Development and Evaluation of Two-Phase Gel Formulations for Enhanced Delivery of Active Ingredients: Sodium Diclofenac and Camphor.

The formulation of biphasic gels as potential semi-solid carriers for hydrophilic and lipophilic active substances is promising for the development of pharmaceutical preparations. The aim of this study was to design a stable bigel composition and to determine the influence of the organogel/hydrogel ratio on the gel's physical-chemical and structural-mechanical properties. The investigated compositions of organogel/hydrogel remained stable at ratios ranging from 5/95 to 40/60. After texture and microstructure analysis, bigels with 20/80 and 25/75 ratios were selected as carriers for the active ingredients, sodium diclofenac and camphor, for use as topical preparations for the treatment of muscle-joint inflammation and pain. Although other researchers have published data on the preparation and evaluation of bigels, there are no scientific results on the development of a two-phase gel with our proposed combination of APIs. Sodium diclofenac release was found to be higher when combined with camphor, which revealed the advantages of the biphasic formulation. The pseudoplastic behavior, thixotropy, and thermal stability of flow of the studied bigel samples was investigated by rheological analysis. Ongoing stability studies confirmed the minimal 6-month period.

Theoretical and Experimental Aspects of Sodium Diclofenac Salt Release from Chitosan-Based Hydrogels and Possible Applications.

Two formulations based on diclofenac sodium salt encapsulated into a chitosan hydrogel were designed and prepared, and their drug release was investigated by combining in vitro results with mathematical modeling. To understand how the pattern of drug encapsulation impacted its release, the formulations were supramolecularly and morphologically characterized by scanning electron microscopy and polarized light microscopy, respectively. The mechanism of diclofenac release was assessed by using a mathematical model based on the multifractal theory of motion. Various drug-delivery mechanisms, such as Fickian- and non-Fickian-type diffusion, were shown to be fundamental mechanisms. More precisely, in a case of multifractal one-dimensional drug diffusion in a controlled-release polymer-drug system (i.e., in the form of a plane with a certain thickness), a solution that allowed the model's validation through the obtained experimental data was established. The present research reveals possible new perspectives, for example in the prevention of intrauterine adhesions occurring through endometrial inflammation and other pathologies with an inflammatory mechanism background, such as periodontal diseases, and also therapeutic potential beyond the anti-inflammatory action of diclofenac as an anticancer agent, with a role in cell cycle regulation and apoptosis, using this type of drug-delivery system.

Characterization of cubosomes immobilized in hydrogels of hyaluronic acid and their use for diclofenac controlled delivery.

Cubosomes are dispersions of bicontinuous surfactant phases that constitute an assertive option to carry and release drugs and biomolecules, offering high efficiency of entrapment and specificity towards biological targets. This paper reports, for the first time to the best of our knowledge, the immobilization and characterization of cubosomes in chemically cross-linked oxi-hyaluronic acid and the evaluation of their use for controlled delivery of diclofenac, which is chosen as a model drug. Immobilized cubosomes prepared with phytantriol and bearing either negative or positive charges (in this case due to the addition of a cationic surfactant) were characterized by small angle X-ray scattering (SAXS) analysis and high-resolution confocal microscopy, confirming that their internal structure remains unaltered and that they appear uniformly distributed within the hydrogel matrix. Their release properties were assessed, and a limited leaching of the cubosomes from the hydrogel matrix with sustained release of the entrapped diclofenac was confirmed. These results enable the use of immobilized cubosomes as an attractive platform for biomedical applications, significantly extending the already promising features of cubosomes.

Antibiofilm potential over time of a tricalcium silicate material and its association with sodium diclofenac.

OBJECTIVES: The objectives of this study are to investigate, over time, the antimicrobial activity against polymicrobial biofilms and ability to inhibit biofilm formation, of Biodentine (BD) alone and with 5% and 10% sodium diclofenac (DC). MATERIAL AND METHODS: The antimicrobial activity of BD alone and modified with 5% and 10% DC against polymicrobial biofilm growth in dentin was determined by a modified direct contact test. The study groups were (1) BD; (2) BD + 5% DC; and (3) BD + 10% DC. The viability of microorganisms after 1 and 4 weeks was quantified by means of an ATP assay and flow cytometry. The antibiofilm efficacy of the materials, preventing polymicrobial biofilm formation over time, was assessed by confocal laser scanning microscopy (CLSM). RESULTS: The results obtained with both the ATP test and flow cytometry showed that BD alone and with 5% and 10% DC exerted antibiofilm activity with respect to the control, in the two evaluated times (p < 0.001). Comparison between groups showed a tendency of increased antimicrobial effect, both over time and depending on the DC concentration. These results coincide with those obtained in CLSM analysis, where efficacy increased with time and DC concentration. CONCLUSIONS AND CLINICAL RELEVANCE: Biodentine, over time, showed antimicrobial and antibiofilm efficacy on polymicrobial biofilms. The addition of 5% and 10% DC to BD enhanced this effect, in a concentration- and time-dependent manner.

Insights into efficient adsorption of the typical pharmaceutical pollutant with an amphiphilic cellulose aerogel.

An amphiphilic cellulose aerogel (HCNC-TPB/TMC) was fabricated by grafting 1,3,5-Tris (4-aminophenyl)benzene (TPB) and trimesoyl chloride (TMC) onto the aldehyde nanocellulose through Schiff alkali and substitution reaction. The obtained HCNC-TPB/TMC exhibited good morphology with cellulose fiber and owned abundant hydrophilic amino and carboxyl groups and hydrophobic aromatic groups. The batch adsorption experiments demonstrated that HCNC-TPB/TMC showed excellent adsorption performance (Qmax = 526.32 mg g-1) for sodium diclofenac (DCF), wide pH applicability (4-10) and outstanding stability and reusability. The DCF adsorption obeyed the pseudo-second-order kinetic model and the Langmuir isotherm, and underwent a spontaneous exothermic process. The main adsorption mechanisms involved electrostatic interaction, hydrogen bonds, π-π stacking interaction and hydrophobic effect. Importantly, the introduced carboxyl aromatic groups on TMC could effectively strengthen the hydrogen bonds and the π-π stacking between HCNC-TPB/TMC and DCF.

Electrochemical Method for Ease Determination of Sodium Diclofenac Trace Levels in Water Using Graphene-Multi-Walled Carbon Nanotubes Paste Electrode.

Sodium diclofenac (DCF) presence reported in water use cycle at various concentrations including trace levels necessitates continuous development of advanced analytical method for its determination. In this work, ease electrochemical methods for DCF determination based on voltammetric and amperometric techniques were proposed using a simple combination of graphene with multi-walled carbon nanotubes as paste electrode. Integration of the graphene with multi-walled carbon nanotubes enlarged the electroactive surface area of the electrode and implicitly enhanced the electrochemical response for DCF determination. On the basis of the sorption autocatalytic effect manifested at low concentration of DCF, we found that the preconcentration step applied prior to differential-pulsed voltammetry (DPV) and multiple-pulsed amperometry (MPA) allowed for the enhancement of the electroanalytical performance of the DCF electrochemical detections, which were validated by testing in tap water. The lowest limit of detection (LOD) of 1.40 ng·L-1 was found using preconcentration prior to DPV under optimized operating conditions, which is better than that reached by other carbon-based electrodes reported in the literature.

Adsorption of sodium diclofenac in aqueous medium using graphene oxide nanosheets.

In this work, the adsorption of sodium diclofenac (DCF) on graphene oxide nanosheets (GON) was evaluated. GON was synthesized by the modified Hummers method and characterized regarding its composition, morphology, and surface load. It was applied in batch adsorption tests. The process was evaluated from the kinetic, isothermal and thermodynamic properties, and parameters such as adsorbent mass and solution pH were optimized. The best working condition was observed at the natural pH of the solution (6.2) and 0.25 g L-1 adsorbent dosage. The pseudo-first-order and pseudo-second-order models were applied to verify the behaviour of the adsorption kinetics, and the adsorption isotherms were also developed at temperatures ranging from 25°C to 45°C. The isotherm models of Langmuir, Freundlich, and Temkim were applied to the equilibrium data. The thermodynamic parameters of enthalpy, entropy, and Gibbs free energy were evaluated to describe the behaviour of the adsorptive process. The maximum adsorption capacity of DCF at 25°C was 128.74 mg g-1 with a removal rate of 74% in 300 min. The process was favourable and spontaneous with adsorptive capacity decreasing with increasing temperature. In addition, an adsorption mechanism was proposed to show the possible bonds that occur between adsorbate and adsorbent and the interactions formed through the influence of pH.

Effects of phonophoresis with diclofenac linked gold nanoparticles in model of traumatic muscle injury.

The use of nanotechnology for administering drugs is a recent development that presents promising results. Therapeutic Pulsed Ultrasound (TPU) is one such therapeutic option and is widely used for treating soft tissue lesions. Thus, the objective of this study was to investigate the therapeutic effect of phonophoresis using diclofenac (DC) linked to gold nanoparticles (GNPs) in the skeletal muscle of rats used as a model of traumatic muscular injury. Wistar rats were divided into eight groups (N = 10): Sham, Muscle injury (MI), MI + TPU, MI + DC, MI + GNPs, MI + TPU + DC, MI + TPU + GNPs, and MI + TPU + DC-GNPs. The traumatic injury was performed in the gastrocnemius with a single direct traumatic impact via an injuring press. The animals received daily treatment for 5 consecutive days with TPU and gel with DC and/or GNPs. Two hours after the last treatment session, animals were euthanized and the gastrocnemius muscle surgically removed for histological and biochemical analysis. The groups exposed to some therapies (MI + TPU + DC, MI + TPU + GNPs and MI + TPU + DC-GNPs) showed reduced levels of pro-inflammatory cytokines, whereas an increase in anti-inflammatory cytokine levels was observed in the group exposed to all therapies combined (MI + TPU + DC-GNPs). Reactive species production and protein damage resulting from oxidative damage was lower for the group exposed to all tested therapies had lower production. Lower protein damage was also observed in the TPU + GNPs group. The group that underwent all tested therapies combined showed a significant increase in antioxidants compared to the MI group. During histological analysis, the MI group showed large amounts of cell infiltration and centralized nuclei, whereas the MI + TPU + DC-GNPs group showed structural improvements. Pain levels in the MI + TPU + DC-GNPs group were lower than those of the MI group. We believe that the association of TPU with DC linked to GNPs decreases the inflammation caused by traumatic muscle injury and accelerates tissue repair.

Efficient degradation of sodium diclofenac via heterogeneous Fenton reaction boosted by Pd/Fe@Fe3O4 nanoparticles derived from bio-recovered palladium.

Dehalogenation of emerging pollutants has attracted worldwide attention. In this study, novel bio-Pd/Fe@Fe3O4 nanoparticles (NPs) were proposed to boost the heterogeneous Fenton reaction for degradation of sodium diclofenac (DCF). Specifically, Enterococcus faecalis (E. faecalis) was employed to achieve bio-recovered palladium (bio-Pd). Results showed that expected preparation of bio-Pd/Fe@Fe3O4 NPs was confirmed by various characterization techniques. The prepared bio-Pd/Fe@Fe3O4 NPs were spherical morphology with average size of 9 nm. Under the optimum conditions, the removal efficiency of 10 mg/L DCF in 20 min and 40 min reached as high as 94.69% and 99.65%, respectively. The dechlorination and mineralization efficiencies of DCF were 85.16% and 59.21% in 120 min, respectively. The main degradation pathway of DCF was complete mineralization with the final products CO2, chloride ions and H2O. The improvement of dechlorination efficiency was ascribed to the accelerated corrosion of nano zero valent iron (nZVI) by Pd/Fe galvanic effect and the rise of active hydrogen. Meanwhile, more ferrous ions were released into this solution, resulting in the higher heterogeneous Fenton reaction rate driven by bio-Pd/Fe@Fe3O4 NPs. Therefore, the findings suggested that bio-Pd/Fe@Fe3O4 NPs were effective catalysts for DCF dechlorination and mineralization. The work provided a novel strategy for degradation of halogen-containing environmental pollutants.

A new azo-azomethine sensor for detection of CN- and AcO- anions: Highly selective chemosensor for naked eye detection of sodium diclofenac.

New azo-azomethine sensor, HL, has been synthesized and characterized using standard spectroscopic methods. HL was found to sense CN- and AcO- in DMSO and semi-aqueous media over other anions such as F-, Cl-, Br-, I-, H2PO4- and HSO4-. The anions recognition ability of HL was also evaluated using UV-Vis absorption and 1H NMR spectroscopy. Importantly, HL can detect CN- and AcO- in DMSO even at 0.7 ppm and 1.3 ppm, respectively. The binding stoichiometry between HL and the mentioned anions was found to be 1:1 with binding constants of 8.81 × 103 M-1 and 3.64 × 104 M-1 for CN- and AcO-, respectively. Successfully, HL was used for the detection of sodium diclofenac over the other opiate drugs such as codeine phosphate, noscapine hydrochloride, papaverine hydrochloride, and morphine sulfate. The designed chemosensor has also shown highly promising results for the qualitative and quantitative detection of sodium diclofenac in oral pills.

Dynamics of biochemical markers of connective tissue metabolism in patients with knee osteoarthritis during conservative treatment with laser therapy.

OBJECTIVE: Introduction: The biochemical markers of the connective tissue metabolism in blood serum may characterize the disturbances in inflammatory, destructive processes, and also serve the criteria for diagnostic evaluation of the state of cartilage and bone tissue of the joints in knee osteoarthritis to control the effectiveness of conservative treatment. The aim: determination of biochemical markers of connective tissue metabolism in the blood of patients with the 1st and 2nd stages of knee osteoarthritis in order to prove the effectiveness of the complex conservative treatment of patients with the use of low-intensity infrared laser radiation. PATIENTS AND METHODS: Materials and methods: During the study we examined 80 patients with the 1st and 2nd stages of knee osteoarthritis according to the Kellgren and Lawrence classification. Some patients were prescribed diclofenac sodium and glucosamine hydrochloride, others were prescribed an additional course of laser therapy. RESULTS: Results: At the end of the treatment the group of patients with knee osteoarthritis who were treated with the use of laser therapy, diclofenac sodium and glucosamine hydrochloride, showed a decrease in the content of the following blood serum components: glycoproteins (by 28.9 %), sialic acids (by 28.8 %), chondroitinsulfates (by 91.3 %) due to chondroitin-6-sulfate, activity of alkaline phosphatase (by 36.1 %) compared with the indicators before treatment. CONCLUSION: Conclusions: a more significant decrease in the inflammation and destruction of the cartilage tissue of the affected joints was observed during knee osteoarthritis treatment with the use of laser therapy than without it.

Utilização dos métodos automáticos em fluxos com detecção espectrofotométrica na determinação de diclofenaco de sódio em formulações farmacêuticas e fluidos corporais / Use of automatic methods in fluxes with spectrophotometric detection in the determination of diclofenac sodium in pharmaceutical formulations and body fluids

RESUMO Este trabalho descreveu e comparou quatro estudos entre si que utilizaram métodos automáticos em fluxo com detecção espectrofotométrica e a reação de oxidação do diclofenaco para determinar diclofenaco em formulações farmacêuticas e fluidos corporais. Para isso, utilizamos os seguintes artigos: Versatility of a multicommuted flow system in the spectrometric determination of three analytes, Sequential injection spectrophotometric method for the assay of anti-inflammatory diclofenac sodium in pharmaceutical preparations, Screening of conditions controlling spectrophotometric sequential injection analysis e Sequential injection spectrophotometric determination of diclofenac in urine and pharmaceutical formulations e detalhamos as metodologias empregadas, os resultados, conclusões obtidas e comparamos entre eles os limites de detecção, desvio padrão relativo e a frequência analítica. Os resultados mostraram diferenças significativas entre métodos empregados e a utilização do Sistema automático do tipo Análise por Injeção Sequencial, apesar deste possuir menor frequência analítica.

SUMMARY This study described and compared four studies that used automatic flow methods with spectrophotometric detection and the oxidation reaction of diclofenac to determine diclofenac in pharmaceutical formulations and body fluids. For this, the following articles were used: Versatility of a multicommuted flow system in the spectrometric determination of three analytes, Sequential injection spectrophotometric method for the assay of anti-inflammatory diclofenac sodium in pharmaceutical preparations, Screening of conditions controlling spectrophotometric sequential injection analysis and Sequential injection spectrophotometric determination of diclofenac in urine and pharmaceutical formulations and we detail the methodologies used, the results, the conclusions obtained and compare the limits of detection, relative standard deviation and analytical frequency. The results showed significant differences between the employed methods and the use of the Automatic System of the Sequential Injection Analysis type, although this one has a lower analytical frequency.

Enhanced Electrochemical Response of Diclofenac at a Fullerene⁻Carbon Nanofiber Paste Electrode.

The requirements of the Water Framework Directive to monitor diclofenac (DCF) concentration in surface water impose the need to find advanced fast and simple analysis methods. Direct voltammetric/amperometric methods could represent efficient and practical solutions. Fullerene⁻carbon nanofibers in paraffin oil as a paste electrode (F⁻CNF) was easily obtained by simple mixing and tested for DCF detection using voltammetric and amperometric techniques. The lowest limit of detection of 0.9 nM was achieved by applying square-wave voltammetry operated under step potential (SP) of 2 mV, modulation amplitude (MA) of 10 mV, and frequency of 25 Hz, and the best sensitivity was achieved by four-level multiple pulsed amperometry (MPA) that allowed in situ reactivation of the F⁻CNF electrode. The selection of the method must take into account the environmental quality standard (EQS), imposed through the "watchlist" of the Water Framework Directive as 0.1 µg·L-1 DCF. A good improvement of the electroanalytical parameters for DCF detection on the F⁻CNF electrode was achieved by applying the preconcentration step for 30 min before the detection step, which assured about 30 times better sensitivity, recommending its application for the monitoring of trace levels of DCF. The electrochemical behavior of F⁻CNF as a pseudomicroelectrode array makes it suitable for practical application in the in situ and real-time monitoring of DCF concentrations in water.

Biochemical markers of connective tissue metabolism in rats' blood serum with experimental knee osteoarthritis and their dynamics during conservative treatment.

OBJECTIVE: Introduction: There are many methods for diagnosis and treatment of knee joints osteoarthritis in modern orthopedics. The infrared radiation is one of the most popular and effective methods though it needs experimental substantiation on rats. The aim: Experimental definition of the effectiveness of the proposed method of conservative treatment of knee joints osteoarthritis using sodium diclofenac, glucosamine hydrochloride and infrared laser radiation, on the basis of biochemical markers of connective tissue metabolism in rats. PATIENTS AND METHODS: Materials and methods: Experimental studies were performed on 40 white male rats. A part of rats received infrared laser radiation in addition to diclofenac sodium and glucosamine hydrochloride. RESULTS: Results: Using a complex of infrared laser radiation and glucosamine hydrochloride and diclofenac sodium in conservative treatment of rats with experimentally induced knee joints osteoarthritis rats after 24 days of treatment. Treatment with the above-mentioned scheme resulted in a significant reduction in the content of glycoproteins (28.5%), chondroitin sulfates (26.1%), alkaline phosphatase activity (32.3%), and I and II fractions of glycosaminoglycans, namely chondroitin-6- (28.7%) and chondroitin-4-sulfate (40.3%). Moreover, these indicators of the studied markers approached the level of intact animals. CONCLUSION: Conclusions: Changes in biochemical markers of connective tissue in rats during experimental knee joints osteoarthritis indicated a higher efficiency of the treatment regimen with the use of low-intensity infrared laser radiation compared with exclusively drug therapy.

Tea waste derived activated carbon for the adsorption of sodium diclofenac from wastewater: adsorbent characteristics, adsorption isotherms, kinetics, and thermodynamics.

The present experimental study reports the performance of tea waste (TW) derived adsorbent for the adsorption of sodium diclofenac (SD) from aqueous solution (SD concentration = 10-50 mg/L). The waste-derived activated carbon was prepared by chemical activation process of raw waste using H2SO4, KOH, ZnCl2, and K2CO3 as activating agents (TW: activating agent = 1:1 by weight). Subsequently, the oven-dried material was carbonized at 600-°C temperature for 2 h. The synthesized adsorbents were porous and their Brunauer-Emmett-Teller (BET) surface area was ranged 115-865 m2/g. Among all synthesized adsorbents, the adsorbent activated by ZnCl2 exhibited the highest adsorption capacity (= 62 mg/g), though it was much lower compared to 91 mg/g obtained with commercial activated carbon (CAC) (SD concentration = 30 mg/L, adsorbent dose = 300 mg/L and initial wastewater pH = 6.47). SD equilibrium data could be described by Langmuir isotherm adequately, while pseudo-second-order rate model showed better fit to the time based adsorption data. Low activation energy of the adsorption process suggests the reaction to be temperature independent. Thermodynamic parameters showed the spontaneous and endothermic nature of adsorption process conducted in the presence of waste derived adsorbent.

Analgesic Effect of Topical Sodium Diclofenac before Retinal Photocoagulation for Diabetic Retinopathy: A Randomized Double-masked Placebo-controlled Intraindividual Crossover Clinical Trial.

PURPOSE: To evaluate the analgesic effect of topical sodium diclofenac 0.1% before retinal laser photocoagulation for diabetic retinopathy. METHODS: Diabetic patients who were candidates for peripheral laser photocoagulation were included in a randomized, placebo-controlled, intraindividual, two-period, and crossover clinical trial. At the first session and based on randomization, one eye received topical sodium diclofenac 0.1% and the other eye received an artificial tear drop (as placebo) three times before laser treatment. At the second session, eyes were given the alternate drug. Patients scored their pain using visual analogue scale (max, 10 cm) at both sessions. Patients and the surgeon were blinded to the drops given. Difference of pain level was the main outcome measure. RESULTS: A total of 200 eyes of 100 patients were enrolled. Both treatments were matched regarding the applied laser. Pain sensation based on visual analogue scale was 5.6 ± 3.0 in the treated group and 5.5 ± 3.0 in the control group. The calculated treatment effect was 0.15 (95% confidence interval, -0.27 to 0.58; p = 0.486). The estimated period effect was 0.24 (p = 0.530) and the carryover effect was not significant (p = 0.283). CONCLUSIONS: Pretreatment with topical sodium diclofenac 0.1% does not have any analgesic effect during peripheral retinal laser photocoagulation in diabetic patients.

Analgesic Effect of Topical Sodium Diclofenac before Retinal Photocoagulation for Diabetic Retinopathy: A Randomized Double-masked Placebo-controlled Intraindividual Crossover Clinical Trial

PURPOSE: To evaluate the analgesic effect of topical sodium diclofenac 0.1% before retinal laser photocoagulation for diabetic retinopathy. METHODS: Diabetic patients who were candidates for peripheral laser photocoagulation were included in a randomized, placebo-controlled, intraindividual, two-period, and crossover clinical trial. At the first session and based on randomization, one eye received topical sodium diclofenac 0.1% and the other eye received an artificial tear drop (as placebo) three times before laser treatment. At the second session, eyes were given the alternate drug. Patients scored their pain using visual analogue scale (max, 10 cm) at both sessions. Patients and the surgeon were blinded to the drops given. Difference of pain level was the main outcome measure. RESULTS: A total of 200 eyes of 100 patients were enrolled. Both treatments were matched regarding the applied laser. Pain sensation based on visual analogue scale was 5.6 ± 3.0 in the treated group and 5.5 ± 3.0 in the control group. The calculated treatment effect was 0.15 (95% confidence interval, −0.27 to 0.58; p = 0.486). The estimated period effect was 0.24 (p = 0.530) and the carryover effect was not significant (p = 0.283). CONCLUSIONS: Pretreatment with topical sodium diclofenac 0.1% does not have any analgesic effect during peripheral retinal laser photocoagulation in diabetic patients.

Effects of Pipemidic Acid, Phenazopyridine HCL and Sodium Diclofenac on Pain Perception Following Endoscopic Urological Surgery: Double-blinded Randomized-Controlled Trial.

AIM: to evaluate the analgesic effect, the side effects and the safety of analgesics following endoscopic urological procedure. METHODS: eighty patients who underwent endoscopic urological surgery at Kardinah Hospital, Tegal from June to July 2015 were divided into four groups. The experimental group was administered analgesic for 4 days pipemidic acid (A) 400 mg bid, or phenazopyridine (B) 200 mg tid, or sodium diclofenac (C) 50 mg bid and the control (D) group was administered placebo tid for 4 days. The analgesic effects were assessed using Visual Analog Scale (VAS). Association between variables was assessed using Cramers V and Kruskall Wallis. RESULTS: the endoscopic urological procedures consisted of 30 patients for URS, 6 patients for lithotripsy, 17 patients for TURP, 24 patients for removal JJ stent and 3 patients for cystoscopy. The mean age of group A, B, C and D (control) was 50.1 (13.7), 50.7 (14.8), 49.1 (13.4), and 49.6 (14.3) years, respectively, and follow-up period was 7 days. The VAS score in all experimental groups was less than control group on day 1 to 7 following endoscopic urological procedures (p<0.05). In the experimental group, there was no difference between groups B and C (p>0.05). Group A demonstrated a more favourable analgesic effect than B and C (p<0.05). No serious side effects were detected in any of the cases. CONCLUSION: we conclude that oral analgesics are effective for pain relief following endoscopic urological surgery. Pipemidic acid was found to have a superior analgesic effect than phenazopyridine HCl and sodium diclofenac.

Tabernaemontana catharinensis ethyl acetate fraction presents antinociceptive activity without causing toxicological effects in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Tabernaemontana catharinensis (Apocynaceae) is a medicinal plant used for the treatment of painful and inflammatory disorders. Here, we investigated the antinociceptive potential of the ethyl acetate fraction (Eta) from T. catharinensis leaves and assessed its toxic effects in mice to validate its popular use. MATERIALS AND METHODS: Adult male Swiss mice (30-35g) were used. The Eta antinociceptive effect (200-800mg/kg, oral route (p.o.)) was evaluated in the acetic acid, formalin, capsaicin and tail-immersion tests. Adverse effects were analyzed using rotarod and open-field tests, body temperature, biochemical analysis and gastric lesions assessment. To evaluate the acute (OECD 423) or sub-acute (OECD 407) toxicity of the Eta, it was administered orally at a single (2000mg/kg) or repeated doses (100-400mg/kg/day for 28 days), respectively. Mortality, behavioral changes, biochemical and hematological parameters were evaluated. The Eta effect on cellular viability also was evaluated. RESULTS: Eta (200-800mg/kg) inhibited the nociception caused by acetic acid (93.9±1.5%), formalin (86.2±10.8%) or capsaicin (75.4±3.3%) without inducing gastric lesions. Moreover, Eta neither altered the body temperature, biochemical parameters, nor forced or spontaneous locomotor activity of mice. The acute administration of the Eta (2000mg/kg) promoted a decrease in blood glucose levels and alanine aminotransferase activity. In the sub-acute toxicity study, Eta increased the aspartate aminotransferase activity (400mg/kg) and platelet distribution width (200mg/kg). Furthermore, Eta did not alter the cellular viability in cortical slices. CONCLUSIONS: Eta presents antinociceptive effects and mild toxicity in mice. These results support its traditional use as a potential analgesic.

Evaluación del desempeño de los métodos analíticos aplicados en el diclofenaco sódico 100 mg retard de producción nacional / Evaluation of the performance of the analytical methods applied to Cuban-made 100mg retard sodium diclofenac

Introducción: el diclofenaco sódico es un derivado del ácido fenilácetico y pertenece al grupo de los antinflamatorios no esteroideos con propiedades antinflamatorios, analgésicas y antipiréticas pronunciadas. En la Farmacopea de los Estados Unidos (USP 36, 2013) aparece reportado los métodos analíticos para el control de calidad del diclofenaco sódico en el ingrediente farmacéutico activo y en las tabletas. Objetivos: evaluar el desempeño de los métodos analíticos que se emplean en el control de la calidad de cuantificación y los estudios de estabilidad del ingrediente farmacéutico activo; así como los ensayos de disolución de las tabletas de diclofenaco sódico 100 mg retard de producción nacional. Métodos: en la evaluación del desempeño del método analítico potenciométrico para la cuantificación del ingrediente farmacéutico activo se analizaron los parámetros de linealidad y de precisión (repetibilidad y precisión intermedia). Para el método cromatográfico aplicable a la cuantificación del ingrediente farmacéutico activo en el producto terminado se analizaron los parámetros de especificidad, precisión y exactitud. En el método espectrofotométrico empleado en el ensayo de disolución se tuvo en cuenta la especificidad, la precisión, la linealidad, la influencia del filtrado y la estabilidad de las soluciones analíticas. Resultados: la evaluación del desempeño realizada a los diferentes métodos analíticos, fueron satisfactorias, demostrando que son lineales, precisos y específicos en el rango de concentraciones estudiadas. Conclusiones: se demostró la confiabilidad de los métodos empleados en el control de la calidad y los estudios de estabilidad del ingrediente farmacéutico activo y de las tabletas de diclofenaco sódico 100 mg retard de producción nacional(AU)

Introduction: sodium dicloflenac is a phenylacetic acid derivate included in the non-steroidal anti-inflammatory group, with marked analgesic and antipyretic properties. The US Pharmacopeia (USP 36, 2013) reports the analytical methods for the quality control of sodium diclofenac in the active ingredient and in tablets. Objectives: to evaluate the performance of the analytical methods used in the quality control of quantitation and the stability studies of the active ingredient as well as the dissolution tests of the Cuban-made 100 mg retard sodium diclofenac. Methods: the evaluation of the performance of the potentiometric analytical method for quantitation of the active ingredient analyzed the parameters called linearity and precision (repeatability and intermediate precision). For the chromatographic method applicable to quantitation of the active ingredient in the finished product, parameters such as specificity, precision and accuracy were analyzed. The spectrophotometric method used in the dissolution test took into account specificity, precision, linearity, filtering effect and stability of the analytical solutions. Results: the evaluation of the performance of the different analytical methods was satisfactory and they proved to be linear, precise and specific in the range of studied concentrations. Conclusions: the reliability of the methods for the quality control and of the stability studies of the active ingredient and of Cuban-made 100 mg retard sodium diclofenac was demonstrated(AU)