Aim To study the exchange reaction characteristics of anion exchange resin for diclofenac sodium. Methods The drug-resin complexes were prepared by a batch method with diclofenac sodium as the model drug and the stron...Aim To study the exchange reaction characteristics of anion exchange resin for diclofenac sodium. Methods The drug-resin complexes were prepared by a batch method with diclofenac sodium as the model drug and the strong anion exchange resin (201 × 7) as the carrier. The effects of different forms (OH~ - and Cl~ - ) of the strong anion exchange resin, the particle size of the resin, and the reaction temperature on the exchange behavior were described. The exchange kinetic profiles were fitted. The related exc...展开更多
The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assay...The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.展开更多
Metal‐organic framework MIL‐100(Fe)and g‐C3N4 heterojunctions(MG‐x,x=5%,10%,20%,and 30%,x is the mass fraction of MIL‐100(Fe)in the hybrids)were facilely fabricated through ball‐milling and annealing,and charact...Metal‐organic framework MIL‐100(Fe)and g‐C3N4 heterojunctions(MG‐x,x=5%,10%,20%,and 30%,x is the mass fraction of MIL‐100(Fe)in the hybrids)were facilely fabricated through ball‐milling and annealing,and characterized by powder X‐ray diffraction,Fourier transform infrared spectroscopy,thermogravimetric analysis,transmission electron microscopy,UV‐visible diffuse‐reflectance spectrometry,and photoluminescence emission spectrometry.The photocatalytic activities of the series of MG‐x heterojunctions toward Cr(VI)reduction and diclofenac sodium degradation were tested upon irradiation with simulated sunlight.The influence of different organic compounds(ethanol,citric acid,oxalic acid,and diclofenac sodium)as hole scavengers and the pH values(2,3,4,6,and 8)on the photocatalytic activities of the series of MG‐x heterojunctions was investigated.MG‐20%showed superior photocatalytic Cr(VI)reduction and diclofenac sodium degradation performance than did the individual MIL‐100(Fe)and g‐C3N4 because of the improved separation of photoinduced electron‐hole charges,which was clarified via photoluminescence emission and electrochemical data.Moreover,the MG‐x exhibited good reusability and stability after several runs.展开更多
Objective:To observe the effects of Methyl Carboprost and Diclofenac Sodium on opening orifice of uterus and pain controlling in patients with uterine cervix cancer (UCC) when receiving intracavitary brachytherapy. Me...Objective:To observe the effects of Methyl Carboprost and Diclofenac Sodium on opening orifice of uterus and pain controlling in patients with uterine cervix cancer (UCC) when receiving intracavitary brachytherapy. Methods: Sixty patients with UCC of stage IIA-IIIB were divided into three groups randomly before receiving the intracavitary brachytherapy: the patients in group A received Methyl Carboprost in the hind fornix of the vagina, group B received Diclofenac Sodium in the anus, while group C was the control group. Results: The painlessness rates in groups A, B and C were 89.9%, 91.3% and 36.4%, respectively. The incidences of patients with relaxed uterus cervix in groups A, B and C were 91.7%, 85.9% and 48.9%, respectively. Conclusion: Methyl Carboprost and Diclofenac Sodium are useful in relaxing uterus cervix and pain controlling in patients with UCC when receiving intracavitary brachytherapy.展开更多
Objective:To discuss the clinical study on Fengshi Qutong capsules combined with diclofenac sodium in the treatment of ankylosing spondylitis.Methods:80 patients who were treated for ankylosing spondylitis from June 2...Objective:To discuss the clinical study on Fengshi Qutong capsules combined with diclofenac sodium in the treatment of ankylosing spondylitis.Methods:80 patients who were treated for ankylosing spondylitis from June 2019 to June 2020 were selected and divided into two groups.The experimental group was treated with Fengshi Qutong capsules combined with diclofenac sodium,and the control group was treated with sulfasalazine enteric-coated tablets.Results:The treatment efficacy,VAS score,BASDAI score,BASFI score,CRP level,TNF-α level,IL-Iβ level,and the incidence of adverse reactions between the two groups were significantly different(P<0.05).Conclusion:The application of Fengshi Qutong capsules combined with diclofenac sodium in the treatment of patients with ankylosing spondylitis is beneficial to improve the treatment efficacy,reduce the levels of CRP,TNF-α,and IL-Iβ,reduce the incidence of adverse reactions,and reduce the VAS,BASDAI and BASFI scores,rendering it of important clinical value.展开更多
Polymethylmethacrylate (PMMA) coated microcapsules of diclofenac sodium (DFS) were prepared by a modified wa-ter-in-oil-in-water (W1/O/W2) emulsion solvent evaporation method using sodium alginate (SAL) as a matrix ma...Polymethylmethacrylate (PMMA) coated microcapsules of diclofenac sodium (DFS) were prepared by a modified wa-ter-in-oil-in-water (W1/O/W2) emulsion solvent evaporation method using sodium alginate (SAL) as a matrix material in the internal aqueous phase (W1).Their performance with respect to controlled release of the drug in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) were evaluated, and compared with non-matrix microcapsules prepared by the conventional W1/O/W2 emulsion solvent evaporation method. Scanning electron micrographs (SEM) revealed that all the microcapsules were discrete and spherical in shape;however, the surface porosity of the matrix microcap-sules appeared to be less than that of the non-matrix microcapsules. In case of non-matrix microcapsules, an increase in the volume of water in W1 phase resulted in decrease in the drug entrapment efficiency (DEE) along with increase in release of the drug in both SGF and SIF. While in case of matrix microcapsules increase in the amount of SAL in W1 phase and concentration of the coating polymer in organic phase led to increase in DEE of the matrix microcapsules and considerable decrease in the drug release in both SGF and SIF. No interaction between the drug and any of the polymers used to prepare microcapsules was evident from Fourier transform infra-red (FTIR) analysis. The matrix microcapsules prepared using higher concentration of SAL and PMMA released the drug following zero order or Case-II transport model. The matrix microcapsules appeared to be suitable for releasing lesser amounts of DFS in SGF and providing extended release in SIF.展开更多
<Abstract>Purpose:To investigate the inhibitory effect of diclofenac sodium on rabbit corneal epithelial cells (RCECs) in vitro and explore its pharmacological mechanism. Methods: The fresh rabbit cornea was cul...<Abstract>Purpose:To investigate the inhibitory effect of diclofenac sodium on rabbit corneal epithelial cells (RCECs) in vitro and explore its pharmacological mechanism. Methods: The fresh rabbit cornea was cultured to get the primary RCECs,and RCECs of passage 2 were used for the research. The cells were divided into experimental groups,the cells in which were incubated with different concentrations(18.18, 27.27, 36.36, 45.45, 54.55 μg/ml) of diclofenac sodium, and control group. The effect of diclofenac sodium on the proliferation of cells was measured by methyl thiazolyl thiazolium (MTT) assay 24, 48 and 72 h after incubation. While the RCECs were divided into experimental groups, the cells in which were incubated with 9 and 12.5 μg/ml diclofenac sodium, and control group. The cell cycle and apoptotic rate were observed by flow cytometer. Results:MTT assay showed that diclofenac sodium had obvious inhibitory effect on RCECs,and the inhibition rate was increasing along with the increase of the concentration of diclofenac sodium and the incubation time(P<0.05). Flow cytometer showed that after incubation with diclofenac sodium, the cells in G0/G1 phase were obviously increased, the apoptosis cusp and apoptotic rate were increased. Conclusion: Diclofenac sodium has obvious inhibitory effect on RCECs, which was dosage-dependent,and it may function by inducing cell apoptosis and ceasing cells cycles.展开更多
This work aimed to find the effect of cranberry extract (75 and 150 mg/kg·b·w) and vit. C (1 g/kg·b·w orally) on renal toxicity induced by Diclofenac sodium in male albino r...This work aimed to find the effect of cranberry extract (75 and 150 mg/kg·b·w) and vit. C (1 g/kg·b·w orally) on renal toxicity induced by Diclofenac sodium in male albino rats. Treated rats with diclofenac sodium with a concentration 150 mg/kg·b·w, expressed a significant increase in several parameters includes, plasma total cholesterol, LDL-cholesterol, and triglyceride as well as renal nitric oxide (NO), tumor necrosis factor-alfa (TNF-α) and TBARS. In addition, a significant reduction in renal superoxide dismutase (SOD), GSH, catalase (CAT) and plasma HDL. The present results explain that, using cranberry extract and vit. C resulted in increasing the level of GSH, CAT and SOD as well as gene expression of renal SOD, CAT and IL-22 and reduce the level of TBARs significantly which led to preventing renal tissue damage. Our results also revealed that cranberry extract can protect DNA from damage as obtained from comet essay. TM-U was elevated in DCLF treated group when compared with normal. However cranberry extract was able to reduce this elevation in dose dependant manner. Histological features in H&E taken to different groups also mirrors this findings. DCLF causes many changes in renal tissue include infiltration by inflammatory cells, attenuated glomeruli, apoptosis in tubular epithelia.展开更多
The release profiles of acidic form of diclofenac sodium adsorbed on mesoporous silicas (Silochrom and two samples of spherical silicas) were compared with the dissolution characteristics of the pure drug. Desorption ...The release profiles of acidic form of diclofenac sodium adsorbed on mesoporous silicas (Silochrom and two samples of spherical silicas) were compared with the dissolution characteristics of the pure drug. Desorption of diclofenac sodium from impregnated silicas with various surface liophilicity and composites of silica with chitosan have been studied using rotating basket method in phosphate buffer, pH 6.8. Sedimentations of sodium diclofenac via adsorption and impregnation from alcohol solution on fumed silica and modified silicas with grafted aminopropyl and trimethylsilyl groups were carried out. Polymer-containing composites have been prepared by capsulation of silica particles with impregnated diclofenac sodium by protonated and deprotonated forms of chitosan. Effect of the silica surface nature on the active substance release rate was ascertained. Significant prolongation of diclofenac sodium release was detected in the case of application of hydrophobic silica as a carrier and protonated chitosan as a polymeric shell.展开更多
Purpose: To determine the effect of 0.1% diclofenac sodium (DS) eyedrops made in China on preventing surgically induced miosis and inflammation. Methods: Seventy cases of cataract inpatients were randomly divided into...Purpose: To determine the effect of 0.1% diclofenac sodium (DS) eyedrops made in China on preventing surgically induced miosis and inflammation. Methods: Seventy cases of cataract inpatients were randomly divided into two groups. DS eyedrops and normal saline as placebo were applied respectively 3h, 1h, 0.5h before operation and once every morning for 7 days after operation. The pupil diameter was measured five times at different stages during the extracapsular cataract extraction. The eyepain, photophobia, conjunctival injection, KP, aqueous flare and light reaction of pupil were observed once a day after operation for a week. Results: 37 eyes in DS group and 33 eyes in placebo group were included in the study. 32 of 37 eyes in DS group (86.5%) maintained mydriasis in all stages of operation and 33 eyes (89. 2%) did not show any obvious sign of inflammation. There was statistically significant difference between the two groups. No serious side effects occurred in the DS group.Conclusions : The DS展开更多
Objective:To investigate the potential synergistic activity of diclofenac with piperine and D-limonene in inducing apoptosis and cell cycle arrest in breast cancer MCF-7 cells.Methods:Molecular docking study was condu...Objective:To investigate the potential synergistic activity of diclofenac with piperine and D-limonene in inducing apoptosis and cell cycle arrest in breast cancer MCF-7 cells.Methods:Molecular docking study was conducted to evaluate the binding affinity of diclofenac with piperine and D-limonene against p53,Bax,and Bcl-2.The MTT assay was used to determine IC50,and the Chou-Talay method was used to determine the synergistic concentration of the combination treatment of diclofenac plus piperine and diclofenac plus D-limonene.Apoptosis detection,cell cycle arrest,reactive oxygen species production,and mitochondrial membrane potential were also investigated.Results:Diclofenac,piperine,and D-limonene showed potent binding affinity for p53,Bax,and Bcl-2.Diclofenac plus piperine and diclofenac plus D-limonene enhanced the formation of reactive oxygen species,which also had an effect on the mitochondrial membrane’s integrity and caused DNA fragmentation.Diclofenac plus piperine and diclofenac plus D-limonene arrested the cells in the sub-G0phase while drastically lowering the percentage of cells in the G2/M phase.Furthermore,the elevated apoptosis in the combined therapy was confirmed by annexin V/propidium iodide staining.Conclusions:The combined therapy prominently enhanced the antiproliferative and apoptotic effects on MCF-7 cells compared with treatment with diclofenac,piperine,and D-limonene alone.展开更多
Diclofenac sodium(DS) is a widely used nonsteroidal anti-inflammatory drug(NSAIDs).NSAIDs are poorly removed during standard wastewater treatment.The consequences of the presence of NSAIDs in rivers and lakes at 10-11...Diclofenac sodium(DS) is a widely used nonsteroidal anti-inflammatory drug(NSAIDs).NSAIDs are poorly removed during standard wastewater treatment.The consequences of the presence of NSAIDs in rivers and lakes at 10-11–10-8 mol/L are not yet established;therefore, ecotoxicologists have focused their efforts on studying the effect of lowconcentration NSAIDs on fish and hydrobionts, and also on predicting the potential risks to humans.Literature provides some information about the bioeffects of some NSAID solutions in low concentrations but there is no physicochemical explanation for these phenomena.Studying the physicochemical patterns of DS solutions in the low range of concentrations and establishing an interconnection between the solutions’ physicochemical properties and bioeffects can provide a conceptually new and important source of information regarding the unknown effects of DS.The physicochemical properties and action of DS solutions on Ceriodaphnia affinis cladocerans,Paramecium caudatum infusoria, Chlorella vulgaris unicellular green algae, as well as on the growth of the roots of Triticum vulgare wheat seeds, were studied in the calculated concentration range of 1 × 10-3–1 × 10-18 mol/L.The relationship between these phenomena was established using the certified procedures for monitoring the toxicity of natural water and wastewater.It was shown for the first time that water solutions of DS are dispersed systems in which the dispersed phase undergoes a rearrangement with dilution, accompanied by changes in its size and properties, which affects the nonmonotonic dependences of the system’s physicochemical properties and could cause nonmonotonic changes in action on hydrobionts in the low concentration range.展开更多
Two different salts of diclofenac,diclofenac sodium and diclofenac potassium,in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experiment...Two different salts of diclofenac,diclofenac sodium and diclofenac potassium,in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study.Biochemical and physiological parameters were also measured in both normal and dehydrated states.Diclofenac levels in plasma were determined using a validated reversed phase HPLC method.Primary kinetic parameters i.e.AUC0-∞,Cmax,Tmax and other disposition kinetics were obtained with non-compartmental procedure.Biochemical parameters i.e.packed cell volume,plasma glucose and total lipid concentration in dehydrated rabbits increased significantly.Plasma concentration of diclofenac sodium and diclofenac potassium decreased significantly in water deprived rabbits.In comparison,diclofenac potassium in normal and dehydrated state of the same group of rabbits showed a significantly increased plasma concentration when compared with diclofenac sodium.展开更多
This study evaluated whether the administration of a NSAID, sodium diclofenac, can promote alterations in the expression of Fos protein in central amygdala (CEA) and the lateral hypothalamus (LH) after 6 h of experime...This study evaluated whether the administration of a NSAID, sodium diclofenac, can promote alterations in the expression of Fos protein in central amygdala (CEA) and the lateral hypothalamus (LH) after 6 h of experimental tooth movement with a controlled force of 70 g, applied to the superior central incisors of rats. Adult male rats were anesthetized and divided into four groups: Control, no orthodontic appliance (OA);OA activated with 70 g;OA activated with 70 g and pretreated with diclofenac sodium (5 mg/kg, intramuscular);and diclofenac sodium alone. Six hours after the onset of the experiment the rats were reanesthetized and perfused with 4% paraformaldehyde. The brains were removed and fixed, and sections containing the CEA and LH were processed for Fos protein immunohistochemistry. The results show that in the control group, intramuscular injection of a ketamine/xylazine mixture did not induce IR-Fos cells in the CEA or LH. However, in the 70 g group, IR-Fos was the strongest observed展开更多
Liposomes are known to have considerable potential as drug carriers such as liposomal suspension, freeze dried and cream-based systems among many other liposomal formulations. In this study a new drug-in-adhesive patc...Liposomes are known to have considerable potential as drug carriers such as liposomal suspension, freeze dried and cream-based systems among many other liposomal formulations. In this study a new drug-in-adhesive patch was fabricated using liposome-based nanocarrier. Transfersomes as ultra-deformable liposomes are based on phosphatidylcholin 95% (phospholipon 90G) and phosphatidylcholin 50% (phosal 50PG) were prepared and further optimized in a final acrylic patch system for effective adhesion. The prepared liposomes were added to an acrylic adhesive to obtain a new hybrid transdermal patch termed as “lipo-drug-in-adhesive” patch system. The sodium diclofenac was selected as a model drug and the permeation of the drug across rat skin was evaluated (P > 0.05), using the lipo-drug-in-adhesive patch system with various percentages of transfersomes (4% - 8%w/w) and constant concentration of the drug (2% w/w). The peel strength and tack value of samples were also examined and quantified. The maximum flux of sodium diclofenac was observed in samples containing 8% (w/w) phosphatidylcholin 50%. The peel strength and tack value in samples containing phosphatidylcholin 50% were lower than those samples containing phosphatidylcholin 95%. It was observed that with increased amount of liposome in drug-in-adhesive patch system, the rate of skin permeation of the drug was also increased. It can be concluded that the developed lipo-drug-in-adhesive patch system enhances the drug release potential of transdermal delivering systems.展开更多
文摘Aim To study the exchange reaction characteristics of anion exchange resin for diclofenac sodium. Methods The drug-resin complexes were prepared by a batch method with diclofenac sodium as the model drug and the strong anion exchange resin (201 × 7) as the carrier. The effects of different forms (OH~ - and Cl~ - ) of the strong anion exchange resin, the particle size of the resin, and the reaction temperature on the exchange behavior were described. The exchange kinetic profiles were fitted. The related exc...
文摘The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.
基金supported by the National Natural Science Foundation of China(51578034,51878023)the Great Wall Scholars Training Program Project of Beijing Municipality Universities(CIT&TCD20180323)+3 种基金the Project of Construction of Innovation Teams and Teacher Career Development for Universities and Colleges Under Beijing Municipality(IDHT20170508)the Beijing Talent Project(2017A38)the Fundamental Research Funds for Beijing Universities(X18075/X18076/X18124/X18125/X18276)the Scientific Research Foundation of Beijing University of Civil Engineering and Architecture(KYJJ2017033/KYJJ2017008)~~
文摘Metal‐organic framework MIL‐100(Fe)and g‐C3N4 heterojunctions(MG‐x,x=5%,10%,20%,and 30%,x is the mass fraction of MIL‐100(Fe)in the hybrids)were facilely fabricated through ball‐milling and annealing,and characterized by powder X‐ray diffraction,Fourier transform infrared spectroscopy,thermogravimetric analysis,transmission electron microscopy,UV‐visible diffuse‐reflectance spectrometry,and photoluminescence emission spectrometry.The photocatalytic activities of the series of MG‐x heterojunctions toward Cr(VI)reduction and diclofenac sodium degradation were tested upon irradiation with simulated sunlight.The influence of different organic compounds(ethanol,citric acid,oxalic acid,and diclofenac sodium)as hole scavengers and the pH values(2,3,4,6,and 8)on the photocatalytic activities of the series of MG‐x heterojunctions was investigated.MG‐20%showed superior photocatalytic Cr(VI)reduction and diclofenac sodium degradation performance than did the individual MIL‐100(Fe)and g‐C3N4 because of the improved separation of photoinduced electron‐hole charges,which was clarified via photoluminescence emission and electrochemical data.Moreover,the MG‐x exhibited good reusability and stability after several runs.
文摘Objective:To observe the effects of Methyl Carboprost and Diclofenac Sodium on opening orifice of uterus and pain controlling in patients with uterine cervix cancer (UCC) when receiving intracavitary brachytherapy. Methods: Sixty patients with UCC of stage IIA-IIIB were divided into three groups randomly before receiving the intracavitary brachytherapy: the patients in group A received Methyl Carboprost in the hind fornix of the vagina, group B received Diclofenac Sodium in the anus, while group C was the control group. Results: The painlessness rates in groups A, B and C were 89.9%, 91.3% and 36.4%, respectively. The incidences of patients with relaxed uterus cervix in groups A, B and C were 91.7%, 85.9% and 48.9%, respectively. Conclusion: Methyl Carboprost and Diclofenac Sodium are useful in relaxing uterus cervix and pain controlling in patients with UCC when receiving intracavitary brachytherapy.
文摘Objective:To discuss the clinical study on Fengshi Qutong capsules combined with diclofenac sodium in the treatment of ankylosing spondylitis.Methods:80 patients who were treated for ankylosing spondylitis from June 2019 to June 2020 were selected and divided into two groups.The experimental group was treated with Fengshi Qutong capsules combined with diclofenac sodium,and the control group was treated with sulfasalazine enteric-coated tablets.Results:The treatment efficacy,VAS score,BASDAI score,BASFI score,CRP level,TNF-α level,IL-Iβ level,and the incidence of adverse reactions between the two groups were significantly different(P<0.05).Conclusion:The application of Fengshi Qutong capsules combined with diclofenac sodium in the treatment of patients with ankylosing spondylitis is beneficial to improve the treatment efficacy,reduce the levels of CRP,TNF-α,and IL-Iβ,reduce the incidence of adverse reactions,and reduce the VAS,BASDAI and BASFI scores,rendering it of important clinical value.
文摘Polymethylmethacrylate (PMMA) coated microcapsules of diclofenac sodium (DFS) were prepared by a modified wa-ter-in-oil-in-water (W1/O/W2) emulsion solvent evaporation method using sodium alginate (SAL) as a matrix material in the internal aqueous phase (W1).Their performance with respect to controlled release of the drug in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) were evaluated, and compared with non-matrix microcapsules prepared by the conventional W1/O/W2 emulsion solvent evaporation method. Scanning electron micrographs (SEM) revealed that all the microcapsules were discrete and spherical in shape;however, the surface porosity of the matrix microcap-sules appeared to be less than that of the non-matrix microcapsules. In case of non-matrix microcapsules, an increase in the volume of water in W1 phase resulted in decrease in the drug entrapment efficiency (DEE) along with increase in release of the drug in both SGF and SIF. While in case of matrix microcapsules increase in the amount of SAL in W1 phase and concentration of the coating polymer in organic phase led to increase in DEE of the matrix microcapsules and considerable decrease in the drug release in both SGF and SIF. No interaction between the drug and any of the polymers used to prepare microcapsules was evident from Fourier transform infra-red (FTIR) analysis. The matrix microcapsules prepared using higher concentration of SAL and PMMA released the drug following zero order or Case-II transport model. The matrix microcapsules appeared to be suitable for releasing lesser amounts of DFS in SGF and providing extended release in SIF.
文摘<Abstract>Purpose:To investigate the inhibitory effect of diclofenac sodium on rabbit corneal epithelial cells (RCECs) in vitro and explore its pharmacological mechanism. Methods: The fresh rabbit cornea was cultured to get the primary RCECs,and RCECs of passage 2 were used for the research. The cells were divided into experimental groups,the cells in which were incubated with different concentrations(18.18, 27.27, 36.36, 45.45, 54.55 μg/ml) of diclofenac sodium, and control group. The effect of diclofenac sodium on the proliferation of cells was measured by methyl thiazolyl thiazolium (MTT) assay 24, 48 and 72 h after incubation. While the RCECs were divided into experimental groups, the cells in which were incubated with 9 and 12.5 μg/ml diclofenac sodium, and control group. The cell cycle and apoptotic rate were observed by flow cytometer. Results:MTT assay showed that diclofenac sodium had obvious inhibitory effect on RCECs,and the inhibition rate was increasing along with the increase of the concentration of diclofenac sodium and the incubation time(P<0.05). Flow cytometer showed that after incubation with diclofenac sodium, the cells in G0/G1 phase were obviously increased, the apoptosis cusp and apoptotic rate were increased. Conclusion: Diclofenac sodium has obvious inhibitory effect on RCECs, which was dosage-dependent,and it may function by inducing cell apoptosis and ceasing cells cycles.
文摘This work aimed to find the effect of cranberry extract (75 and 150 mg/kg·b·w) and vit. C (1 g/kg·b·w orally) on renal toxicity induced by Diclofenac sodium in male albino rats. Treated rats with diclofenac sodium with a concentration 150 mg/kg·b·w, expressed a significant increase in several parameters includes, plasma total cholesterol, LDL-cholesterol, and triglyceride as well as renal nitric oxide (NO), tumor necrosis factor-alfa (TNF-α) and TBARS. In addition, a significant reduction in renal superoxide dismutase (SOD), GSH, catalase (CAT) and plasma HDL. The present results explain that, using cranberry extract and vit. C resulted in increasing the level of GSH, CAT and SOD as well as gene expression of renal SOD, CAT and IL-22 and reduce the level of TBARs significantly which led to preventing renal tissue damage. Our results also revealed that cranberry extract can protect DNA from damage as obtained from comet essay. TM-U was elevated in DCLF treated group when compared with normal. However cranberry extract was able to reduce this elevation in dose dependant manner. Histological features in H&E taken to different groups also mirrors this findings. DCLF causes many changes in renal tissue include infiltration by inflammatory cells, attenuated glomeruli, apoptosis in tubular epithelia.
文摘The release profiles of acidic form of diclofenac sodium adsorbed on mesoporous silicas (Silochrom and two samples of spherical silicas) were compared with the dissolution characteristics of the pure drug. Desorption of diclofenac sodium from impregnated silicas with various surface liophilicity and composites of silica with chitosan have been studied using rotating basket method in phosphate buffer, pH 6.8. Sedimentations of sodium diclofenac via adsorption and impregnation from alcohol solution on fumed silica and modified silicas with grafted aminopropyl and trimethylsilyl groups were carried out. Polymer-containing composites have been prepared by capsulation of silica particles with impregnated diclofenac sodium by protonated and deprotonated forms of chitosan. Effect of the silica surface nature on the active substance release rate was ascertained. Significant prolongation of diclofenac sodium release was detected in the case of application of hydrophobic silica as a carrier and protonated chitosan as a polymeric shell.
文摘Purpose: To determine the effect of 0.1% diclofenac sodium (DS) eyedrops made in China on preventing surgically induced miosis and inflammation. Methods: Seventy cases of cataract inpatients were randomly divided into two groups. DS eyedrops and normal saline as placebo were applied respectively 3h, 1h, 0.5h before operation and once every morning for 7 days after operation. The pupil diameter was measured five times at different stages during the extracapsular cataract extraction. The eyepain, photophobia, conjunctival injection, KP, aqueous flare and light reaction of pupil were observed once a day after operation for a week. Results: 37 eyes in DS group and 33 eyes in placebo group were included in the study. 32 of 37 eyes in DS group (86.5%) maintained mydriasis in all stages of operation and 33 eyes (89. 2%) did not show any obvious sign of inflammation. There was statistically significant difference between the two groups. No serious side effects occurred in the DS group.Conclusions : The DS
文摘Objective:To investigate the potential synergistic activity of diclofenac with piperine and D-limonene in inducing apoptosis and cell cycle arrest in breast cancer MCF-7 cells.Methods:Molecular docking study was conducted to evaluate the binding affinity of diclofenac with piperine and D-limonene against p53,Bax,and Bcl-2.The MTT assay was used to determine IC50,and the Chou-Talay method was used to determine the synergistic concentration of the combination treatment of diclofenac plus piperine and diclofenac plus D-limonene.Apoptosis detection,cell cycle arrest,reactive oxygen species production,and mitochondrial membrane potential were also investigated.Results:Diclofenac,piperine,and D-limonene showed potent binding affinity for p53,Bax,and Bcl-2.Diclofenac plus piperine and diclofenac plus D-limonene enhanced the formation of reactive oxygen species,which also had an effect on the mitochondrial membrane’s integrity and caused DNA fragmentation.Diclofenac plus piperine and diclofenac plus D-limonene arrested the cells in the sub-G0phase while drastically lowering the percentage of cells in the G2/M phase.Furthermore,the elevated apoptosis in the combined therapy was confirmed by annexin V/propidium iodide staining.Conclusions:The combined therapy prominently enhanced the antiproliferative and apoptotic effects on MCF-7 cells compared with treatment with diclofenac,piperine,and D-limonene alone.
文摘Diclofenac sodium(DS) is a widely used nonsteroidal anti-inflammatory drug(NSAIDs).NSAIDs are poorly removed during standard wastewater treatment.The consequences of the presence of NSAIDs in rivers and lakes at 10-11–10-8 mol/L are not yet established;therefore, ecotoxicologists have focused their efforts on studying the effect of lowconcentration NSAIDs on fish and hydrobionts, and also on predicting the potential risks to humans.Literature provides some information about the bioeffects of some NSAID solutions in low concentrations but there is no physicochemical explanation for these phenomena.Studying the physicochemical patterns of DS solutions in the low range of concentrations and establishing an interconnection between the solutions’ physicochemical properties and bioeffects can provide a conceptually new and important source of information regarding the unknown effects of DS.The physicochemical properties and action of DS solutions on Ceriodaphnia affinis cladocerans,Paramecium caudatum infusoria, Chlorella vulgaris unicellular green algae, as well as on the growth of the roots of Triticum vulgare wheat seeds, were studied in the calculated concentration range of 1 × 10-3–1 × 10-18 mol/L.The relationship between these phenomena was established using the certified procedures for monitoring the toxicity of natural water and wastewater.It was shown for the first time that water solutions of DS are dispersed systems in which the dispersed phase undergoes a rearrangement with dilution, accompanied by changes in its size and properties, which affects the nonmonotonic dependences of the system’s physicochemical properties and could cause nonmonotonic changes in action on hydrobionts in the low concentration range.
文摘Two different salts of diclofenac,diclofenac sodium and diclofenac potassium,in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study.Biochemical and physiological parameters were also measured in both normal and dehydrated states.Diclofenac levels in plasma were determined using a validated reversed phase HPLC method.Primary kinetic parameters i.e.AUC0-∞,Cmax,Tmax and other disposition kinetics were obtained with non-compartmental procedure.Biochemical parameters i.e.packed cell volume,plasma glucose and total lipid concentration in dehydrated rabbits increased significantly.Plasma concentration of diclofenac sodium and diclofenac potassium decreased significantly in water deprived rabbits.In comparison,diclofenac potassium in normal and dehydrated state of the same group of rabbits showed a significantly increased plasma concentration when compared with diclofenac sodium.
文摘This study evaluated whether the administration of a NSAID, sodium diclofenac, can promote alterations in the expression of Fos protein in central amygdala (CEA) and the lateral hypothalamus (LH) after 6 h of experimental tooth movement with a controlled force of 70 g, applied to the superior central incisors of rats. Adult male rats were anesthetized and divided into four groups: Control, no orthodontic appliance (OA);OA activated with 70 g;OA activated with 70 g and pretreated with diclofenac sodium (5 mg/kg, intramuscular);and diclofenac sodium alone. Six hours after the onset of the experiment the rats were reanesthetized and perfused with 4% paraformaldehyde. The brains were removed and fixed, and sections containing the CEA and LH were processed for Fos protein immunohistochemistry. The results show that in the control group, intramuscular injection of a ketamine/xylazine mixture did not induce IR-Fos cells in the CEA or LH. However, in the 70 g group, IR-Fos was the strongest observed
文摘Liposomes are known to have considerable potential as drug carriers such as liposomal suspension, freeze dried and cream-based systems among many other liposomal formulations. In this study a new drug-in-adhesive patch was fabricated using liposome-based nanocarrier. Transfersomes as ultra-deformable liposomes are based on phosphatidylcholin 95% (phospholipon 90G) and phosphatidylcholin 50% (phosal 50PG) were prepared and further optimized in a final acrylic patch system for effective adhesion. The prepared liposomes were added to an acrylic adhesive to obtain a new hybrid transdermal patch termed as “lipo-drug-in-adhesive” patch system. The sodium diclofenac was selected as a model drug and the permeation of the drug across rat skin was evaluated (P > 0.05), using the lipo-drug-in-adhesive patch system with various percentages of transfersomes (4% - 8%w/w) and constant concentration of the drug (2% w/w). The peel strength and tack value of samples were also examined and quantified. The maximum flux of sodium diclofenac was observed in samples containing 8% (w/w) phosphatidylcholin 50%. The peel strength and tack value in samples containing phosphatidylcholin 50% were lower than those samples containing phosphatidylcholin 95%. It was observed that with increased amount of liposome in drug-in-adhesive patch system, the rate of skin permeation of the drug was also increased. It can be concluded that the developed lipo-drug-in-adhesive patch system enhances the drug release potential of transdermal delivering systems.
