Tolmetin 600mg tablets

BACKGROUND Various non-steroidal anti-inflammatory drugs (NSAIDs) have been used for juvenile idiopathic arthritis (JIA). However, the optimal method for JIA has not yet been developed. AIM To perform a systematic review and network meta-analysis to determine the optimal instructions. METHODS We searched for randomized controlled trials (RCTs) from PubMed, EMBASE, Google Scholar, CNKI, and Wanfang without restriction for publication date or language at August, 2023. Any RCTs that comparing the effectiveness of NSAIDs with each other or placebo for JIA were included in this network meta-analysis. The surface under the cumulative ranking curve (SUCRA) analysis was used to rank the treatments. P value less than 0.05 was identified as statistically significant. RESULTS We included 8 RCTs (1127 patients) comparing 8 different instructions including meloxicam (0.125 qd and 0.250 qd), Celecoxib (3 mg/kg bid and 6 mg/kg bid), piroxicam, Naproxen (5.0 mg/kg/d, 7.5 mg/kg/d and 12.5 mg/kg/d), inuprofen (30-40 mg/kg/d), Aspirin (60-80 mg/kg/d, 75 mg/kg/d, and 55 mg/kg/d), Tolmetin (15 mg/kg/d), Rofecoxib, and placebo. There were no significant differences between any two NSAIDs regarding ACR Pedi 30 response. The SUCRA shows that celecoxib (6 mg/kg bid) ranked first (SUCRA, 88.9%), rofecoxib ranked second (SUCRA, 68.1%), Celecoxib (3 mg/kg bid) ranked third (SUCRA, 51.0%). There were no significant differences between any two NSAIDs regarding adverse events. The SUCRA shows that placebo ranked first (SUCRA, 88.2%), piroxicam ranked second (SUCRA, 60.5%), rofecoxib (0.6 mg/kg qd) ranked third (SUCRA, 56.1%), meloxicam (0.125 mg/kg qd) ranked fourth (SUCRA, 56.1%), and rofecoxib (0.3 mg/kg qd) ranked fifth (SUCRA, 56.1%). CONCLUSION In summary, celecoxib (6 mg/kg bid) was found to be the most effective NSAID for treating JIA. Rofecoxib, piroxicam, and meloxicam may be safer options, but further research is needed to confirm these findings in larger trials with higher quality studies.

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Novel tolmetin derivatives 5a–f to 8a–c were designed, synthesised, and evaluated for antiproliferative activity by NCI (USA) against a panel of 60 tumour cell lines. The cytotoxic activity of the most active tolmetin derivatives 5b and 5c was examined against HL-60, HCT-15, and UO-31 tumour cell lines. Compound 5b was found to be the most potent derivative against HL-60, HCT-15, and UO-31 cell lines with IC50 values of 10.32 ± 0.55, 6.62 ± 0.35, and 7.69 ± 0.41 µM, respectively. Molecular modelling studies of derivative 5b towards the VEGFR-2 active site were performed. Compound 5b displayed high inhibitory activity against VEGFR-2 (IC50 = 0.20 µM). It extremely reduced the HUVECs migration potential exhibiting deeply reduced wound healing patterns after 72 h. It induced apoptosis in HCT-15 cells (52.72-fold). This evidence was supported by an increase in the level of apoptotic caspases-3, -8, and -9 by 7.808-, 1.867-, and 7.622-fold, respectively. Compound 5b arrested the cell cycle in the G0/G1 phase. Furthermore, the ADME studies showed that compound 5b possessed promising pharmacokinetic properties.

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The objective of the present study was to develop rectal mucoadhesive hydrogels loaded with Tolmetin Sodium, a non-steroidal anti-inflammatory drug, for prolonged duration of action and increased bioavailability. Fourteen formulae were prepared with different types and concentrations of polymers as hydroxypropylmethyl cellulose, hydroxylethyl cellulose, carboxymethyl cellulose and sodium alginate. Each formulation contain Tolmetin Sodium equivalent to 5% w/w active drug. The effect of the employed gel bases on pH, gel strength, mucoadhesion, viscosity and the in vitro release profile of drug was examined. In addition, hydrogel formulations were subjected to rheological and stability studies. The physicochemical characterization revealed that all hydrogels had a suitable pH (6.64-7.75) and gel strength (15.5-65.29 s) for rectal application. The in-vitro drug release from the formulations showed a controlled drug release pattern, reaching 72-92.6% after 8 h. The kinetic analysis of the release data revealed that the drug release from all tested hydrogel bases obeyed the diffusion mechanism. The degradation of Tolmetin Sodium from its rectal hydrogel formulations was found to be a zero-order reaction. All formulations except sodium alginate hydrogel were quite stable. Considering the in-vitro release, rheological properties and shelf life, (CMC; 2%w/w) hydrogel formula was the best among the studied formulations. Therefore, further histopathological and bioavailability studies were carried out to detect different pharmacokinetic parameters of the established formulations compared with commercially available capsules. Formula containing 2% CMC showed relative bioavailability 357.93%. Finally, good correlation was observed between in-vitro and in-vivo profile.

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• Modification of cellulose paper by in situ synthesis of metal-organic framework-5. • Bonding between functional groups on cellulose paper with organic ligand. • Cellulose/MOF-5 was used in the thin film solid-phase microextraction method . • Thin film showed a good ability to extraction of selective drugs in urine samples. • The method is effective, sensitive, cost-effective and have wide LDRs and low LODs. This work, reports the successful preparation a thin film by a simple and inexpensive process for quantification of a model analytes in the urine sample using HPLC-UV. To this end, cellulose paper was employed as a substrate for the in-situ synthesis of MOF-5, to increase the resistance of the prepared film. The prepared film can be reused 26 times with no reduction in its performance. The thin film prepared by MOF-5 modified cellulose substrate was utilized in thin film microextraction (TFME) method for the extraction and preconcentration of naproxen, aspirin, tolmetin, and celecoxib. Under optimal conditions, the linear dynamic range of the target analytes was 2–500 µg L − 1 with correlation coefficients (R 2 ) ranging from 0.9961 to 0.9990. Also, the limits of detection (LODs), the limits of quantification (LOQs) and relative standard deviation (RSD%) of the proposed method for selected analytes ranged between 0.57 and 0.77 µg L − 1 , 1.7 to 2.3 and 3.5 % to 6.2 %, respectively. Moreover, relative recoveries varied from of 94 % to 108 %, indicating the absence of matrices effect in the proposed method. Eventually, the TFME was successfully used for the extraction of selected analytes from urine samples.

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An aqueous colloidal suspension of gold nanoparticles (AuNPs) may be condensed into a thin fractal film at the polarizable liquid-liquid interface formed between two immiscible electrolyte solutions upon injection of millimolar concentrations of sodium chloride to the aqueous phase. By adjusting the interfacial polarization conditions (negative, intermediate, and positive open-circuit potentials), the morphology of the film is modified, resulting in unique surface plasmon properties of the film, which enable in situ surface-enhanced Raman spectroscopy (SERS). Intense SERS signals are observed at the polarizable liquid-liquid interface when micromolar concentrations of tolmetin, a nonsteroidal anti-inflammatory drug, are entrapped in the AuNP fractal film. The change in the signal intensity, averaged over multiple spectra, with respect to the concentration of tolmetin, depends on the polarization conditions and suggests the presence of chemical-induced damping effects on the surface plasmons of the gold film.

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Tolmetin sodium (TOL) is a non-steroidal anti-inflammatory drug used to treat arthritis. Potentiometric ion selective electrodes (ISEs) bypass sample pre-treatment, high-tech apparatus, and toxic chemicals. The current study aimed to develop and validate a potentiometric analyser for the direct assay of TOL in pharmaceutical dosage form and human plasma. We designed an experimental approach to determine the factors that affect the performance of the developed sensor. A solid contact glassy carbon electrode was utilized as a support for the developed sensor. The interaction of TOL with several ionophore was studied using molecular docking. The optimized sensor was fabricated using dioctyl phthalate as plasticizer, tetra dodecyl ammonium bromide as anion exchanger, and β cyclodextrin as ionophore.The sensor achieved −58.78 Nernstian response within 1.00 × 10 −2 –2.00 × 10 −6 mol l −1 linear range, 1.56 × 10 −6 mol l −1 LOD, and fast response within 7 s. The greenness of the proposed method was assessed using the Analytical Eco-scale and the “Green Analytical Procedure Index” (GAPI) metric tools and compared with the reported methods and gained high scores. The proposed method has several advantages in encouraging quality control and clinical labs to routinely use the developed sensor in the assay of TOL in pharmaceutical dosage forms and human plasma.

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Herein, a reliable and sensitive method for the determination of tolmetin in biological samples was developed by combining solid-liquid hollow fiber liquid phase microextraction (HF-LPME) method with electromembrane extraction (EME) followed by high-performance liquid chromatography with UV detection (HPLC-UV), to enable safe and effective therapeutic monitoring. The proposed method performance was significantly enhanced through incorporating of MOF-199, synthesized via the solvothermal method and characterized by FE-SEM, XRD, FT-IR and BET analyses. Optimization of key extraction parameters was initially performed using the one-at-a-time method, while other parameters were systematically optimized through experimental design to achieve high sensitivity and reproducibility. Under the optimal condition (1-octanol as supported liquid membrane (SLM) solvent, 40 V as applied voltage, donor phase pH of 9.0, acceptor phase pH of 12.7, stirring rate of 400 rpm, extraction time of 5 min and MOF-199 loading of 4 mg mL −1 ) the method yielded linear dynamic ranges of 1–200 µg L −1 (water and urine matrices) and 2–100 µg L −1 (plasma matrix), with correlation coefficients (r²) above 0.9926. The limits of detection were 0.34, 0.38 and 0.41 µg L −1 in water, urine, and plasma, respectively. The method showed relative recovery rates between 90 % and 100 % in real plasma and urine samples. Additionally, the method attained a Blue Applicability Grade Index (BAGI) score of 67.5, confirming its high applicability and resource-efficient design. This approach offers high sensitivity, short extraction time, and excellent selectivity and reproducibility, making it well suited for trace analysis of tolmetin in complex matrices. • This study introduces a hybrid method by integrating solid-liquid HF-LPME with EME. • Incorporating MOF-199 into HF greatly enhances the tolmetin extraction efficiency. • This method showcasing its practical application in biological analysis.

Abstract licence: CC BY-NC-ND