Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples

Romani, Luciana F.A.; Yoshida, María Irene; Gomes, Elionai Cassiana Lima; Machado, Renes R.; Rodrigues, Felipe F.; Coelho, Márcio M.; Oliveira, Marcos Antônio de; Freitas-Marques, Maria Betânia de; Gil, Rosane A. S. San; Mussel, Wagner da Nova

doi:10.1016/j.jpha.2017.12.006

Cited by 16 publications

(5 citation statements)

References 23 publications

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“…3 b). The 13 C NMR of meloxicam shows definitive peaks in region > 150 ppm as reported in literature [ 39 ]. The diminishment of peaks in 156 and 160 ppm ranges reported for meloxicam in the literature depicts the formation of complex through these groups [ 40 ].…”

Section: Resultssupporting

confidence: 64%

Synthesis, Spectroscopic and Biological Investigation of a New Ca(II) Complex of Meloxicam as Potential COX-2 Inhibitor

et al. 2022

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Drug development on basis of coordination compounds provides versatile structural and functional properties as compared to other organic compounds. In the present study, a new Ca(II) complex of meloxicam was synthesized and characterized by elemental analysis, FT-IR, UV–Vis, 13 C NMR, SEM–EDX, powder XRD and thermal analysis (TGA). The Ca(II) complex was investigated for its in vitro, in vivo biological activities and in silico docking analysis against COX-1 and COX-2. The spectral analysis indicates that the meloxicam acts as a deprotonated bidentate ligand (coordinated to the metal atom through the amide oxygen and the nitrogen atom of the thiazolyl ring) in the complex. SEM–EDX and powder XRD analysis depicted crystalline morphology of Ca(II) complex with a crystalline size of 32.86 nm. The in vitro biological activities were evaluated by five different antioxidant methods and COX inhibition assay, while in vivo activities were evaluated by carrageenan-, histamine- and PGE 2 -induced paw edema methods and acetic acid-induced writhing test. The Ca(II) complex showed prominent antioxidant activities and was found to be more selective toward COX-2 (43.77) than COX-1 as compared to meloxicam. It exhibited lower toxicity (LD 50 1000 mg/Kg) and significantly inhibited carrageenan- and PGE 2 -induced inflammation at 10 mg/Kg ( P < 0.05), but no significant effect was observed on histamine-induced inflammation. Moreover, Ca(II) complex significantly reduced the number of writhes induced by acetic acid ( P < 0.05). The in silico molecular docking data revealed that Ca(II) complex obstructed COX-2 (dock score 6438) more effectively than COX-1 (dock score 5732) as compared to meloxicam alone.

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Section: Resultssupporting

confidence: 64%

Synthesis, Spectroscopic and Biological Investigation of a New Ca(II) Complex of Meloxicam as Potential COX-2 Inhibitor

et al. 2022

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“…1668 cm −1 (C-O); 1614 cm −1 (benzene ring); 1428 cm −1 (C=O/OH); 1110 cm −1 (C-F)] 27,28 and meloxicam [e.g. 1620 cm −1 (N-H); 1550 cm −1 (thiazole ring); 1346 and 1264 cm −1 (sulfone)] 29,30 (Fig. 4).…”

Section: Resultsmentioning

confidence: 99%

Application of pulsed laser ablation (PLA) for the size reduction of non-steroidal anti-inflammatory drugs (NSAIDs)

Gera

Nagy

Smausz

et al. 2020

Sci Rep

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We studied the application of pulsed laser ablation (PLA) for particle size reduction in non-steroidal anti-inflammatory drugs (NSAIDs). Grinding of the poorly water-soluble NSAID crystallites can considerably increase their solubility and bioavailability, thereby the necessary doses can be reduced significantly. We used tablets of ibuprofen, niflumic acid and meloxicam as targets. Nanosecond laser pulses were applied at various wavelengths (KrF excimer laser, λ = 248 nm, FWHM = 18 ns and Nd:YAG laser, λ1 = 532 nm/λ2 = 1064 nm, FWHM = 6 ns) and at various fluences. FTIR and Raman spectra showed that the chemical compositions of the drugs had not changed during ablation at 532 nm and 1064 nm laser wavelengths. The size distribution of the ablated products was established using two types of particle size analyzers (SMPS and OPC) having complementary measuring ranges. The mean size of the drug crystallites decreased from the initial 30–80 µm to the submicron to nanometer range. For a better understanding of the ablation mechanism we made several investigations (SEM, Ellipsometry, Fast photography) and some model calculations. We have established that PLA offers a chemical-free and simple method for the size reduction of poorly water-soluble drugs and a possible new way for pharmaceutical drug preformulation for nasal administration.

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“…To our knowledge, this is the first report of meloxicam causing adverse effects on mouse behavior. We hypothesized that these adverse effects in mice might be related to variables in the meloxicam formulations 34,35 . Besides that, other variables might have interfered with, for example, phenotype differences between mouse strains 36,37 .…”

Section: Discussionmentioning

confidence: 99%

Assessment of general activity and anxietylike behavior in mice following tramadol and meloxicam administration for managing immediate post-operative pain

Antiorio¹,

Alemán-Laporte²,

Garcia-Gomes³

et al. 2022

Biol M Res & Tech

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After analgesic administration, we evaluated general activity in the Open-Field and anxiety-like behavior in the Elevated Plus Maze of vasectomized mice. We divided C57BL/6J male mice into eight groups: saline, three non-operated control groups treated with 10 mg/kg meloxicam, 20 mg/kg tramadol, or both intraperitoneally, and four vasectomized mice groups treated with the same analgesic protocol as the control groups. One group of vasectomized mice received both treatments and an additional 10 mg/kg lidocaine at the incision site. We conducted the vasectomy via scrotal approach under isoflurane inhalation anesthesia and performed behavioral tests after full anesthesia recovery. Mice treated with meloxicam demonstrated low ambulation, spontaneous activity, and rearing frequency. Mice treated with tramadol showed spontaneous behavior compared with the saline control. Due to behavior changes demonstrated by meloxicam controls, we were unable to identify whether meloxicam provided adequate analgesia. Vasectomized mice treated with tramadol showed general activity behavior similar to their control but displayed significantly less rearing, suggesting that they were under potential signs of pain or discomfort. In conclusion, the Open Field test and the Elevated Plus Maze can usefully pre-evaluate analgesic protocols to identify possible interference caused by adverse drug effects. For future directions, an appropriate regimen of meloxicam and tramadol for enhancing mice welfare post vasectomy should be better investigated.

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Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples

Cited by 16 publications

References 23 publications

Synthesis, Spectroscopic and Biological Investigation of a New Ca(II) Complex of Meloxicam as Potential COX-2 Inhibitor

Synthesis, Spectroscopic and Biological Investigation of a New Ca(II) Complex of Meloxicam as Potential COX-2 Inhibitor

Application of pulsed laser ablation (PLA) for the size reduction of non-steroidal anti-inflammatory drugs (NSAIDs)

Assessment of general activity and anxietylike behavior in mice following tramadol and meloxicam administration for managing immediate post-operative pain

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