergoing orthopaedic surgery prescribed with coxibs (celecoxib capsules, etoricoxib tablets, parecoxib injections) and tNSAIDs (dexketoprofen injections, diclofenac sodium tablets). Data were analysed descriptively. This research was approved by the academic institution and the hospital research ethics committee.

    RESULT: A total of 195 records of patients who received NSAIDs were randomly selected among 1169 cases. In term of the types of orthopaedic surgery, the ratio of included records for arthroscopy:fracture fixation:reconstructive surgery was 55.4:35.9:8.7. Most of the inpatients had low rates of common comorbidities such as cardiovascular disease as supported by their baseline parameters. The majority were not prescribed with other concomitant prescriptions that could cause drug interaction (74.9%), or gastroprotective agents (77.4%). Overall, DDDs per 100 admissions for all NSAIDs were less than 100, except for parecoxib injections (389.23). The UD/UR for all NSAIDs were less than 100, except for etoricoxib tablets (105.75) and parecoxib injections (108.00).

    DISCUSSION: As per guidelines, the majority (96.9%) received other analgesics to ensure a multimodal approach was carried out to control pain. From the UD/UR results, the arthroscopy surgery was probably the most appropriate in terms of NSAID utilization.

    CONCLUSION: The prescribing pattern of NSAIDs except parecoxib was appropriate based on adverse effect and concurrent medication profile. The findings of this DUR provide insight for a low-risk patient population at a private specialized teaching hospital on the recommended use of NSAIDs for postoperative orthopaedic pain control.

    Matched MeSH terms: Diclofenac
  12. Saravanan M, Bhaskar K, Maharajan G, Pillai KS
    J Drug Target, 2011 Feb;19(2):96-103.
    PMID: 20380621 DOI: 10.3109/10611861003733979
    We have previously reported on the targeting of diclofenac sodium in joint inflammation using gelatin magnetic microspheres. To overcome complications in the administration of magnetic microspheres and achieve higher targeting efficiency, the present work focuses on the formulation of gelatin microspheres for intra-articular administration. Drug-loaded microspheres were prepared by the emulsification/cross-linking method, characterized by drug loading, size distribution, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), gas chromatography, and in vitro release studies. The targeting efficiency of microspheres was studied in vivo in rabbits. The microspheres showed drug loading of 9.8, 18.3, and 26.7% w/w with an average size range of 37-46 µm, depending upon the drug-polymer ratio. They were spherical in nature and free from surface drug as evidenced by the SEM photographs. FT-IR, DSC, and XRD revealed the absence of drug-polymer interaction and amorphous nature of entrapped drug. Gas chromatography confirms the absences of residual glutaraldehyde. The formulated microspheres could prolong the drug release up to 30 days in vitro. About 81.2 and 43.7% of administered drug in the microspheres were recovered from the target joint after 1 and 7 days of postintra-articular injection, respectively, revealing good targeting efficiency.
    Matched MeSH terms: Diclofenac/administration & dosage*; Diclofenac/pharmacokinetics
  13. Billa N, Yuen KH, Peh KK
    Drug Dev Ind Pharm, 1998 Jan;24(1):45-50.
    PMID: 15605596
    Ethyl acrylate-methyl methacrylate copolymer (Eudragit NE40D) was evaluated as matrix material for preparing controlled-release tablets of diclofenac sodium. Drug release could be modified in a predictable manner by varying the Eudragit NE40D content, but was pH dependent, being markedly reduced at lower pH. This could be attributed to the low solubility of the drug at these pH values. Thermal treatment of the tablets at 60 degrees C was also found to affect the rate of drug release, which was found to decrease with an increase in the treatment duration, but could be stabilized after 96 hr of treatment. This was also associated with a corresponding increase in the tablet tensile strength. However, treatment of the granules for 5 hr prior to compaction into tablets could shorten the stabilizing time of the drug release to 48 hr and that of the tensile strength to 24 hr. The effect of thermal treatment may be ascribed to better coalescence of the Eudragit particles to form a fine network, resulting in matrix of higher tortuosity and lower porosity.
    Matched MeSH terms: Diclofenac/chemistry*
  14. Chew CC, Ng S, Chee YL, Koo TW, Liew MH, Chee EL, et al.
    Invest New Drugs, 2017 08;35(4):399-411.
    PMID: 28285369 DOI: 10.1007/s10637-017-0447-y
    Coadministration of diclofenac and sunitinib, tyrosine kinase inhibitor, led to sex-divergent pharmacokinetic drug-drug interaction outcomes. Male and female mice were administered 60 mg/kg PO sunitinib alone (control groups) or with 30 mg/kg PO diclofenac. Sunitinib concentration in plasma, brain, kidney and liver were determined by HPLC and non-compartmental pharmacokinetic parameters calculated. In male mice, diclofenac decreased AUC0→∞ 38% in plasma (p diclofenac increased the liver uptake efficiency in male (27%, p diclofenac with probable clinical translatability due to potential different effects in male and female patients requiring careful selection of the NSAID and advanced TDM to implement a personalized treatment.
    Matched MeSH terms: Diclofenac/pharmacology*
  15. Dua K, Pabreja K, Ramana MV, Lather V
    J Pharm Bioallied Sci, 2011 Jul;3(3):417-25.
    PMID: 21966164 DOI: 10.4103/0975-7406.84457
    The objective of the present investigation was to study the effect of β-cyclodextrin (β-CD) on the in vitro dissolution of aceclofenac (AF) from molecular inclusion complexes. Aceclofenac molecular inclusion complexes in 1:1 and 1:2 M ratio were prepared using a kneading method. The in vitro dissolution of pure drug, physical mixtures, and cyclodextrin inclusion complexes was carried out. Molecular inclusion complexes of AF with β-CD showed a considerable increase in the dissolution rate in comparison with the physical mixture and pure drug in 0.1 N HCl, pH 1.2, and phosphate buffer, pH 7.4. Inclusion complexes with a 1:2 M ratio showed the maximum dissolution rate in comparison to other ratios. Fourier transform infrared spectroscopy and differential scanning calorimetry studies indicated no interaction between AF and β-CD in complexes in solid state. Molecular modeling results indicated the relative energetic stability of the β-CD dimer-AF complex as compared to β-CD monomer-AF. Dissolution enhancement was attributed to the formation of water soluble inclusion complexes with β-CD. The in vitro release from all the formulations was best described by first-order kinetics (R(2) = 0.9826 and 0.9938 in 0.1 N HCl and phosphate buffer, respectively) followed by the Higuchi release model (R(2) = 0.9542 and 0.9686 in 0.1 N HCl and phosphate buffer, respectively). In conclusion, the dissolution of AF can be enhanced by the use of a hydrophilic carrier like β-CD.
    Matched MeSH terms: Diclofenac
  16. Madzuki IN, Lau SF, Mohamad Shalan NAA, Mohd Ishak NI, Mohamed S
    J Biosci, 2019 Sep;44(4).
    PMID: 31502578
    Chondrosenescence (chondrocyte senescence) and subchondral bone deterioration in osteoarthritic rats were analyzed after treatment with the estrogenic herb Labisia pumila (LP) or diclofenac. Osteoarthritis (OA) was induced in bilaterally ovariectomized (OVX) rats by injecting mono-iodoacetate into the right knee joints. Rats were grouped (n = 8) into nontreated OVX+OA control, OVX+OA + diclofenac (5 mg/kg) (positive control), OVX+OA + LP leaf extract (150 and 300 mg/kg) and healthy sham control. After 8 weeks' treatment, their conditions were evaluated via serum biomarkers, knee joint histology, bone histomorphometry, protein and mRNA expressions. The LP significantly reduced cartilage erosion, femur bone surface alteration, bone loss and porosity and increased trabecular bone thickness better than diclofenac and the non-treated OA. The cartilage catabolic markers' (matrix metalloproteinase (MMP)-13, RUNX2, COL10a, ERa, CASP3 and HIF-2 alpha) mRNA expressions were down-regulated and serum bone formation marker, PINP, was increased by LP in a dose-dependent manner. The LP (containing myricetin and gallic acid) showed protection against chondrosenescence, chondrocyte death, hypoxia-induced cartilage catabolism and subchondral bone deterioration. The bone and cartilage protective effects were by suppressing proteases (collagen break-down), bone resorption and upregulating subchondral bone restoration. The cartilage ER alpha over-expression showed a strong positive correlation with MMP-13, COL10 alpha1, histological, micro-computed tomography evidence for cartilage degradation and chondrosenescence.
    Matched MeSH terms: Diclofenac/pharmacology
  17. Siddiqui R, Lakhundi S, Iqbal J, Khan NA
    Exp Parasitol, 2016 Jul 2;168:45-50.
    PMID: 27381503 DOI: 10.1016/j.exppara.2016.06.011
    Non-steroidal anti-inflammatory drug, Diclofenac, targeting COX have shown promise in the treatment of Acanthamoeba keratitis, but the underlying mechanisms remain unknown. Using various NSAIDs, Diclofenac sodium, Indomethacin, and Acetaminophen, here we determined the effects of NSAIDs on the biological properties of Acanthamoeba castellanii belonging to the T4 genotype. Using amoebicidal assays, the results revealed that Diclofenac sodium, and Indomethacin affected growth of A. castellanii. In contrast, none of the compounds tested had any effect on the viability of A. castellanii. Importantly, all NSAIDs tested abolished A. castellanii encystation. This is a significant finding as the ability of amoebae to transform into the dormant cyst form presents a significant challenge in the successful treatment of infection. The NSAIDs inhibit production of cyclo-oxegenase, which regulates the synthesis of prostaglandins suggesting that cyclooxygenases (COX-1 and COX-2) and prostaglandins play significant role(s) in Acanthamoeba biology. As NSAIDs are routinely used in the clinical practice, these findings may help design improved preventative strategies and/or of therapeutic value to improve prognosis, when used in combination with other anti-amoebic drugs.
    Matched MeSH terms: Diclofenac
  18. Wong TW, Wahab S, Anthony Y
    Drug Dev Ind Pharm, 2007 Jul;33(7):737-46.
    PMID: 17654022
    The drug release behavior of beads made of poly(methyl vinyl ether-co-maleic acid) was investigated with respect to the influence of microwave irradiation. The beads were prepared by an extrusion method with sodium diclofenac as a model water-soluble drug. The beads were subjected to microwave irradiation at 80 W for 5 and 20 min, and at 300 W for 1 min 20 s and 5 min 20 s. The profiles of drug dissolution, drug content, drug-polymer interaction, and polymer-polymer interaction were determined by using dissolution testing, drug content assay, differential scanning calorimetry, and Fourier transform infra-red spectroscopy. Keeping the level of supplied irradiation energy identical, treatment of beads by microwave at varying intensities of irradiation did not bring about similar drug release profiles. The extent and rate of drug released from beads were markedly enhanced through treating the samples by microwave at 80 W as a result of loss of polymer-polymer interaction via the (CH(2))(n) moiety, but decreased upon treating the beads by microwave at 300 W following polymer-polymer interaction via the O-H, COOH, and COO(-) moieties as well as drug-polymer interaction via the N-H, O-H, COO(-), and C-O moieties. The beads treated by microwave at 300 W exhibited a higher level of drug release retardation capacity than those that were treated by microwave at 80 W in spite of polymer-polymer interaction via the (CH(2))(n) moiety was similarly reduced in the matrix. The mechanism of drug release of both microwave-treated and untreated beads tended to follow zero order kinetics. The drug release was markedly governed by the state of polymer relaxation of the matrix and was in turn affected by the state of polymer-polymer and/or drug-polymer interaction in beads.
    Matched MeSH terms: Diclofenac/radiation effects; Diclofenac/chemistry*
  19. Mardziah RE, Wong TW
    Drug Dev Ind Pharm, 2010 Oct;36(10):1149-67.
    PMID: 20380595 DOI: 10.3109/03639041003695063
    Microspheres prepared from rigid guluronic acid- (MG) and flexible mannuronic acid-rich (MC) alginate will undergo different drug release changes with respect to the influence of microwave on the matrix. An in-depth understanding of their differences in drug release changes is attainable through investigating cross-linking agent-free alginate microspheres prepared by spray-drying technique.
    Matched MeSH terms: Diclofenac/pharmacokinetics
  20. Hui KC, Ang WL, Yahya WZN, Sambudi NS
    Chemosphere, 2022 Mar;290:133377.
    PMID: 34952025 DOI: 10.1016/j.chemosphere.2021.133377
    The present work demonstrates the coupling of titanium dioxide, TiO2 nanoparticles (TNP) with N-doped, Bi-doped, and N-Bi co-doped rice husk-derived carbon dots (CDs) via a facile dispersion method, forming respective photocatalyst composites of CDs/TNP, N-CDs/TNP, Bi-CDs/TNP and N-Bi-CDs/TNP. Characterization analyzes verified the successful incorporation of respective CDs samples into TNP, forming photocatalyst composite with narrowed band gap and quenched photoluminescence intensity. Photocatalytic activity of TNP and the respective composites was investigated for photodegradation of diclofenac (DCF) under both simulated sunlight and natural sunlight irradiation. The as-prepared N-Bi-CDs/TNP composite showed the best photocatalytic performance among all composites, able to completely degrade 5 ppm of DCF within 60 min and 180 min under both types of visible light irradiation, respectively. The N-Bi-CDs/TNP composite also showed a TOC removal efficiency up to 87.63%. N-Bi-CDs, worked as photosensitizer and electron reservoir, contributed to the outstanding photocatalytic activity of N-Bi-CDs/TNP, whereby the recombination was prolonged and light absorption was shifted towards the visible light region. Furthermore, the composite of N-Bi-CDs/TNP also demonstrated good stability and reusability over repeated degradation cycles. The photodegradation of DCF resulted into several intermediates, which were identified from LC-MS analysis. The present work could provide an insight on the application of heteroatoms doped and co-doped carbon dots in semiconductor oxide as high performance photocatalysts.
    Matched MeSH terms: Diclofenac
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