Exchange Reaction Characteristics of Anion Exchange Resin for Diclofenac Sodium

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...

Pharmacokinetics and Relative Bioavailability ofsustained-release Tablets of Diclofenac Sodiumin Male Volunteers

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.

Enhanced photocatalytic Cr(Ⅵ) reduction and diclofenac sodium degradation under simulated sunlight irradiation over MIL-100(Fe)/g-C_3N_4 heterojunctions

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.

Polymethylmethacrylate Coated Alginate Matrix Microcapsules for Controlled Release of Diclofenac Sodium

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.

Inhibitory Effect of Diclofenac Sodium on the Proliferation of Rabbit Corneal Epithelial Cells in vitro

<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.

A New Liposomal-Drug-in-Adhesive Patch for Transdermal Delivery of Sodium Diclofenac

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.

Effects of Sodium Diclofenac on the Distribution of Fos Protein in Central Amygdala and Lateral Hypothalamus during Experimental Tooth Movement in Rats

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

Clinical analysis on the analgesic effect of Methyl Carboprost and Diclofenac Sodium for intracavitary brachytherapy

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.

Controlled Release of Diclofenac Sodium from Silica-Chitosan Composites

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.

Protective Effect of Cranberry Extracts against Oxidative Stress and DNA Damage Induced by Diclofenac Sodium in Kidney of Male Albino Rate

This work aimed to find the effect of cranberry extract (75 and 150 mg/kg&middot;b&middot;w) and vit. C (1 g/kg&middot;b&middot;w orally) on renal toxicity induced by Diclofenac sodium in male albino rats. Treated rats with diclofenac sodium with a concentration 150 mg/kg&middot;b&middot;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.

Combinatorial effect of diclofenac with piperine and D-limonene on inducing apoptosis and cell cycle arrest of breast cancer cells

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.

Clinical Study on Treatment to Ankylosing Spondylitis with Fengshi Qutong Capsule-Diclofenac Sodium Combination

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.

Clinical Study of Diclofenac Sodium Eyedrops Used before and after Cataract Operation

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

UiO-66-NH_(2)/SiO_(2)-ZrO_(2)杂化陶瓷纳滤膜的制备及性能研究

将UiO-66-NH_(2)晶体加入SiO_(2)-ZrO_(2)溶胶中,通过溶胶-凝胶法在陶瓷载体上制备出UiO-66-NH_(2)/SiO_(2)-ZrO_(2)膜,利用UiO-66-NH_(2)的多孔结构和亲水基团改进SiO_(2)-ZrO_(2)膜的纳滤性能。考察了不同UiO-66-NH_(2)加入量对杂化膜纳滤双氯芬酸钠(DCF)水溶液的影响,并对杂化膜进行表征,以聚乙烯醇截留分子质量评价膜孔径。结果表明,在DCF的纳滤测试中,随着UiO-66-NH_(2)质量分数的增大,UiO-66-NH_(2)/SiO_(2)-ZrO_(2)膜水通量先增大后降低,但均高于未添加的SiO_(2)-ZrO_(2)膜,对DCF的截留率均保持在98.7%以上;最佳UiO-66-NH_(2)/SiO_(2)-ZrO_(2)掺杂为0.3时,杂化膜通量提高至4.8 L/(h·m^(2)),通量增加了84%。随着操作压力和料液温度的提高,膜通量增大,截留率变化较小。在70℃、0.6 MPa下,杂化膜通量达到14.25 L/(h·m^(2)),对DCF水溶液的截留率为98.1%。

生长抑素联合双氯芬酸钠对内镜逆行胰胆管造影术后轻中度胰腺炎的临床效果

目的:探究生长抑素联合双氯芬酸钠对内镜逆行胰胆管造影(ERCP)术后胰腺炎患者的临床价值。方法:将2022年3月—2024年3月在九江市第一人民医院经ERCP治疗后继发轻中度胰腺炎的患者86例,按随机数字表法将患者分为常规组和研究组,各43例。常规组给予抗感染、补充体液、控制饮食和胃肠道减压等常规基础治疗,研究组在此基础上联合生长抑素和双氯芬酸钠进行治疗。观察两组临床有效情况,比较两组血清淀粉酶(AMS)、脂肪酶指标;记录两组炎症因子[白细胞介素6(IL-6)和C反应蛋白(CRP)]水平变化和不良反应。结果:常规组临床总有效率[72.09%(31/43)]显著低于研究组[90.70%(39/43)],差异有统计学意义(P<0.05)。治疗前,两组AMS、脂肪酶指标比较,差异均无统计学意义(P>0.05);治疗后,两组AMS、脂肪酶指标较治疗前均有下降,且研究组下降均更显著,差异均有统计学意义(P<0.05)。治疗前,两组IL-6和CRP水平比较,差异均无统计学意义(P>0.05);治疗后,两组IL-6和CRP水平均较治疗前下降,且研究组下降均更显著,差异均有统计学意义(P<0.05)。两组不良反应发生率比较,差异无统计学意义(P>0.05)。结论:相较于常规疗法,生长抑素联合双氯芬酸钠对ERCP术后胰腺炎患者效果更显著,可以显著降低胰腺炎患者AMS、脂肪酶指标和炎症因子水平,且安全性好。

经皮神经电刺激联合通络祛痹膏外敷对膝骨性关节炎疗效及关节滑液免疫细胞的影响

目的:探究经皮神经电刺激(transcutaneous electrical nerve stimulation,TENS)联合通络祛痹膏外敷治疗膝骨性关节炎(knee osteoarthritis,KOA)疗效及对关节滑液免疫细胞和膝关节功能的影响。方法:将KOA患者60例按随机数字表法分为对照组A、对照组B及观察组各20例。对照组A予TENS治疗,对照组B予通络祛痹膏外敷+扶他林治疗,观察组予通络祛痹膏外敷+TENS治疗,各组均治疗6周。比较3组患者治疗前后关节滑液中白细胞介素1(interleukin-1,IL-1)、白细胞介素6(interleukin-6,IL-6)、肿瘤坏死因子α(tumor necrosis factor-α,TNF-α)、干扰素γ(interferon-γ,IFN-v)、一氧化氮(nitric oxide,NO)、超氧化物歧化酶(superoxide dismutase,SOD)和丙二醛(malondialdehyde,MDA)的表达水平,并采用疼痛视觉模拟量表(visual analogue score,VAS)评分和膝关节康复量表(lysholm knee score scale,LKSS)评分评估膝关节恢复情况。结果:治疗后观察组VAS评分低于对照组A及对照组B(P<0.05),LKSS评分高于对照组A及对照组B(P<0.05);治疗后观察组IL-1、IL-6、TNF-α、IFN-γ表达水平均降低,与对照组A及对照组B比较,差异有统计学意义(P<0.05);治疗后观察组NO、MDA表达水平降低,SOD表达水平升高,与对照组A及对照组B比较,差异有统计学意义(P<0.05)。结论:TENS联合通络祛痹膏治疗KOA疗效明显,止痛效果显著,能有效减轻患者关节炎症及氧化应激反应。

双氯芬酸钠胶囊联合运动康复治疗急性期原发性冻结肩的临床疗效观察

目的探讨及分析运动康复联合双氯芬酸钠胶囊应用于急性期原发性冻结肩的临床效果。方法选取2022年6月—2023年12月于北京大学深圳医院就诊的52例急性期原发性冻结肩患者作为研究对象。所有患者采用双氯芬酸钠双释放肠溶胶囊口服联合运动康复治疗。比较患者在治疗前及治疗后1个月的美国肩肘外科协会评分(American Shoulder and Elbow Surgeons Scale,ASES)、疼痛视觉模拟评分法(Visual Analog Scale,VAS)评分及肩关节活动度,并评估治疗的有效率及患者的满意度。结果所有患者治疗后1个月ASES评分、VAS评分、肩关节活动度均高于本组治疗前,差异有统计学意义(P<0.05)。治疗的有效率达94.23%,患者满意度为(7.88±1.43)分。结论对于急性期原发性冻结肩患者,使用双氯芬酸钠双释放肠溶胶囊治疗联合运动康复,能显著缓解患者的肩部疼痛并改善活动度,治疗有效率及患者满意度较高。

舒筋通络法推拿联合双氯芬酸钠治疗肩周炎疗效观察

目的:观察舒筋通络法推拿联合双氯芬酸钠治疗肩周炎的疗效。方法:将280例肩周炎患者按随机数字表法分为观察组和对照组各140例。对照组给予双氯芬酸钠治疗,同时配合肩部功能锻炼,观察组在对照组基础上联合舒筋通络法推拿治疗,两组均治疗4周。观察两组治疗前后肩关节功能、肩关节活动度、简化版McGill疼痛问卷(SF-MPQ)评分、实验室指标[P物质(SP)、前列腺素E_(2)(PGE_(2))、5-羟色胺(5-HT)]的变化情况,并评估疗效。结果:治疗后,两组疼痛评分、关节活动度(ROM)评分、日常生活能力(ADL)评分、肌力评分、肩关节局部形态(LF)评分、肩关节功能评价量表总分、肩关节活动度均改善(P<0.05),且观察组优于对照组(P<0.05)。治疗后,两组疼痛分级指数(PRI)评分、视觉模拟评分法评分(VAS)、当前疼痛强度(PPI)评分,以及SP、PGE_(2)、5-HT水平均低于治疗前(P<0.05),且观察组低于对照组(P<0.05)。观察组总有效率94.29%,对照组87.14%,观察组疗效优于对照组(P<0.05)。结论:舒筋通络法推拿联合双氯芬酸钠治疗可改善肩周炎患者的肩关节功能,增加肩关节活动度,减少疼痛介质的分泌,缓解肩关节疼痛。

芳基烷酸类NSAIDs四乙酰基葡萄糖衍生物的制备及抗炎活性

目的:制备3种NSAIDs(双氯芬酚钠,萘普生和吲哚美辛)的葡萄糖酯,考察其生物活性。方法:用均相反应法制备葡萄糖酯,用1H NMR、13C NMR、IR和MS确认结构,用小鼠耳肿胀法评价其抗炎活性。结果:用羧酸盐均相反应法和羧酸-有机碱均相反应法合成了3个乙酰基葡萄糖酯,收率为53%～67%;所合成的3个目标化合物其抗炎活性均高于原药,刺激性低于原药。结论:均相反应法制备糖酯简便易行,优于相转移催化法;糖酯化修饰可提高芳基烷酸类NSAIDs的生物活性,降低刺激性。

揿针治疗亚急性甲状腺炎临床观察

目的:观察揿针治疗亚急性甲状腺炎的临床疗效。方法:将110例亚急性甲状腺炎患者按照随机数字表法分为治疗组和对照组,每组各55例。对照组给予口服双氯芬酸钠缓释片治疗,治疗组在对照组治疗的基础上给予揿针治疗,不服用醋酸泼尼松片。观察两组患者治疗前后中医证候积分、减分率、甲状腺肿痛消失时间、血沉恢复正常时间、甲状腺摄碘率恢复正常时间、血清淀粉样蛋白A(serum amyloid A,SAA)、肿瘤坏死因子(tumor necrosis factor,TNF)-β、白细胞介素(interleukin,IL)-6及临床疗效、1年后复发率。结果:治疗组治疗后中医证候积分低于对照组,差异有统计学意义(P<0.05)。治疗组中医证候积分减分率为71.1%,对照组中医证候积分减分率为36.7%,治疗组高于对照组,差异有统计学意义(P<0.05)。治疗组治疗后SAA、TNF-β、IL-6水平低于对照组,差异有统计学意义(P<0.05)。治疗组治疗后甲状腺肿痛消失时间、血沉恢复正常时间、甲状腺摄碘率恢复正常时间短于对照组,差异有统计学意义(P<0.05)。治疗组有效率为100%,1年后复发率为3.6%,对照组有效率为90.9%,1年后复发率为16.4%,治疗组有效率高于对照组,1年后复发率低于对照组,差异有统计学意义(P<0.05)。结论:揿针治疗亚急性甲状腺炎,可以更快缓解患者临床症状,改善中医证候,降低SAA、TNF-β、IL-6水平和复发率。