Diclofenac Sodium (diclofenac + sodium)

Distribution by Scientific Domains


Selected Abstracts


Diclofenac sodium and occlusal splint therapy in TMJ osteoarthritis: a randomized controlled trial

JOURNAL OF ORAL REHABILITATION, Issue 10 2008
C. MEJERSJÖ
Summary, The aim of the study was to compare treatment with diclofenac sodium (Voltaren 3 × 50 mg) to occlusal splint therapy in a randomized, single-blind controlled trial of patients with a diagnosis of temporomandibular joint (TMJ) osteoarthritis (OA) in accordance with Research Diagnostic Criteria for temporomandibular disorders. Patients with general joint disorders or restrictions against medication with non-steroidal anti-inflammatory drug were not included. Twenty-seven females and two males (aged 36,76 years) included, answered a standardized questionnaire and were clinically examined and they underwent TMJ tomography. The treatment was randomized to either splint (n = 15) or diclofenac (n = 14). The temperatures over the TMJs were determined. The patients were re-examined 1 week, 1 month and 3 months after the start of treatment. A 1-year follow-up was carried out using questionnaires. After 1 week of treatment with diclofenac, significant reductions of pain and discomfort, TMJ tenderness and joint pain on jaw movements were noted. The splint therapy gave a significant reduction of reported symptoms after 1 month of treatment. Both treatments gave few adverse effects and were on an equal level. Estimation of the degree of inflammation by measuring the surface temperature over the TMJ was not reliable. Structural changes of the symptomatic TMJs were radiographically found in 82%, the contralateral, symptom-free TMJ had changes in 36%. There was a discrepancy between the clinical and the radiographical findings. Diclofenac gave a more rapid improvement, but both treatments gave a significant reduction of symptoms of TMJ OA within 3 months which remained at the one-year follow-up. [source]


Biowaiver monographs for immediate release solid oral dosage forms: Diclofenac sodium and diclofenac potassium,

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2009
B. Chuasuwan
Abstract Literature data are reviewed regarding the scientific advisability of allowing a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing either diclofenac potassium and diclofenac sodium. Within the biopharmaceutics classification system (BCS), diclofenac potassium and diclofenac sodium are each BCS class II active pharmaceutical ingredients (APIs). However, a biowaiver can be recommended for IR drug products of each salt form, due to their therapeutic use, therapeutic index, pharmacokinetic properties, potential for excipient interactions, and performance in reported BE/bioavailability (BA) studies, provided: (a) test and comparator contain the same diclofenac salt; (b) the dosage form of the test and comparator is identical; (c) the test product contains only excipients present in diclofenac drug products approved in ICH or associated countries in the same dosage form, for instance as presented in this paper; (d) test drug product and comparator dissolve 85% in 30 min or less in 900 mL buffer pH 6.8, using the paddle apparatus at 75 rpm or the basket apparatus at 100 rpm; and (e) test product and comparator show dissolution profile similarity in pH 1.2, 4.5, and 6.8. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:1206,1219, 2009 [source]


Synthesis, analgesic, anti-inflammatory and ulcerogenic index activities of novel 2-methylthio-3-substituted-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-ones

DRUG DEVELOPMENT RESEARCH, Issue 3 2007
V. Alagarsamy
Abstract A variety of novel 2-methylthio-3-substituted amino-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-ones were synthesized by reacting 3-amino-2-methylthio-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-one with different aldehydes and ketones. The starting material 3-amino-2-methylthio-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-one was synthesized from 2-amino-3-carbethoxy-4,5-dimethyl thiophene. The compounds were investigated for their analgesic activity in albino mice, and for their anti-inflammatory and ulcerogenic index activities in Wistar rats. The compound 2-(1-ethylpropylideneamino)-2-methylthio-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-one (AS2) showed the most potent analgesic activity of the series. It also showed more potent anti-inflammatory activity when compared to the reference standard, diclofenac sodium. The test compounds showed only mild ulcerogenic potential when compared to aspirin. Drug Dev Res 68:134,142, 2007. © 2007 Wiley-Liss, Inc. [source]


In vitro permeation of diclofenac sodium from novel microemulsion formulations through rabbit skin

DRUG DEVELOPMENT RESEARCH, Issue 1 2005
Gülten Kantarc
Abstract In order to increase topical penetration of the nonsteroidal anti-inflammatory drug, diclofenac sodium, new microemulsion formulations were prepared to increase drug solubility and in vitro penetration of the drug. The influence of dimethyl sulfoxide and propylene glycol were also investigated as enhancers on the in vitro penetration of diclofenac sodium using Franz diffusion cells using excised dorsal rabbit skin. Factorial randomized design was performed to analyze the results of in vitro permeation studies. Microemulsions prepared with isopropyl alcohol were superior to those prepared with propanol. Enhancers had different effects depending on the formulation. Propylene glycol was superior to dimethyl sulfoxide when incorporated into isopropyl alcohol microemulsion, whereas dimethyl sulfoxide was superior to propylene glycol in propanol microemulsions. There were no observable histopathological differences between the skin of the control group and the treated groups at the light microscope level due to swelling of the skin tissue. The present study shows that microemulsion formulations containing isopropyl alcohol as co-surfactant and propylene glycol as enhancer represent a promising approach for a topical vehicle for diclofenac sodium. Drug Dev. Res. 65:17,25, 2005. © 2005 Wiley-Liss, Inc. [source]


Oxidation of diclofenac sodium by diperiodatoargantate(III) in aqueous alkaline medium and its determination in urine and blood by kinetic methods

INTERNATIONAL JOURNAL OF CHEMICAL KINETICS, Issue 6 2010
P. N. Naik
The kinetics and oxidation of diclofenac sodium (DFS) by diperiodatoargentate(III) (DPA) in alkaline medium at 298 K and at a constant ionic strength of 0.60 mol dm,3 were studied spectrophotometrically. The oxidation products were [2-(2,6-dicloro-phynylamino)-phenyl]-methenol and Ag(I), identified by LC-ESI-MS and IR spectral studies. The reaction between DFS and DPA in alkaline medium exhibits 1:1 stoichiometry. The reaction is first order in [DPA] and has a less than unit order dependence each in [DFS] and [alkali]. Increasing concentrations of IO,4 retard the reaction. The active species of DPA proposed to be monoperiodatoargentate(III), and a mechanism is suggested. The rate constants involved in the different steps of the mechanism were determined and are discussed. The activation parameters with respect to a rate-limiting step of the mechanism were determined. The thermodynamic quantities were also determined. Using the oxidation of DFS by DPA, DFS was analyzed by kinetic methods in urine and blood sample. The proposed method enables DFS analysis in the range from 5.0 × 10,5 to 5.0 × 10,3 mol dm,3. © 2010 Wiley Periodicals, Inc. Int J Chem Kinet 42: 336,346, 2010 [source]


Glutaraldehyde-crosslinked chitosan beads for controlled release of diclofenac sodium

JOURNAL OF APPLIED POLYMER SCIENCE, Issue 1 2007
V. H. Kulkarni
Abstract An inexpensive and simple method was adopted for the preparation of chitosan beads, crosslinked with glutaraldehyde (GA), for the controlled release of diclofenac sodium (DS). The beads were prepared by varying the experimental conditions such as pH, temperature, and extent of crosslinking. The absence of any chemical interaction among drug, polymer, and the crosslinking agent was confirmed by FTIR and thermal analysis. The beads were characterized by microscopy, which indicated that the particles were in the size range of 500,700 ,m and SEM studies revealed smooth surface and spherical shape of beads. The beads produced at higher temperature and extended exposure to GA exhibited lower drug content, whereas increased drug loading resulted in enhanced drug release. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 103: 211,217, 2007 [source]


Enhancing therapeutic loading and delaying transport via molecular imprinting and living/controlled polymerization

AICHE JOURNAL, Issue 1 2010
Asa D. Vaughan
Abstract This work demonstrates for the first time molecular imprinting using a "living/controlled" polymerization (LCP) strategy to enhance template loading/affinity and delay release in weakly crosslinked gels. Two gel systems were studied: poly(DEAEM- co -HEMA- co -PEG200DMA) gels imprinted for diclofenac sodium and poly(MAA- co -EGDMA) gels imprinted for ethyl adenine-9-acetate. Experimental evidence confirms that template diffusion coefficients within imprinted gels can be heavily influenced by template binding affinity. Recognition studies revealed significant increases in template loading/affinity with large increases in loading for LCP, and dynamic template release studies showed that imprinting via LCP extends the template release profile by twofold over that of imprinting via conventional free-radical polymerization techniques and fourfold over the control network (less Fickian and toward zero-order release with a profile coefficient of 0.70). Analysis of reaction kinetics indicated that LCP with reversible termination events increases the chemically controlled chain propagation mechanism, and that binding sites are formed during this phase of the polymerization. © 2009 American Institute of Chemical Engineers AIChE J, 2010 [source]


Diclofenac sodium and occlusal splint therapy in TMJ osteoarthritis: a randomized controlled trial

JOURNAL OF ORAL REHABILITATION, Issue 10 2008
C. MEJERSJÖ
Summary, The aim of the study was to compare treatment with diclofenac sodium (Voltaren 3 × 50 mg) to occlusal splint therapy in a randomized, single-blind controlled trial of patients with a diagnosis of temporomandibular joint (TMJ) osteoarthritis (OA) in accordance with Research Diagnostic Criteria for temporomandibular disorders. Patients with general joint disorders or restrictions against medication with non-steroidal anti-inflammatory drug were not included. Twenty-seven females and two males (aged 36,76 years) included, answered a standardized questionnaire and were clinically examined and they underwent TMJ tomography. The treatment was randomized to either splint (n = 15) or diclofenac (n = 14). The temperatures over the TMJs were determined. The patients were re-examined 1 week, 1 month and 3 months after the start of treatment. A 1-year follow-up was carried out using questionnaires. After 1 week of treatment with diclofenac, significant reductions of pain and discomfort, TMJ tenderness and joint pain on jaw movements were noted. The splint therapy gave a significant reduction of reported symptoms after 1 month of treatment. Both treatments gave few adverse effects and were on an equal level. Estimation of the degree of inflammation by measuring the surface temperature over the TMJ was not reliable. Structural changes of the symptomatic TMJs were radiographically found in 82%, the contralateral, symptom-free TMJ had changes in 36%. There was a discrepancy between the clinical and the radiographical findings. Diclofenac gave a more rapid improvement, but both treatments gave a significant reduction of symptoms of TMJ OA within 3 months which remained at the one-year follow-up. [source]


Biowaiver monographs for immediate release solid oral dosage forms: Diclofenac sodium and diclofenac potassium,

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2009
B. Chuasuwan
Abstract Literature data are reviewed regarding the scientific advisability of allowing a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing either diclofenac potassium and diclofenac sodium. Within the biopharmaceutics classification system (BCS), diclofenac potassium and diclofenac sodium are each BCS class II active pharmaceutical ingredients (APIs). However, a biowaiver can be recommended for IR drug products of each salt form, due to their therapeutic use, therapeutic index, pharmacokinetic properties, potential for excipient interactions, and performance in reported BE/bioavailability (BA) studies, provided: (a) test and comparator contain the same diclofenac salt; (b) the dosage form of the test and comparator is identical; (c) the test product contains only excipients present in diclofenac drug products approved in ICH or associated countries in the same dosage form, for instance as presented in this paper; (d) test drug product and comparator dissolve 85% in 30 min or less in 900 mL buffer pH 6.8, using the paddle apparatus at 75 rpm or the basket apparatus at 100 rpm; and (e) test product and comparator show dissolution profile similarity in pH 1.2, 4.5, and 6.8. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:1206,1219, 2009 [source]


Influence of magnesium aluminium silicate on rheological, release and permeation characteristics of diclofenac sodium aqueous gels in-vitro

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 4 2005
Thaned Pongjanyakul
The effect of magnesium aluminium silicate (MAS) on rheological, release and permeation characteristics of diclofenac sodium (DS) aqueous gels was investigated. DS aqueous gels were prepared using various gelling agents, such as 15% w/w poloxamer 407 (PM407), 1% w/w hydroxypropylmethylcellulose (HPMC), and 1% w/w high and low viscosity grades of sodium alginate (HV-SA and LV-SA, respectively). Different amounts of MAS (0.5, 1.0 and 1.5% w/w) were incorporated into the DS gels. Incorporation of MAS into the DS gels prepared using SA or PM407 caused a statistical increase in viscosity (P<0.05) and a shift from Newtonian flow to pseudoplastic flow with thixotropic property. The DS release rates of these composite gels were significantly decreased (P<0.05) when compared with the control gels. This was due to an interaction between MAS and PM407 or SA, and adsorption of DS onto MAS particles. Moreover, a longer lag time and no change in DS permeation flux were found when MAS was added to the gels. The findings suggest that the rheological characteristics of gels prepared using PM407 or SA could be improved by incorporating MAS. However, the use of MAS could retard the DS release and extend the lag time of DS permeation. [source]


Analgesic, antipyretic and Ulcerogenic properties of an indigenous formulation , Kalpaamruthaa

PHYTOTHERAPY RESEARCH, Issue 6 2007
Rajendran Mythilypriya
Abstract A modified indigenous Siddha formulation Kalpaamruthaa (KA), containing Semecarpus anacardium nut milk extract (SA), dried powder of Emblica officinalis (EO) fruit and honey was evaluated for its analgesic, antipyretic and Ulcerogenic properties. Both SA and KA, at a dose of 150 mg/kg b. wt were compared with the standard drug diclofenac sodium. KA exhibited an enhanced effect on all properties compared with that found with sole SA treatment, and is likely to be due to synergistic and additive interactions within the complex mixture of phytochemicals present in KA. Copyright © 2007 John Wiley & Sons, Ltd. [source]


,Multimodal' approach to management of prostate biopsy pain and effects on sexual function: efficacy of levobupivacaine adjuvant to diclofenac sodium , a prospective randomized trial

ANDROLOGIA, Issue 1 2010
T. Aktoz
Summary We assessed the analgesic efficacy of levobupivacaine when administered as an adjuvant to diclofenac sodium in prostate biopsy pain management and effects of prostate biopsy on sexual function. Ninety patients underwent transrectal ultrasound (TRUS)-guided biopsy of the prostate and were randomly assigned to three groups: group D received diclofenac sodium suppository; Group L received periprostatic injection of levobupivacaine; group DL received diclofenac suppository and levobupivacaine in addition. Patients were asked to use a visual analogue scale score (VAS) questionnaire about pain after 10 core prostate biopsy. Sixty-two patients reported to be prostate cancer-free underwent further evaluation with the International Index of Erectile Function-5 (IIEF-5) questionnaire at 1 and 3 months after biopsy. Mean pain scores during prostate biopsy were significantly lower in group DL and were superior to the group L and group D (P < 0.001). Mean IIEF-5 score prior to biopsies was significantly higher when compared with the mean IIEF-5 score 1 month after biopsy (P < 0.0001). Mean IIEF-5 scores 1 month after biopsy were significantly lower when compared with the mean IIEF-5 scores 3 months after biopsy (P = 0.002). TRUS-guided prostate biopsies have a statistically significant impact on short-term erectile function, but this difference is not clinically significant; however, medium-term erectile function is not affected both statistically and clinically. [source]


Synthesis of New 2,3-Dihydroquinazolin-4(1H)-one Derivatives for Analgesic and Anti-inflammatory Evaluation

ARCHIV DER PHARMAZIE, Issue 5 2010
Osama I. El-Sabbagh
Abstract Starting from isatoic anhydrides, several new 2,3-dihydroquinazolin-4(1H)-one derivatives bearing chalcone or pyrazole or thiazole moieties at the third position were synthesized. The analgesic and anti-inflammatory activities for most compounds were studied at a dose level of 50 mg/kg via the acetic-acid-induced writhing-response method and carrageenan-induced edema method, respectively. The study showed that the chalcones bearing a 4-chlorophenyl group 4c or 4-nitrophenyl group 4b were the most active ones as analgesics. Both chalcone 4c and N -phenyl pyrazole bearing 4-methoxy phenyl group 5b showed a higher anti-inflammatory activity than celecoxib but still lower than that of diclofenac sodium. Moreover, the chalcone 4c has nearly the same ulcerogenic index as the selective cyclooxygenase-2 inhibitor celecoxib. [source]


Clinical efficacy of diclofenac sodium and flunixin meglumine as adjuncts to antibacterial treatment of respiratory disease of calves

AUSTRALIAN VETERINARY JOURNAL, Issue 6 2010
M Guzel
Objective To compare the efficacy of the non-steroidal antiinflammatory drugs, diclofenac sodium and flunixin meglumine as adjuncts to the antibiotic treatment of bovine respiratory disease (BRD). Procedure We randomly allocated 80 Holstein calves with BRD to three groups. All the calves received a dose of 2.5 mg/kg tulathromycin by single subcutaneous injection and two of the groups received, in addition, either 2.5 mg/kg diclofenac sodium as a single intramuscular injection (diclofenac group, n = 30) or 2.2 mg/kg flunixin meglumine as an intravenous injection on the first three consecutive days after tulathromycin administration (flunixin group, n = 30). All calves were given a clinical score prior to initial treatment (day 0) and after treatment (days 1, 2, 3, 7 and 14) by observing appetite, demeanour, rectal temperature, the rate and type of respiration, presence or absence of coughing, and nasal discharge. Results During the first 48 h, improvement of adverse signs of respiratory disease, such as pyrexia and elevated respiratory rate, and of a high clinical index score was significant in the two adjunct groups compared with the calves receiving antibiotic alone. The reduction in pyrexia was greatest in the diclofenac group. There were no statically significant differences between treatment groups with regard to eventual perceived recovery from respiratory disease in 14 days. Conclusion In this trial, a single intramuscular dose of diclofenac sodium was equally effective as three intravenous injections of flunixin meglumine given on consecutive days as adjunctive therapy for BRD. [source]


Antinociceptive effect of a ruthenium complex in mice

AUTONOMIC & AUTACOID PHARMACOLOGY, Issue 4 2008
M. P. Cristiano
Summary 1,The ruthenium complexes are important tools in inorganic chemistry. Different biological properties are found in the presence of distinct coordinate ligands, which offer a variety of potential clinical and pharmacological uses. 2,The aim of this work was to evaluate the antinociceptive and behavioural effects of the ruthenium complex, trans -[RuCl2(i-dinic)4]Cl, in mice. 3,The potential analgesic activity was tested using the formalin and hot plate tests and the behavioural effect was evaluated using the rotarod and spontaneous locomotor tests. The complex was administered at concentrations of 1.3, 4.5 and 18.0 ,mol kg,1 i.p. Morphine (6.0 mg kg,1, i.p.) and diclofenac sodium (20.0 mg kg,1, i.p.) were used as reference drugs. 4,The compound had no sedative activity on motor ataxia in the behavioural and analgesic tests. No significant effect was observed in the first phase of the formalin test, however, an effect was observed in the second phase. 5,The complex studied was probably more powerful than the reference drugs as an antinociceptive agent, as this mechanism also involved the nitric oxide (NO) pathway. From this perspective, further experimental studies will be useful to understand the effect of these compounds on NO and the relationship between prostaglandin and NO biosynthesis. [source]


Quantitative separation of oxytocin, norfloxacin and diclofenac sodium in milk samples using capillary electrophoresis

BIOMEDICAL CHROMATOGRAPHY, Issue 9 2009
Amber R. Solangi
Abstract A simple, sensitive and rapid method has been developed for simultaneous separation and quantification of three different drugs: oxytocin (OT), norfloxacin (NOR) and diclofenac (DIC) sodium in milk samples using capillary electrophoresis (CE) with UV detection at 220 nm. Factors affecting the separation were pH, concentration of buffer and applied voltage. Separation was obtained in less than 9 min with sodium tetraborate buffer of pH 10.0 and applied voltage 30 kV. The separation was carried out from uncoated fused silica capillary with effective length of 50 cm with 75 µm i.d. The carrier electrolyte gave reproducible separation with calibration plots linear over 0.15,4.0 µg/mL for OT, 5,1000 µg/mL for NOR and 3,125 µg/mL for DIC. The lower limits of detection (LOD) were found to be 50 ng/mL for OT, and 1 µg/mL for NOR and DIC. The method was validated for the analysis of drugs in milk samples and pharmaceutical preparations with recovery of drugs within the range 96,100% with RSD 0.9,2.8%. Copyright © 2009 John Wiley & Sons, Ltd. [source]